Bifunctional compounds for cancer treatment
Bifunctional compounds targeting Fibroblast Activation Protein-α (FAP) enhance diagnostic imaging and therapeutic efficacy by increasing uptake and residence time in FAP-expressing cells, addressing the limitations of current treatments for FAP-associated diseases.
Patent Information
- Application Number
- PCT/US2025/031283
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-05-28
- Filing Date
- 2025-05-28
- Publication Date
- 2025-12-04
AI Technical Summary
Current treatments for diseases characterized by Fibroblast Activation Protein-α (FAP) expression, such as cancer and fibrosis, lack effective diagnostic and therapeutic agents that can selectively target and accumulate in FAP-expressing tissues.
Development of bifunctional compounds, including radiolabeled and bifunctional compounds, that combine a Chelator and FAP Ligand to enhance uptake and residence time in FAP-expressing cells, allowing for superior efficacy and selectivity in diagnosis and treatment.
The bifunctional compounds demonstrate increased uptake and residence time in FAP-expressing cells, improving diagnostic imaging and therapeutic outcomes for conditions like cancer.
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Abstract
Description
[0001]Attorney Docket No.: A2219-7000WO BIFUNCTIONAL COMPOUNDS FOR CANCER TREATMENT CLAIM OF PRIORITY The instant application claims priority to U.S. Application No.63 / 652,564, filed on May 28, 2024. The contents of the foregoing application are incorporated herein by reference in their entirety. SUMMARY The present disclosure features bifunctional compounds and related compositions that, inter alia, may be used in the diagnosis, imaging, and treatment of a disease, disorder, or condition, for example, a cancer, e.g., a cancer associated with expression of Fibroblast Activation Protein-α (FAP), as well as methods of use thereof. Additionally, such compounds can be useful in the diagnosis, imaging, and treatment of other conditions characterized by FAP expression, such as fibrosis, endometriosis, inflammatory conditions or other conditions that involve tissue remodeling. In an embodiment, the bifunctional compounds described herein are bifunctional compounds of Formula (I) (e.g., Formulas (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g), (I-h), (I-i), (I-j), (I-k), (I-l), (I-m), (I-n), (I-o), (I-p)) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, or stereoisomers thereof. The present disclosure additionally provides methods of using the bifunctional compounds of the disclosure (e.g., compounds of Formulas (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g), (I-h), (I-i), (I-j), (I-k), (I-l), (I-m), (I-n), (I- o), (I-p)) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers thereof, and compositions thereof, e.g., to treat cancer. In another aspect, the bifunctional compounds described herein may be used for the prevention and / or treatment of a disease, disorder, or condition, e.g., a disease, disorder or condition associated with the presence of FAP protein, e.g., overexpression of FAP protein. In some embodiments, the bifunctional compounds described herein (e.g., bifunctional compounds of Formulas (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g), (I-h), (I-i), (I-j), (I-k), (I-l), (I-m), (I-n), (I-o), (I-p)) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers thereof) and compositions thereof are used for the prevention and / or treatment of a proliferative disease, disorder, or condition (e.g., a disease, disorder, or condition characterized by unwanted cell proliferation, e.g., a cancer) in a subject. 1 Attorney Docket No.: A2219-7000WO In one aspect, the present disclosure provides radiolabeled and bifunctional compounds of Formula (I): a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein (i) the Chelator comprises a moiety capable of binding to an ion (e.g., a radiometal ion); (ii) L1 comprises a linker; (iii) the FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP); and x is 1, 2, 3, or 4. In another aspect, the present disclosure provides radiolabeled and bifunctional compounds of Formula (V): ate, hydrate Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP); and x is 1, 2, 3, or 4. In one aspect, the present disclosure provides compounds of Formula (VIII): O R3aR3bm alt, onocyclic o cyc c a y o e e oa y g, op o a y su s u e w - occu e ces o ; each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 2 Attorney Docket No.: A2219-7000WO haloalkyl, and C1-6 heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -NH(R7)-, or -OH; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In another aspect, the present invention provides pharmaceutical compositions comprising a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, and optionally a pharmaceutically acceptable excipient. In an embodiment, the pharmaceutical compositions described herein include an effective amount (e.g., a therapeutically effective amount, or amount effective for imaging applications) of a bifunctional compound of Formula (I) (e.g., a bifunctional compound of Formulas (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g), (I-h), (I-i), (I-j), (I-k), (I-l), (I-m), (I-n), (I- o), (I-p)), or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof. In another aspect, the present disclosure provides methods for preventing and / or treating a disease, disorder, or condition in a subject by administering a bifunctional compound of Formula (I) or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, or related compositions. In some embodiments, the disease or disorder is a proliferative disease, disorder, or condition, or an inflammatory, or fibrotic condition. Exemplary proliferative diseases include cancer. In another aspect, the present disclosure provides compositions for use in preventing and / or treating and / or imaging disease, disorder, or condition in a subject by administering a bifunctional compound of Formula (I) (e.g., a bifunctional compound of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g), (I-h), (I-i), (I-j), (I-k), (I-l), (I-m), (I-n), (I-o), (I-p)) or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, or related compositions. In some embodiments, the disease or disorder is a proliferative disease, disorder, or condition. Exemplary proliferative diseases include cancer. The details of one or more embodiments of the invention are set forth herein. Other features, objects, and advantages of the invention will be apparent from the Brief Description of 3 Attorney Docket No.: A2219-7000WO the Drawings, Detailed Description, the Examples, and the Claims. BRIEF DESCRIPTION OF THE DRAWINGS FIGS.1A-1B demonstrate the tumor uptake of specified68Ga-compounds in FAP- positive tumor (HT1080-FAP) bearing mice. FIG.1A are68Ga-PET imaging showing biodistribution of specified68Ga-compounds (Compounds 101, 102, 103, 106, 107, 108, 109, 110, 111, 112) at 4 hours post-injection. FIG.1B is a bar graph depicting the tumor uptake (as % ID / g) of specified68Ga-compounds (Compounds 101, 102, 103, 106, 107, 108, 109, 110, 111, 112) at 4 hours post-injection. FIGS.2A-2B are86Y-PET imaging and biodistribution study of86Y-Compound 109. FIG.2A is a86Y-PET FAP-HT1080 xenograft image showing biodistribution of Y-Compound 109 at 6h and 48h. FIG.2B is a bar graph depicting the biodistribution of86Y-Compound 109 (as % ID / g) at 48 hours post-injection. FIGS.3A-3B illustrate86Y-PET imaging and tumor uptake of the specified compounds. FIG.3A is a86Y-PET FAP-HT1080 xenograft image showing biodistribution of specified86Y- compounds (Compounds 109, 112, 116, 119, and 120) at 48 hours post-injection. FIG.3B is a bar graph depicting the tumor uptake (as % ID / g) of specified86Y-compounds (Compounds 109, 112, 116, 119, and 120) at 48 hours post-injection. FIGS.4A-4B depict86Y-PET imaging and biodistribution study of86Y-Compound 112. FIG.4A is a86Y-PET FAP-HT1080 xenograft image showing biodistribution of86Y-Compound 112 at 1h, 4h, and 48h. FIG.4B is a bar graph depicting the biodistribution of86Y-Compound 112 (as %ID / g) at 48 hours post-injection. FIGS.5A-5B depict86Y-PET imaging and biodistribution study of86Y-Compound 119. FIG.5A is a86Y-PET FAP-HT1080 xenograft image showing biodistribution of86Y-Compound 119 at 1h, 4h, and 48h. FIG.5B is a bar graph depicting the biodistribution of86Y-Compound 119 (as %ID / g) at 48 hours post-injection. DETAILED DESCRIPTION The present disclosure features bifunctional compounds, such as radiolabeled compounds, for the treatment of a disease, disorder, or condition, e.g., such as cancer. Without being bound by theory, the inventors have shown that the bifunctional compounds described herein, e.g., 4 Attorney Docket No.: A2219-7000WO radiolabeled compounds of Formula (I) or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, demonstrate an increased uptake by a cancer cell or tissue (e.g., a tumor), thus increasing the residence time of the bifunctional compounds bearing a radioisotope (e.g., radiolabeled compounds) at the cancer cell or tissue (e.g., a tumor). This increased residence time allows for superior efficacy, selectivity, and potency of the bifunctional compounds (e.g., radiolabeled compounds) over other chemotherapeutic modalities. Selected Chemical Definitions Definitions of specific functional groups and chemical terms are described in more detail below. The chemical elements are identified in accordance with the Periodic Table of the Elements, CAS version, Handbook of Chemistry and Physics, 75thEd., inside cover, and specific functional groups are generally defined as described therein. Additionally, general principles of organic chemistry, as well as specific functional moieties and reactivity, are described in Thomas Sorrell, Organic Chemistry, University Science Books, Sausalito, 1999; Smith and March, March’s Advanced Organic Chemistry, 5thEdition, John Wiley & Sons, Inc., New York, 2001; Larock, Comprehensive Organic Transformations, VCH Publishers, Inc., New York, 1989; and Carruthers, Some Modern Methods of Organic Synthesis, 3rdEdition, Cambridge University Press, Cambridge, 1987. The abbreviations used herein have their conventional meaning within the chemical and biological arts. The chemical structures and formulae set forth herein are constructed according to the standard rules of chemical valency known in the chemical arts. When a range of values is listed, it is intended to encompass each value and sub–range within the range. For example, “C1-C6alkyl” or “C1-6alkyl” is intended to encompass, C1, C2, C3, C4, C5, C6, C1-C6, C1-C5, C1-C4, C1-C3, C1-C2, C2-C6, C2-C5, C2-C4, C2-C3, C3-C6, C3-C5, C3- C4, C4-C6, C4-C5, and C5-C6 alkyl. The following terms are intended to have the meanings presented therewith below and are useful in understanding the description and intended scope of the present invention. As used herein, the term “alkyl” refers to a radical of a straight–chain or branched saturated hydrocarbon group having from 1 to 24 carbon atoms (“C1-C24 alkyl”). In some embodiments, an alkyl group has 1 to 12 carbon atoms (“C1-C12alkyl”). In some embodiments, an alkyl group has 1 to 8 carbon atoms (“C1-C8alkyl”). In some embodiments, an alkyl group has 1 to 6 carbon atoms (“C1-C6 alkyl”). In some embodiments, an alkyl group has 2 to 6 carbon 5 Attorney Docket No.: A2219-7000WO atoms (“C2-C6 alkyl”). In some embodiments, an alkyl group has 1 carbon atom (“C1 alkyl”). Examples of C1-C6 alkyl groups include methyl (C1), ethyl (C2), propyl (C3) (e.g., n-propyl, isopropyl), butyl (C4) (e.g., n-butyl, tert-butyl, sec-butyl, isobutyl), pentyl (C5) (e.g., n-pentyl, 3- pentanyl, amyl, neopentyl, 3-methyl-2-butanyl, tertiary amyl), and hexyl (C6) (e.g., n-hexyl). Additional examples of alkyl groups include n–heptyl (C7), n–octyl (C8) and the like. Each instance of an alkyl group may be independently optionally substituted, i.e., unsubstituted (an “unsubstituted alkyl”) or substituted (a “substituted alkyl”) with one or more substituents; e.g., for instance from 1 to 5 substituents, 1 to 3 substituents, or 1 substituent. In certain embodiments, the alkyl group is unsubstituted C1–C10alkyl (e.g., –CH3). In certain embodiments, the alkyl group is substituted C1–C6alkyl. As used herein, the term “alkenyl” refers to a radical of a straight–chain or branched hydrocarbon group having from 2 to 24 carbon atoms, one or more carbon–carbon double bonds, and no triple bonds (“C2-C24alkenyl”). In some embodiments, an alkenyl group has 2 to 10 carbon atoms (“C2-C10 alkenyl”). In some embodiments, an alkenyl group has 2 to 8 carbon atoms (“C2-C8 alkenyl”). In some embodiments, an alkenyl group has 2 to 6 carbon atoms (“C2- C6alkenyl”). In some embodiments, an alkenyl group has 2 carbon atoms (“C2alkenyl”). The one or more carbon–carbon double bonds can be internal (such as in 2–butenyl) or terminal (such as in 1–butenyl). Examples of C2-C4 alkenyl groups include ethenyl (C2), 1–propenyl (C3), 2– propenyl (C3), 1–butenyl (C4), 2–butenyl (C4), butadienyl (C4), and the like. Examples of C2-C6alkenyl groups include the aforementioned C2–4alkenyl groups as well as pentenyl (C5), pentadienyl (C5), hexenyl (C6), and the like. Additional examples of alkenyl include heptenyl (C7), octenyl (C8), octatrienyl (C8), and the like. Each instance of an alkenyl group may be independently optionally substituted, i.e., unsubstituted (an “unsubstituted alkenyl”) or substituted (a “substituted alkenyl”) with one or more substituents e.g., for instance from 1 to 5 substituents, 1 to 3 substituents, or 1 substituent. In certain embodiments, the alkenyl group is unsubstituted C1–C10alkenyl. In certain embodiments, the alkenyl group is substituted C2–C6alkenyl. As used herein, the term “alkynyl” refers to a radical of a straight–chain or branched hydrocarbon group having from 2 to 24 carbon atoms, one or more carbon–carbon triple bonds (“C2-C24alkenyl”). In some embodiments, an alkynyl group has 2 to 10 carbon atoms (“C2-C10alkynyl”). In some embodiments, an alkynyl group has 2 to 8 carbon atoms (“C2-C8 alkynyl”). In 6 Attorney Docket No.: A2219-7000WO some embodiments, an alkynyl group has 2 to 6 carbon atoms (“C2-C6 alkynyl”). In some embodiments, an alkynyl group has 2 carbon atoms (“C2 alkynyl”). The one or more carbon– carbon triple bonds can be internal (such as in 2–butynyl) or terminal (such as in 1–butynyl). Examples of C2-C4 alkynyl groups include ethynyl (C2), 1–propynyl (C3), 2–propynyl (C3), 1– butynyl (C4), 2–butynyl (C4), and the like. Each instance of an alkynyl group may be independently optionally substituted, i.e., unsubstituted (an “unsubstituted alkynyl”) or substituted (a “substituted alkynyl”) with one or more substituents e.g., for instance from 1 to 5 substituents, 1 to 3 substituents, or 1 substituent. In certain embodiments, the alkynyl group is unsubstituted C2–10alkynyl. In certain embodiments, the alkynyl group is substituted C2–6alkynyl. As used herein, the term "haloalkyl," refers to a non-cyclic stable straight or branched chain, or combinations thereof, including at least one carbon atom and at least one halogen selected from the group consisting of F, Cl, Br, I, and At. The halogen(s) F, Cl, Br, I, and At may be placed at any position of the haloalkyl group. Exemplary haloalkyl groups include, but are not limited to: -CF3, -CCl3, -CH2-CF3, -CH2-CCl3, -CH2-CBr3, -CH2-CI3, -CH2-CH2-CH(CF3)-CH3, - CH2-CH2-CH(Br)-CH3, and -CH2-CH=CH-CH2-CF3. Each instance of a haloalkyl group may be independently optionally substituted, i.e., unsubstituted (an “unsubstituted haloalkyl”) or substituted (a “substituted haloalkyl”) with one or more substituents e.g., for instance from 1 to 5 substituents, 1 to 3 substituents, or 1 substituent. As used herein, the term “heteroalkyl”, refers to a non-cyclic stable straight or branched chain, or combinations thereof, including at least one carbon atom and at least one heteroatom selected from the group consisting of O, N, P, Si, and S, and wherein the nitrogen and sulfur atoms may optionally be oxidized, and the nitrogen heteroatom may optionally be quaternized. The heteroatom(s) O, N, P, S, and Si may be placed at any position of the heteroalkyl group. In certain embodiments, a heteroalkyl group refers to a saturated group having from 1 to 10 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1–10alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 9 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1–9 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 8 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1–8alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 7 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1–7 7 Attorney Docket No.: A2219-7000WO alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 6 carbon atoms and 1 or more heteroatoms within the parent chain (“heteroC1–6 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 5 carbon atoms and 1 or 2 heteroatoms within the parent chain (“heteroC1–5 alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 4 carbon atoms and 1or 2 heteroatoms within the parent chain (“heteroC1–4alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 3 carbon atoms and 1 heteroatom within the parent chain (“heteroC1–3alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 to 2 carbon atoms and 1 heteroatom within the parent chain (“heteroC1–2alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 1 carbon atom and 1 heteroatom (“heteroC1alkyl”). In some embodiments, a heteroalkyl group is a saturated group having 2 to 6 carbon atoms and 1 or 2 heteroatoms within the parent chain (“heteroC2–6 alkyl”). Unless otherwise specified, each instance of a heteroalkyl group is independently unsubstituted (an “unsubstituted heteroalkyl”) or substituted (a “substituted heteroalkyl”) with one or more substituents. In certain embodiments, the heteroalkyl group is an unsubstituted heteroC1–10 alkyl. In certain embodiments, the heteroalkyl group is a substituted heteroC1–10alkyl. Exemplary heteroalkyl groups include, but are not limited to: -CH2-CH2-O-CH3, -CH2-CH2-NH-CH3, -CH2-CH2-N(CH3)-CH3, -CH2-S-CH2- CH3, -CH2-CH2, -S(O)-CH3, -CH2-CH2-S(O)2-CH3, -CH=CH-O-CH3, -Si(CH3)3, -CH2-CH=N- OCH3, -CH=CH-N(CH3)-CH3, -O-CH3, and -O-CH2-CH3. Up to two or three heteroatoms may be consecutive, such as, for example, -CH2-NH-OCH3and -CH2-O-Si(CH3)3. Where "heteroalkyl" is recited, followed by recitations of specific heteroalkyl groups, such as –CH2O, – NRBRC, or the like, it will be understood that the terms heteroalkyl and –CH2O or –NRBRCare not redundant or mutually exclusive. Rather, the specific heteroalkyl groups are recited to add clarity. Thus, the term "heteroalkyl" should not be interpreted herein as excluding specific heteroalkyl groups, such as –CH2O, –NRBRC, or the like. Each instance of a heteroalkyl group may be independently optionally substituted, i.e., unsubstituted (an “unsubstituted heteroalkyl”) or substituted (a “substituted heteroalkyl”) with one or more substituents e.g., for instance from 1 to 5 substituents, 1 to 3 substituents, or 1 substituent. As used herein, “aryl” refers to a radical of a monocyclic or polycyclic (e.g., bicyclic or tricyclic) 4n+2 aromatic ring system (e.g., having 6, 10, or 14 π electrons shared in a cyclic array) having 6–14 ring carbon atoms and zero heteroatoms provided in the aromatic ring system 8 Attorney Docket No.: A2219-7000WO (“C6-C14 aryl”). In some embodiments, an aryl group has six ring carbon atom “C6 aryl”; e.g., phenyl). In some embodiments, an aryl group has ten ring carbon atoms (“C10 aryl”; e.g., naphthyl such as 1–naphthyl and 2–naphthyl). In some embodiments, an aryl group has fourteen ring carbon atoms (“C14 aryl”; e.g., anthracyl). An aryl group may be described as, e.g., a C6-C10- membered aryl, wherein the term “membered” refers to the non-hydrogen ring atoms within the moiety. Examples of aryl groups include, but are not limited to, phenyl, 1-naphthyl, 2-naphthyl, indenyl, tetrahydronaphthyl, and the like. The related term “aryl ring” likewise refers to a stable, aromatic, mono- or bicyclic ring having the specified number of ring carbon atoms. Each instance of an aryl group may be independently optionally substituted, i.e., unsubstituted (an “unsubstituted aryl”) or substituted (a “substituted aryl”) with one or more substituents. In certain embodiments, the aryl group is unsubstituted C6-C14 aryl. In certain embodiments, the aryl group is substituted C6-C14 aryl. As used herein, “heteroaryl” refers to a radical of a 5–10 membered monocyclic or bicyclic 4n+2 aromatic ring system (e.g., having 6 or 10 π electrons shared in a cyclic array) having ring carbon atoms and 1–6 ring heteroatoms provided in the aromatic ring system, wherein each heteroatom is independently selected from nitrogen, oxygen and sulfur (“5–10 membered heteroaryl”). The related term “heteroaryl ring” likewise refers to a stable, aromatic, mono- or bicyclic ring having the specified number of ring atoms and comprising one or more heteroatoms individually selected from nitrogen, oxygen and sulfur. In heteroaryl groups that contain one or more nitrogen atoms, the point of attachment can be a carbon or nitrogen atom, as valency permits. Heteroaryl bicyclic ring systems can include one or more heteroatoms in one or both rings. “Heteroaryl” also includes ring systems wherein the heteroaryl ring, as defined above, is fused with one or more aryl groups wherein the point of attachment is either on the aryl or heteroaryl ring, and in such instances, the number of ring members designates the number of ring members in the fused (aryl / heteroaryl) ring system. Bicyclic heteroaryl groups wherein one ring does not contain a heteroatom (e.g., indolyl, quinolinyl, carbazolyl, and the like) the point of attachment can be on either ring, i.e., either the ring bearing a heteroatom (e.g., 2–indolyl) or the ring that does not contain a heteroatom (e.g., 5–indolyl). A heteroaryl group may be described as, e.g., a 6-10-membered heteroaryl, wherein the term “membered” refers to the non-hydrogen ring atoms within the moiety. Each instance of a heteroaryl group may be independently optionally substituted, i.e., unsubstituted (an “unsubstituted heteroaryl”) or substituted (a “substituted 9 Attorney Docket No.: A2219-7000WO heteroaryl”) with one or more substituents e.g., for instance from 1 to 5 substituents, 1 to 3 substituents, or 1 substituent. Exemplary 5–membered heteroaryl groups containing one heteroatom include, without limitation, pyrrolyl, furanyl and thiophenyl. Exemplary 5–membered heteroaryl groups containing two heteroatoms include, without limitation, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, and isothiazolyl. Exemplary 5–membered heteroaryl groups containing three heteroatoms include, without limitation, triazolyl, oxadiazolyl, and thiadiazolyl. Exemplary 5–membered heteroaryl groups containing four heteroatoms include, without limitation, tetrazolyl. Exemplary 6–membered heteroaryl groups containing one heteroatom include, without limitation, pyridinyl. Exemplary 6–membered heteroaryl groups containing two heteroatoms include, without limitation, pyridazinyl, pyrimidinyl, and pyrazinyl. Exemplary 6– membered heteroaryl groups containing three or four heteroatoms include, without limitation, triazinyl and tetrazinyl, respectively. Exemplary 7–membered heteroaryl groups containing one heteroatom include, without limitation, azepinyl, oxepinyl, and thiepinyl. Exemplary 5,6– bicyclic heteroaryl groups include, without limitation, indolyl, isoindolyl, indazolyl, benzotriazolyl, benzothiophenyl, isobenzothiophenyl, benzofuranyl, benzoisofuranyl, benzimidazolyl, benzoxazolyl, benzisoxazolyl, benzoxadiazolyl, benzthiazolyl, benzisothiazolyl, benzthiadiazolyl, indolizinyl, and purinyl. Exemplary 6,6–bicyclic heteroaryl groups include, without limitation, naphthyridinyl, pteridinyl, quinolinyl, isoquinolinyl, cinnolinyl, quinoxalinyl, phthalazinyl, and quinazolinyl. Other exemplary heteroaryl groups include heme and heme derivatives. As used herein, the term “cycloalkyl” refers to a stable, saturated or unsaturated, non- aromatic, mono- or bicyclic (fused, bridged, or spiro) ring radical having the specified number of ring carbon atoms. The related term “carbocyclic ring” likewise refers to a stable, saturated or unsaturated, non-aromatic, mono- or bicyclic (fused, bridged, or spiro) ring having the specified number of ring carbon atoms. In some embodiments, a cycloalkyl group has 3 to 8 ring carbon atoms (“C3-C8 cycloalkyl”). In some embodiments, a cycloalkyl group has 3 to 6 ring carbon atoms (“C3-C6 cycloalkyl”). In some embodiments, a cycloalkyl group has 3 to 6 ring carbon atoms (“C3-C6cycloalkyl”). In some embodiments, a cycloalkyl group has 5 to 10 ring carbon atoms (“C5-C10cycloalkyl”). A cycloalkyl group may be described as, e.g., a C4-C7-membered cycloalkyl, wherein the term “membered” refers to the non-hydrogen ring atoms within the 10 Attorney Docket No.: A2219-7000WO moiety. Exemplary C3-C6 cycloalkyl groups include, without limitation, cyclopropyl (C3), cyclopropenyl (C3), cyclobutyl (C4), cyclobutenyl (C4), cyclopentyl (C5), cyclopentenyl (C5), cyclohexyl (C6), cyclohexenyl (C6), cyclohexadienyl (C6), and the like. Exemplary C3-C8cycloalkyl groups include, without limitation, the aforementioned C3-C6 cycloalkyl groups as well as cycloheptyl (C7), cycloheptenyl (C7), cycloheptadienyl (C7), cycloheptatrienyl (C7), cyclooctyl (C8), cyclooctenyl (C8), cubanyl (C8), bicyclo[1.1.1]pentanyl (C5), bicyclo[2.2.2]octanyl (C8), bicyclo[2.1.1]hexanyl (C6), bicyclo[3.1.1]heptanyl (C7), and the like. Exemplary C3-C10 cycloalkyl groups include, without limitation, the aforementioned C3-C8 cycloalkyl groups as well as cyclononyl (C9), cyclononenyl (C9), cyclodecyl (C10), cyclodecenyl (C10), octahydro–1H–indenyl (C9), decahydronaphthalenyl (C10), spiro[4.5]decanyl (C10), and the like. As the foregoing examples illustrate, in certain embodiments, the cycloalkyl group is either monocyclic (“monocyclic cycloalkyl”) or contain a fused, bridged or spiro ring system such as a bicyclic system (“bicyclic cycloalkyl”) and can be saturated or can be partially unsaturated. “Cycloalkyl” also includes ring systems wherein the cycloalkyl ring, as defined above, is fused with one or more aryl groups wherein the point of attachment is on the cycloalkyl ring, and in such instances, the number of carbons continue to designate the number of carbons in the cycloalkyl ring system. Each instance of a cycloalkyl group may be independently optionally substituted, i.e., unsubstituted (an “unsubstituted cycloalkyl”) or substituted (a “substituted cycloalkyl”) with one or more substituents. In certain embodiments, the cycloalkyl group is unsubstituted C3-C10cycloalkyl. In certain embodiments, the cycloalkyl group is a substituted C3-C10 cycloalkyl. As used herein, the term “heterocyclyl” refers to a stable, saturated or unsaturated, non- aromatic, mono- or bicyclic (fused, bridged, or spiro) ring radical having the specified number of ring atoms and comprising one or more heteroatoms individually selected from nitrogen, oxygen, sulfur, boron, phosphorus, and silicon. The related term “heterocyclic ring” likewise refers to a stable, saturated or unsaturated, non-aromatic, mono- or bicyclic (fused, bridged, or spiro) ring having the specified number of ring atoms and comprising one or more heteroatoms individually selected from nitrogen, oxygen, sulfur, boron, phosphorus, and silicon. In an embodiment, the specified number is C3–C12carbons. In heterocyclyl, groups that contain one or more nitrogen atoms, the point of attachment can be a carbon or nitrogen atom, as valency permits. A heterocyclyl group can either be monocyclic (“monocyclic heterocyclyl”) or a fused, bridged or 11 Attorney Docket No.: A2219-7000WO spiro ring system such as a bicyclic system (“bicyclic heterocyclyl”), and can be saturated or can be partially unsaturated. Heterocyclyl bicyclic ring systems can include one or more heteroatoms in one or more rings. “Heterocyclyl” also includes ring systems wherein the heterocyclyl ring, as defined above, is fused with one or more cycloalkyl groups wherein the point of attachment is either on the cycloalkyl or heterocyclyl ring, or ring systems wherein the heterocyclyl ring, as defined above, is fused with one or more aryl or heteroaryl groups, wherein the point of attachment is on the heterocyclyl ring, and in such instances, the number of ring members continue to designate the number of ring members in the heterocyclyl ring system. A heterocyclyl group may be described as, e.g., a 3-7-membered heterocyclyl, wherein the term “membered” refers to the non-hydrogen ring atoms, i.e., carbon, nitrogen, oxygen, sulfur, boron, phosphorus, and silicon, within the moiety. Each instance of heterocyclyl may be independently optionally substituted, i.e., unsubstituted (an “unsubstituted heterocyclyl”) or substituted (a “substituted heterocyclyl”) with one or more substituents. In certain embodiments, the heterocyclyl group is unsubstituted 3–16 membered heterocyclyl. In certain embodiments, the heterocyclyl group is substituted 3–16 membered heterocyclyl. Exemplary 3–membered heterocyclyl groups containing one heteroatom include, without limitation, azirdinyl, oxiranyl, thiorenyl. Exemplary 4–membered heterocyclyl groups containing one heteroatom include, without limitation, azetidinyl, oxetanyl and thietanyl. Exemplary 5– membered heterocyclyl groups containing one heteroatom include, without limitation, tetrahydrofuranyl, dihydrofuranyl, tetrahydrothiophenyl, dihydrothiophenyl, pyrrolidinyl, dihydropyrrolyl and pyrrolyl–2,5–dione. Exemplary 5–membered heterocyclyl groups containing two heteroatoms include, without limitation, dioxolanyl, oxasulfuranyl, disulfuranyl, and oxazolidin–2–one. Exemplary 5–membered heterocyclyl groups containing three heteroatoms include, without limitation, triazolinyl, oxadiazolinyl, and thiadiazolinyl. Exemplary 6– membered heterocyclyl groups containing one heteroatom include, without limitation, piperidinyl (e.g., 2,2,6,6-tetramethylpiperidinyl), tetrahydropyranyl, dihydropyridinyl, pyridinonyl (e.g., 1-methylpyridin2-onyl), and thianyl. Exemplary 6–membered heterocyclyl groups containing two heteroatoms include, without limitation, piperazinyl, morpholinyl, pyridazinonyl (2-methylpyridazin-3-onyl), pyrimidinonyl (e.g., 1-methylpyrimidin-2-onyl, 3- methylpyrimidin-4-onyl), dithianyl, dioxanyl. Exemplary 6–membered heterocyclyl groups containing two heteroatoms include, without limitation, triazinanyl. Exemplary 7–membered 12 Attorney Docket No.: A2219-7000WO heterocyclyl groups containing one heteroatom include, without limitation, azepanyl, oxepanyl and thiepanyl. Exemplary 8–membered heterocyclyl groups containing one heteroatom include, without limitation, azocanyl, oxecanyl and thiocanyl. Exemplary 5–membered heterocyclyl groups fused to a C6 aryl ring (also referred to herein as a 5,6–bicyclic heterocyclyl ring) include, without limitation, indolinyl, isoindolinyl, dihydrobenzofuranyl, dihydrobenzothienyl, benzoxazolinonyl, and the like. Exemplary 5–membered heterocyclyl groups fused to a heterocyclyl ring (also referred to herein as a 5,5–bicyclic heterocyclyl ring) include, without limitation, octahydropyrrolopyrrolyl (e.g., octahydropyrrolo[3,4-c]pyrrolyl), and the like. Exemplary 6-membered heterocyclyl groups fused to a heterocyclyl ring (also referred to as a 4,6-membered heterocyclyl ring) include, without limitation, diazaspirononanyl (e.g., 2,7- diazaspiro[3.5]nonanyl). Exemplary 6–membered heterocyclyl groups fused to an aryl ring (also referred to herein as a 6,6–bicyclic heterocyclyl ring) include, without limitation, tetrahydroquinolinyl, tetrahydroisoquinolinyl, and the like. Exemplary 6–membered heterocyclyl groups fused to a cycloalkyl ring (also referred to herein as a 6,7-bicyclic heterocyclyl ring) include, without limitation, azabicyclooctanyl (e.g., (1,5)-8-azabicyclo[3.2.1]octanyl). Exemplary 6–membered heterocyclyl groups fused to a cycloalkyl ring (also referred to herein as a 6,8-bicyclic heterocyclyl ring) include, without limitation, azabicyclononanyl (e.g., 9- azabicyclo[3.3.1]nonanyl). The terms "alkylene," “alkenylene,” “alkynylene,” “haloalkylene,” “heteroalkylene,” “cycloalkylene,” or “heterocyclylene,” alone or as part of another substituent, mean, unless otherwise stated, a divalent radical derived from an alkyl, alkenyl, alkynyl, haloalkylene, heteroalkylene, cycloalkyl, or heterocyclyl respectively. For example, the term "alkenylene," by itself or as part of another substituent, means, unless otherwise stated, a divalent radical derived from an alkene. An alkylene, alkenylene, alkynylene, haloalkylene, heteroalkylene, cycloalkylene, or heterocyclylene group may be described as, e.g., a C1-C6-membered alkylene, C2-C6-membered alkenylene, C2-C6-membered alkynylene, C1-C6-membered haloalkylene, C1- C6-membered heteroalkylene, C3-C8-membered cycloalkylene, or C3-C8-membered heterocyclylene, wherein the term “membered” refers to the non-hydrogen atoms within the moiety. In the case of heteroalkylene and heterocyclylene groups, heteroatoms can also occupy either or both of the chain termini (e.g., alkyleneoxy, alkylenedioxy, alkyleneamino, alkylenediamino, and the like). Still further, no orientation of the linking group is implied by the 13 Attorney Docket No.: A2219-7000WO direction in which the formula of the linking group is written. For example, the formula - C(O)2R’- may represent both -C(O)2R’- and –R’C(O)2-. As used herein, the terms “cyano” or “–CN” refer to a substituent having a carbon atom joined to a nitrogen atom by a triple bond, e.g., C≡N. As used herein, the terms “halogen” or “halo” refer to fluorine (fluoro, -F), chlorine (chloro, -Cl), bromine (bromo, -Br), or iodine (iodo, -I). As used herein, the term “hydroxy” refers to –OH. As used herein, the term “nitro” refers to a substituent having two oxygen atoms bound to a nitrogen atom, e.g., -NO2. As used herein, “oxo” refers to a carbonyl, i.e., -C(O)-. The symbol “ ” as used herein in relation to a bifunctional compound of Formula (I)refers to an attachment point to another moiety or functional group within the bifunctional compound. Alkyl, alkenyl, alkynyl, haloalkyl, heteroalkyl, cycloalkyl, heterocyclyl, aryl, and heteroaryl groups, as defined herein, are optionally substituted. In general, the term “substituted”, whether preceded by the term “optionally” or not, means that at least one hydrogen present on a group (e.g., a carbon or nitrogen atom) is replaced with a permissible substituent, e.g., a substituent which upon substitution results in a stable compound, e.g., a compound which does not spontaneously undergo transformation such as by rearrangement, cyclization, elimination, or other reaction. Unless otherwise indicated, a “substituted” group has a substituent at one or more substitutable positions of the group, and when more than one position in any given structure is substituted, the substituent is either the same or different at each position. The term “substituted” is contemplated to include substitution with all permissible substituents of organic compounds, such as any of the substituents described herein that result in the formation of a stable compound. The present disclosure contemplates any and all such combinations in order to arrive at a stable compound. For purposes of this invention, heteroatoms such as nitrogen may have hydrogen substituents and / or any suitable substituent as described herein which satisfy the valencies of the heteroatoms and results in the formation of a stable moiety. Two or more substituents may optionally be joined to form aryl, heteroaryl, cycloalkyl, or heterocyclyl groups. Such so-called ring-forming substituents are typically, though not necessarily, found attached to a cyclic base structure. In one embodiment, the ring-forming 14 Attorney Docket No.: A2219-7000WO substituents are attached to adjacent members of the base structure. For example, two ring- forming substituents attached to adjacent members of a cyclic base structure create a fused ring structure. In another embodiment, the ring-forming substituents are attached to a single member of the base structure. For example, two ring-forming substituents attached to a single member of a cyclic base structure create a spirocyclic structure. In yet another embodiment, the ring- forming substituents are attached to non-adjacent members of the base structure. The compounds provided herein may exist in one or more particular geometric, optical, enantiomeric, diastereomeric, epimeric, stereoisomeric, tautomeric, conformational, or anomeric forms, including but not limited to: cis- and trans-forms; E- and Z-forms; endo- and exo-forms; R-, S-, and meso-forms; D- and L-forms; d- and l-forms; (+) and (-) forms; keto-, enol-, and enolate-forms; syn- and anti-forms; synclinal- and anticlinal-forms; α- and β-forms; axial and equatorial forms; boat-, chair-, twist-, envelope-, and half chair-forms; and combinations thereof, hereinafter collectively referred to as "isomers" (or "isomeric forms"). Compounds described herein can comprise one or more asymmetric centers, and thus can exist in various isomeric forms, e.g., enantiomers and / or diastereomers. For example, the compounds described herein can be in the form of an individual enantiomer, diastereomer or geometric isomer, or can be in the form of a mixture of stereoisomers, including racemic mixtures and mixtures enriched in one or more stereoisomer. In an embodiment, the stereochemistry depicted in a compound is relative rather than absolute. Isomers can be isolated from mixtures by methods known to those skilled in the art, including chiral high-performance liquid chromatography (HPLC) and the formation and crystallization of chiral salts; or preferred isomers can be prepared by asymmetric syntheses or by using chirally pure starting materials. See, for example, Jacques et al., Enantiomers, Racemates and Resolutions (Wiley Interscience, New York, 1981); Wilen et al., Tetrahedron 33:2725 (1977); Eliel, Stereochemistry of Carbon Compounds (McGraw–Hill, NY, 1962); and Wilen, Tables of Resolving Agents and Optical Resolutions p.268 (E.L. Eliel, Ed., Univ. of Notre Dame Press, Notre Dame, IN 1972). This disclosure additionally encompasses compounds described herein as individual isomers substantially free of other isomers, and alternatively, as mixtures of various isomers. As used herein, a pure enantiomeric compound is substantially free from other enantiomers or stereoisomers of the compound (i.e., in enantiomeric excess). In other words, an “S” form of the compound is substantially free from the “R” form of the compound and is, thus, 15 Attorney Docket No.: A2219-7000WO in enantiomeric excess of the “R” form. The term “enantiomerically pure” or “pure enantiomer” denotes that the compound comprises more than 75% by weight, more than 80% by weight, more than 85% by weight, more than 90% by weight, more than 91% by weight, more than 92% by weight, more than 93% by weight, more than 94% by weight, more than 95% by weight, more than 96% by weight, more than 97% by weight, more than 98% by weight, more than 99% by weight, more than 99.5% by weight, or more than 99.9% by weight, of the enantiomer. In certain embodiments, the weights are based upon total weight of all enantiomers or stereoisomers of the compound. In the compositions provided herein, an enantiomerically pure compound can be present with other active or inactive ingredients. For example, a pharmaceutical composition comprising an enantiomerically pure R–compound can comprise, for example, about 90% excipient and about 10% enantiomerically pure R–compound. In certain embodiments, the enantiomerically pure R–compound in such compositions can, for example, comprise, at least about 95% by weight R–compound and at most about 5% by weight S–compound, by total weight of the compound. For example, a pharmaceutical composition comprising an enantiomerically pure S– compound can comprise, for example, about 90% excipient and about 10% enantiomerically pure S–compound. In certain embodiments, the enantiomerically pure S–compound in such compositions can, for example, comprise, at least about 95% by weight S–compound and at most about 5% by weight R–compound, by total weight of the compound. In some embodiments, a diastereomerically pure compound can be present with other active or inactive ingredients. For example, a pharmaceutical composition comprising a diastereomerically pure exo compound can comprise, for example, about 90% excipient and about 10% diastereomerically pure exo compound. In certain embodiments, the diastereomerically pure exo compound in such compositions can, for example, comprise, at least about 95% by weight exo compound and at most about 5% by weight endo compound, by total weight of the compound. For example, a pharmaceutical composition comprising a diastereomerically pure endo compound can comprise, for example, about 90% excipient and about 10% diastereomerically pure endo compound. In certain embodiments, the diastereometrically pure endo compound in such compositions can, for example, comprise, at least about 95% by weight endo compound and at most about 5% by weight exo compound, by total weight of the compound. 16 Attorney Docket No.: A2219-7000WO In some embodiments, an isomerically pure compound can be present with other active or inactive ingredients. For example, a pharmaceutical composition comprising an isomerically pure exo compound can comprise, for example, about 90% excipient and about 10% isomerically pure exo compound. In certain embodiments, the isomerically pure exo compound in such compositions can, for example, comprise, at least about 95% by weight exo compound and at most about 5% by weight endo compound, by total weight of the compound. For example, a pharmaceutical composition comprising an isomerically pure endo compound can comprise, for example, about 90% excipient and about 10% isomerically pure endo compound. In certain embodiments, the isomerically pure endo compound in such compositions can, for example, comprise, at least about 95% by weight endo compound and at most about 5% by weight exo compound, by total weight of the compound. In certain embodiments, the active ingredient can be formulated with little or no excipient or carrier. Compounds described herein may also comprise one or more isotopic substitutions. For example, H may be in any isotopic form, including1H,2H (D or deuterium), and3H (T or tritium); C may be in any isotopic form, including12C,13C, and14C; O may be in any isotopic form, including16O and18O; Br may be in any isotopic form, including79Br,81Br and77Br;82Br,76Br; B may be in any isotopic form, including11B and10B; N may be in any isotopic form, including14N and15N; F may be in any isotopic form, including18F,19F, and the like. The term "pharmaceutically acceptable salt" is meant to include salts of the active compounds that are prepared with relatively nontoxic acids or bases, depending on the particular substituents found on the compounds described herein. When compounds of the present disclosure contain relatively acidic functionalities, base addition salts can be obtained by contacting the neutral form of such compounds with a sufficient amount of the desired base, either neat or in a suitable inert solvent. Examples of pharmaceutically acceptable base addition salts include sodium, potassium, calcium, ammonium, organic amino, other organic bases, or magnesium salt, or a similar salt. When compounds of the present invention contain relatively basic functionalities, acid addition salts can be obtained by contacting the neutral form of such compounds with a sufficient amount of the desired acid, either neat or in a suitable inert solvent. Examples of pharmaceutically acceptable acid addition salts include those derived from inorganic acids like hydrochloric, hydrobromic, nitric, carbonic, monohydrogencarbonic, 17 Attorney Docket No.: A2219-7000WO phosphoric, monohydrogenphosphoric, dihydrogenphosphoric, sulfuric, monohydrogensulfuric, hydriodic, or phosphorous acids and the like, as well as the salts derived from organic acids like acetic, propionic, isobutyric, maleic, malonic, benzoic, succinic, suberic, fumaric, lactic, mandelic, phthalic, benzenesulfonic, p-tolylsulfonic, citric, tartaric, methanesulfonic, trifluoroacetic, and the like. Also included are salts of amino acids such as arginate and the like, and salts of organic acids like glucuronic or galacturonic acids and the like (see, e.g., Berge et al, Journal of Pharmaceutical Science 66: 1-19 (1977)). Certain specific compounds of the present invention contain both basic and acidic functionalities that allow the compounds to be converted into either base or acid addition salts. These salts may be prepared by methods known to those skilled in the art. Other pharmaceutically acceptable carriers known to those of skill in the art are suitable for the present invention. In addition to salt forms, the present disclosure provides compounds in a prodrug form. Prodrugs of the compounds described herein are those compounds that readily undergo chemical changes under physiological conditions to provide the compounds of the present invention. Additionally, prodrugs can be converted to the compounds of the present invention by chemical or biochemical methods in an ex vivo or in vivo environment. For example, prodrugs can be slowly converted to the compounds of the present invention when placed in a transdermal patch reservoir with a suitable enzyme or chemical reagent. The term “solvate” refers to forms of the compound that are associated with a solvent, usually by a solvolysis reaction. This physical association may include hydrogen bonding. Conventional solvents include water, methanol, ethanol, acetic acid, DMSO, THF, diethyl ether, and the like. The bifunctional compounds of Formula (I) may be prepared, e.g., in crystalline form, and may be solvated. Suitable solvates include pharmaceutically acceptable solvates and further include both stoichiometric solvates and non-stoichiometric solvates. In certain instances, the solvate will be capable of isolation, for example, when one or more solvent molecules are incorporated in the crystal lattice of a crystalline solid. “Solvate” encompasses both solution-phase and isolable solvates. Representative solvates include hydrates, ethanolates, and methanolates. The term “hydrate” refers to a compound which is associated with water. Typically, the number of the water molecules contained in a hydrate of a compound is in a definite ratio to the number of the compound molecules in the hydrate. Therefore, a hydrate of a compound may be 18 Attorney Docket No.: A2219-7000WO represented, for example, by the general formula R⋅x H2O, wherein R is the compound and wherein x is a number greater than 0. A given compound may form more than one type of hydrate, including, e.g., monohydrates (x is 1), lower hydrates (x is a number greater than 0 and smaller than 1, e.g., hemihydrates (R⋅0.5 H2O)), and polyhydrates (x is a number greater than 1, e.g., dihydrates (R⋅2 H2O) and hexahydrates (R⋅6 H2O)). The term “tautomer” refers to compounds that are interchangeable forms of a particular compound structure, and that vary in the displacement of hydrogen atoms and electrons. Thus, two structures may be in equilibrium through the movement of π electrons and an atom (usually H). For example, enols and ketones are tautomers because they are rapidly interconverted by treatment with either acid or base. Another example of tautomerism is the aci- and nitro- forms of phenylnitromethane that are likewise formed by treatment with acid or base. Tautomeric forms may be relevant to the attainment of the optimal chemical reactivity and biological activity of a bifunctional compound of interest. Other Definitions The following definitions are more general terms used throughout the present disclosure. The articles “a” and “an” refer to one or more than one (e.g., to at least one) of the grammatical object of the article. By way of example, “an element” means one element or more than one element. The term “and / or” means either “and” or “or” unless indicated otherwise. The term “about” is used herein to mean within the typical ranges of tolerances in the art. For example, “about” can be understood as within 2 standard deviations from the mean. In certain embodiments, “about” means +10%. In certain embodiments, “about” means +5%. When “about” is present before a series of numbers or a range, it is understood that “about” can modify each of the numbers in the series or range. “Acquire” or “acquiring” as used herein, refer to obtaining possession of a value, e.g., a numerical value, or image, or a physical entity (e.g., a sample), by “directly acquiring” or “indirectly acquiring” the value or physical entity. “Directly acquiring” means performing a process (e.g., performing an analytical method or protocol) to obtain the value or physical entity. “Indirectly acquiring” refers to receiving the value or physical entity from another party or source (e.g., a third-party laboratory that directly acquired the physical entity or value). Directly acquiring a value or physical entity includes performing a process that includes a physical change in a physical substance or the use of a machine or device. Examples of directly acquiring 19 Attorney Docket No.: A2219-7000WO a value include obtaining a sample from a human subject. Directly acquiring a value includes performing a process that uses a machine or device, e.g., mass spectrometer to acquire mass spectrometry data. The terms “administer,” “administering,” or “administration,” as used herein refers to implanting, absorbing, ingesting, injecting, inhaling, or otherwise introducing an inventive compound, or a pharmaceutical composition thereof. As used herein, the terms “condition,” “disease,” and “disorder” are used interchangeably. An “effective amount” of a bifunctional compound of Formula (I) refers to an amount sufficient to elicit the desired biological response, i.e., treating the condition. As will be appreciated by those of ordinary skill in this art, the effective amount of a compound of Formula (I) may vary depending on such factors as the desired biological endpoint, the pharmacokinetics of the compound, the condition being treated, the mode of administration, and the age and health of the subject. An effective amount encompasses therapeutic and prophylactic treatment. For example, in treating cancer, an effective amount of an inventive compound may reduce the tumor burden or stop the growth or spread of a tumor. The “therapeutically effective amount” of a compound described herein refers to an amount of compound sufficient to provide a therapeutic benefit in the treatment of a condition or to delay or minimize one or more symptoms associated with the condition. In some embodiments, a therapeutically effective amount is an amount sufficient to provide a therapeutic benefit in the treatment of a condition or to minimize one or more symptoms associated with the condition. A therapeutically effective amount of a compound means an amount of therapeutic agent, alone or in combination with other therapies, which provides a therapeutic benefit in the treatment of the condition. The term “therapeutically effective amount” can encompass an amount that improves overall therapy, reduces or avoids symptoms or causes of the condition, or enhances the therapeutic efficacy of another therapeutic agent. The terms “peptide,” “polypeptide,” and “protein” are used interchangeably, and refer to a compound comprised of amino acid residues covalently linked by peptide bonds. A protein or peptide must contain at least two amino acids, and no limitation is placed on the maximum number of amino acids that can be comprised therein. Polypeptides include any peptide or protein comprising two or more amino acids joined to each other by peptide bonds. As used 20 Attorney Docket No.: A2219-7000WO herein, the term refers to both short chains, which also commonly are referred to in the art as peptides, oligopeptides and oligomers, for example, and to longer chains, which generally are referred to in the art as proteins, of which there are many types. “Prevention,” “prevent,” and “preventing” as used herein refers to a treatment that comprises administering a therapy, e.g., administering a compound described herein (e.g., a bifunctional compound of Formula (I)) prior to the onset of a disease, disorder, or condition in order to preclude the physical manifestation of said disease, disorder, or condition. In some embodiments, “prevention,” “prevent,” and “preventing” require that signs or symptoms of the disease, disorder, or condition have not yet developed or have not yet been observed. In some embodiments, treatment comprises prevention and in other embodiments it does not. A “subject” to which administration is contemplated includes, but is not limited to, humans (i.e., a male or female of any age group, e.g., a pediatric subject (e.g., infant, child, adolescent) or adult subject (e.g., young adult, middle–aged adult, or senior adult)) and / or other non–human animals, for example, mammals (e.g., primates (e.g., cynomolgus monkeys, rhesus monkeys); commercially relevant mammals such as cattle, pigs, horses, sheep, goats, cats, and / or dogs) and birds (e.g., commercially relevant birds such as chickens, ducks, geese, and / or turkeys). In certain embodiments, the animal is a mammal. The animal may be a male or female and at any stage of development. A non–human animal may be a transgenic animal. As used herein, the terms “treatment,” “treat,” and “treating” refer to reversing, alleviating, delaying the onset of, or inhibiting the progress of one or more of a symptom, manifestation, or underlying cause of a disease, disorder, or condition (e.g., as described herein), e.g., by administering a therapy, e.g., administering a compound described herein (e.g., a bifunctional compound of Formula (I)). In an embodiment, treating comprises reducing, reversing, alleviating, delaying the onset of, or inhibiting the progress of a symptom of a disease, disorder, or condition. In an embodiment, treating comprises reducing, reversing, alleviating, delaying the onset of, or inhibiting the progress of a manifestation of a disease, disorder, or condition. In an embodiment, treating comprises reducing, reversing, alleviating, reducing, or delaying the onset of, an underlying cause of a disease, disorder, or condition. In some embodiments, “treatment,” “treat,” and “treating” require that signs or symptoms of the disease, disorder, or condition have developed or have been observed. In other embodiments, treatment may be administered in the absence of signs or symptoms of the disease or condition, e.g., in 21 Attorney Docket No.: A2219-7000WO preventive treatment. For example, treatment may be administered to a susceptible individual prior to the onset of symptoms (e.g., in light of a history of symptoms and / or in light of genetic or other susceptibility factors). Treatment may also be continued after symptoms have resolved, for example, to delay or prevent recurrence. In some embodiments, treatment comprises prevention and in other embodiments it does not. A “proliferative disease” refers to a disease that occurs due to abnormal extension by the multiplication of cells (Walker, Cambridge Dictionary of Biology; Cambridge University Press: Cambridge, UK, 1990). A proliferative disease may be associated with: 1) the pathological proliferation of normally quiescent cells; 2) the pathological migration of cells from their normal location (e.g., metastasis of neoplastic cells); 3) the pathological expression of proteolytic enzymes such as the matrix metalloproteinases (e.g., collagenases, gelatinases, and elastases); 4) the pathological angiogenesis as in proliferative retinopathy and tumor metastasis; or 5) evasion of host immune surveillance and elimination of neoplastic cells. Exemplary proliferative diseases include cancers (i.e., “malignant neoplasms”), benign neoplasms, and angiogenesis. A “non-proliferative disease” refers to a disease that does not primarily extend through the abnormal multiplication of cells. A non-proliferative disease may be associated with any cell type or tissue type in a subject. Exemplary non-proliferative diseases include neurological diseases or disorders (e.g., a repeat expansion disease); autoimmune disease or disorders; immunodeficiency diseases or disorders; lysosomal storage diseases or disorders; inflammatory diseases or disorders; cardiovascular conditions, diseases, or disorders; metabolic diseases or disorders; respiratory conditions, diseases, or disorders; renal diseases or disorders; and infectious diseases. Throughout the application, embodiments for any one of Formulas (I), (III), (IV), (VI) and (VIII) apply, where relevant, to any of the other Formulas described herein, for example, any one of Formulas (I), (III), (IV), (VI) and (VIII). In addition, the embodiments provided for Formula (III) apply equally, where relevant, to subformulae (III-a) to (III-m). Similarly, the embodiments provided for Formula (IV) apply equally, where relevant, to subformulae (IV-a) to (IV-k). Similarly, the embodiments provided for Formula (VI) apply equally, where relevant, to subformulae (VI-a) to (VI-m). Similarly, the embodiments provided for Formula (IV) apply equally, where relevant, to Formula (VIII) and subformulae (VIII-a) to (VIII-o). Similarly, the embodiments provided for Formula (VIII) apply equally, where relevant, to subformulae (VIII-a) 22 Attorney Docket No.: A2219-7000WO to (VIII-o). Bifunctional Compounds The present disclosure features bifunctional compounds of Formula (I): a pharmaceutically acceptable salt, so vate, ydrate, tautomer, or stereo somer t ereo , w ere n (i) the Chelator comprises a moiety capable of binding to a metal ion (e.g., a radiometal ion); (ii) L1 comprises a linker; (iii) the FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP); and x is 1, 2, 3, 4, 5, or 6. In some embodiments, the bifunctional compound of Formula (I) comprises a metal ion (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I) does not comprise a metal ion (e.g., a radiometal ion). In one aspect, the bifunctional compound of Formula (I) is a bifunctional compound of Formula (I-a): Chelator L1 FAP Ligand(I-a), or a pharmaceutically acceptable salt, stereoisomer thereof, wherein (i) the Chelator comprises a moiety capable of binding to a metal ion (e.g., a radiometal ion); (ii) L1 comprises a linker; and (iii) the FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP). In one aspect, the bifunctional compound of Formula (I) is a compound of Formula (I-b): Chelator L1 FAP Ligandr a pharmaceutically acceptable salt, i) the Chelator comprises a moiety . ., (e.g., a radiometal ion); (ii) L1 comprises a linker; and (iii) each FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP). In one aspect, the bifunctional compound of Formula (I) is a compound of Formula (I-c): 23 Attorney Docket No.: A2219-7000WO c), wherein (i) t he Chelator comprises a moiety capable of binding to a positively charged ion (e.g., a cation) (e.g., a radiometal ion); (ii) L1 comprises a linker; Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, heteroaryl, and aryl are optionally further substituted; R6aand R6bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the bifunctional compound of Formula (I) is a compound of Formula (I-d): R5aO R3aR3bm R5bN r a herein: (i) ation) (e.g., a radiometal ion); (ii) L1 comprises a linker; each R1is independently selected from H, 24 Attorney Docket No.: A2219-7000WO halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5a, R5a’, R5b, and R5b’are independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the bifunctional compound of Formula (I) is a compound of Formula (I-e): R6aR6bR5kOR3a R3bm r a wherein: (i) the Chelator comprises a moiety capable of binding to a positively charged ion (e.g., a cation) (e.g., a radiometal ion); (ii) L1 comprises a linker; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5k, R5l, R5m, and R5nare independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2- heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, 25 Attorney Docket No.: A2219-7000WO and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the bifunctional compound of Formula (I) is a compound of Formula (I-f): O R3a 1R3b(R )pf), wherein (i) the n (e.g., a cation) (e.g., a radiometal ion); (ii) L1 comprises a linker; Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R1ais -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, or -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, - SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6 heteroalkyl, aryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, heteroaryl, and aryl are optionally further substituted; R6aand R6bare independently selected from H, C1-6 alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the bifunctional compound of Formula (I) is a compound of Formula (I-g): R1bR1b'O R3aR3bg), wherein (i) the Chelator (e.g., a cation) (e.g., a Attorney Docket No.: A2219-7000WO radiometal ion); (ii) L1 comprises a linker; Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R1ais -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, or -CN; R1band R1b’are independently selected from H, halo, C1-6 haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6 heteroalkyl, aryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, heteroaryl, and aryl are optionally further substituted; R6aand R6bare independently selected from H, C1-6 alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the bifunctional compound of Formula (I) is a compound of Formula (I-h): (R1OR3aR3b)ph), wherein (i) the Chelator iometal ion); (ii) L1 comprises a linker; Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; each R1is independently selected from H, halo, -OR2a, - B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6heteroalkyl; R2band R2care each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6 heteroalkyl, aryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, heteroaryl, and aryl are optionally further substituted; and p is 1, 2, 3, 4, 5, or 6. 27 Attorney Docket No.: A2219-7000WO In one aspect, the bifunctional compound of Formula (I) is a compound of Formula (I-i): R21a-i), w ere n: ng s se ecte rom monocyc c or cyc c ary or eteroary r ng, opt ona y substituted with 1-5 occurrences of R5; each R1is independently selected from H, halo, -OR2a, - B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; R10a, R10b, R11a, R11b, R12a, and R12bare each independently selected from -L2- [FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl-aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; R15is H or C1–6 alkyl; R20aand R20bare independently selected from H, C1-6alkyl, C1-6heteroalkyl, -C(O)OH, and -C(O)OR; each of R21a, R21b, R21cis selected from -CH2-C(O)OH, or -CH2-heteroaryl-C(O)OH; Q is absent, N(R15), or heterocyclyl; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, 28 Attorney Docket No.: A2219-7000WO C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2- heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, - SO2-heteroaryl, or -OSO2F; L2is a linker; a is 1, 2, 3, 4, 5, or 6; b and b’ are independently selected from 0, 1, or 2; c is 0, 1, or 2; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; p is 1, 2, 3, 4, 5, or 6; r is 0, 1, 2, 3, or 4; and y and z are each independently an integer between 0 and 10. In some embodiments, REis H, C1-4alkyl, or cycloalkyl. In some embodiments, REis H or C1-4alkyl. In some embodiments, REis H or C1-2alkyl. In some embodiments, REis H or CH3. In some embodiments, REis H. In some embodiments, REis CH3. In some embodiments, R20aand R20bare independently selected from H, C1-6 alkyl, C1-6 heteroalkyl, -C(O)OH, and -C(O)OR. In some embodiments, R20aand R20bare independently selected from H, C1-6 alkyl, C1-6 heteroalkyl, -C(O)OH, and -C(O)OR, wherein R is selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl. In some embodiments, R20aand R20bare independently selected from H, C1-6alkyl, C1-6heteroalkyl, and -C(O)OH. In some embodiments, the bifunctional compound of Formula (I) is a compound of Formula (I-j): OH N O r a pharmaceutically accepta M is N(R16) or O; and eac , , , , , C1-4alkyl, halo, - OH, -OSO2F, -SO2F, -SO2-heteroaryl, and substituted aryl, wherein at least one of R13f, R13h, or R13imust not be H; and R16is H or C1-4 alkyl. In some embodiments, the bifunctional compound of Formula (I) is a compound of Formula (I-k): 29 Attorney Docket No.: A2219-7000WO OH r a pharma ceut ca y acceptab e sa t, so vate, ydrate, tautomer, or stereo somer t ereof, wherein: M is N(CH3) or O; R13jis halo or C1-4alkyl; and each of R13f, R13g, R13h, and R13iare independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, and substituted aryl, wherein at least one of R13f, R13h, or R13imust not be H. In an embodiment, the bifunctional compound of Formula (I) is a compound of Formula (I-l): OH r a pharma hereof, wherein: M is N(CH3) or O; each of R13f, R13h, and R13iare independently selected from H, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, and substituted aryl, wherein one of R13f, R13h, or R13imust not be H. In one aspect, the bifunctional compound of Formula (I) is a compound of Formula (I-m): R11bR11aH O Chelator N M FAP Ligand m), wherein (i) e.g., a cation) ises a moiety 30 Attorney Docket No.: A2219-7000WO capable of binding to the fibroblast activation protein (FAP); R10a, R10b, R11a, and R11bare each independently selected from H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, - NRBRC, C1-6alkyl-aryl; or each of R10aand R10b, R11aand R11b, independently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclyl, or heteroalkylene, wherein each heteroalkyl and heterocyclyl is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, - SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; REis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; and y is an integer between 0 and 10. In an embodiment, the bifunctional compound of Formula (I) is a compound of Formula (I-n): O H Chelator N N r a pharmaceutically wherein: RKis H or -SO2F; g . e embodiments, RKis H. In some embodiments, RKis -SO2F. In an embodiment, the bifunctional compound of Formula (I) is a compound of Formula (I-o): 31 Attorney Docket No.: A2219-7000WO O lly a ccepta e sa t, sovate, y rate, tautomer, or stereo somer t ereo , w ere n: s or -SO2F; and wherein the Chelator is as defined herein. In an embodiment, the bifunctional compound of Formula (I) is a compound of Formula (I-p): HO O H O N r a pharmaceutically RKis H or -SO2F. Chelators The chelator is a moiety capable of binding to a metal ion (e.g., a radiometal ion). The chelator as described herein refers to a molecule having one or more electron pairs available for donation to a metal ion. The metal ion is usually coordinated by two or more electron pairs to the chelator. The terms “bidentate chelator”, “tridentate chelator”, and “tetradentate chelator” refer to chelators having respectively, two, three, or four electron pairs readily available for donation to a metal ion coordinated by the chelator. Usually, the electron pairs of a chelator forms 32 Attorney Docket No.: A2219-7000WO coordinate bonds with a single metal ion; however, in certain examples, a chelator may form coordinate bonds with more than one metal ion, with a variety of binding modes being possible. In an embodiment, the chelator is a moiety which forms a complex with divalent or trivalent metal cations. In an embodiment, the chelator is selected from 1,4,7,10- tetraazacyclododecane-N,N’,N,N’-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-1,4,7- triacetic acid (NOTA), triethylenetetramine (TETA), 1,4,7,10-tetraazacyclododecane-1-(glutamic acid)-4,7,10-triacetic acid (DOTAGA), ethylenediaminetetraacetic acid (EDTA), iminodiacetic acid, diethylenetriamine-N,N,N’,N’,N"-pentaacetic acid (DTPA), bis- (carboxymethylimidazole)glycine, nitrilotriacetic acid (NTA), 1,4,7,10-tetraazacyclododecane- 1,4,7-triacetic acid (DO3A) and 6-Hydrazinopyridine-3-carboxylic acid (HYNIC). In some embodiments, the chelator comprises a macrocycle, e.g., a macrocycle comprising an O and / or a N, DOTA, NOTA, one or more amines, one or more ethers, one or more carboxylic acids, EDTA, DTPA, TETA, DO3A, PCTA, or desferrioxamine. In some embodiments, the chelator comprises a plurality of amines. In some embodiments, the chelator includes 4 or more N, 4 or more carboxylic acid groups, or a combination thereof. In some embodiments, the chelator does not comprise S. In some embodiments, the chelator comprises a ring. In some embodiments, the ring comprises an O and / or an N. In some embodiments, the chelator is a ring that includes 3 or more N, 3 or more carboxylic acid groups, or a combination thereof. In some embodiments, the chelator is polydentate. In some embodiments, the chelator described herein comprises a cyclic chelating agent. Exemplary cyclic chelating agents include, but are not limited to, AAZTA, BAT, BAT-TM, Crown, Cyclen, DO2A, CB-DO2A, DO3A, H3HP-DO3A, Oxo-DO3A, p-NH2-Bn-Oxo-DO3A, DOTA, DOTA-3py, DOTA-PA, DOTA-GA, DOTA-4AMP, DOTA-2py, DOTA-1py, p-SCN- Bn-DOTA, CHX-A"-EDTA, MeO-DOTA-NCS EDTA, DOTAMAP, DOTAGA, DOTAGA- anhydride, DOTMA, DOTASA, DOTAM, DOTP, CB-Cyclam, TE2A, CB-TE2A, CB-TE2P, DM-TE2A, MM-TE2A, NOTA, NOTP, HEHA, HEHA-NCS, p-SCN-Bn-HEHA, DTPA, CHX- A"-DTPA, p-NH2-Bn-CHX-A"-DTPA, p-SCN-DTPA, p-SCN-Bz-Mx-DTPA, 1B4M-DTPA, p- SCN-Bn1B-DTPA, p-SCN-Bn-1B4M-DTPA, p-SCN-Bn-CHX-A"-DTPA, PEPA, p-SCN-Bn- PEPA, TETPA, DOTPA, DOTMP, DOTPM, t-Bu-calix[4]arene-tetracarboxylic acid, macropa, macropa-NCS, macropid, H3L1, H3L4, H2azapa, H5decapa, bispa2, H4pypa, H4octapa, 33 Attorney Docket No.: A2219-7000WO H4CHXoctapa, p-SCN-Bn-H4octapa, p-SCN-Bn-H4octapa, TTHA, p-NO2-Bn-neunpa, H4octox, H2macropa, H2bispa2, H4phospa, H6phospa, p-SCN-Bn-H6phospa, TETA, p-NO2-Bn-TETA, TRAP, TPA, HBED, SHBED, HBED-CC, (HBED-CC)TFP, DMSA, DMPS, DHLA, lipoic acid, TGA, BAL, Bis-thioseminarabazones, p-SCN-NOTA, nNOTA, NODAGA, CB-TE1A1P, 3P-C- NETA-NCS, 3p-C-DEPA, 3P-C-DEPA-NCS, TCMC, PCTA, NODIA-Me, TACN, pycup1A1B, pycup2A, THP, DEDPA, H2DEDPA, p-SCN-Bn-H2DEDPA, p-SCN-Bn-TCMC, motexafin, NTA, NOC, 3p-C-NETA, p-NH2-Bn-TE3A, SarAr, DiAmSar, SarAr-NCS, AmBaSar, BaBaSar, TACN-TM, CP256, C-NE3TA, C-NE3TA-NCS, NODASA, NETA-monoamide, C-NETA, NOPO, BPCA, p-SCN-Bn-DFO, DFO-ChX-Mal, DFO, DFO-IAC, DFO-BAC, DiP-LICAM, EC, SBAD, BAPEN, TACHPYR, NEC-SP, Lpy, L1, L2, L3, and EuK-106. In some embodiments, the chelator is DOTA, TRITA, TETA, DOTA-MA, DO3A-HP, DOTMA, DOTA- pNB, DOTP, DOTMP, DOTEP, DOTMPE, F-DOTPME, DOTPP, DOTBzP, DOTA- monoamide, p-NCS-DOTA, p-NCS-PADOTA, BAT, DO3TMP-Monoamide, p-NCS-TRITA, NOTA, or CHX-A"-DTPA. In some embodiments, a chelator described herein comprises an acyclic chelating agent. Exemplary acyclic chelating agents include, but are not limited to, DTA, CyEDTA, EDTMP, DTPMP, DTPA, CyDTPA, Cy2DTPA, DTPA-MA, DTPA-BA, and BOPA. In some embodiments, a chelator described herein comprises DOTA, DOTP, DOTMA, DOTAM, DTPA, NTA, EDTA, DO3A, DO2A, NOC, NOTA, TETA, TACN, DiAmSar, CB- Cyclam, CB-TE2A, DOTA-4AMP, or NOTP. In some embodiments, a chelator described herein comprises H4pypa, H4octox, H4octapa, p-NO2-Bn-neunpa, p-SCN-Bn-H4neunpa, TTHA,lBu4pypa-C7-NHS, H4neunpa, H2macropa, HP-DO3A, BT-DO3A, DO3A-Nprop, DO3AP, DO2A2P, DOA3P, DOTP, DOTPMB, DOTAMAE, DOTAMAP, DO3AMBu, DOTMA, TCE-DOTA, DEPA, PCTA, p-NO2-Bn-PCTA, p-NO2-Bn-DOTA, symPC2APA, symPCA2PA, asymPC2APA, asymPCA2PA, TRAP, AAZTA, DATAm, THP, HEHA, or HBED. In some embodiments, the chelator is DO3A. In some embodiments, the chelator is PEPA. In some embodiments, the chelator is EDTA. In some embodiments, the chelator is CHX- A"-DTPA. In some embodiments, the chelator is HEHA. In some embodiments, the chelator is DOTMP. In some embodiments, the chelator is t-Bu-calix[4]arene-tetracarboxylic acid. In some embodiments, the chelator is macropa. In some embodiments, the chelator is macropa-NCS. In some embodiments, the chelator is H4pypa. In some embodiments, the chelator is H4octapa. In 34 Attorney Docket No.: A2219-7000WO some embodiments, the chelator is H4CHXoctapa. In some embodiments, the chelator is DOTP. In some embodiments, the chelator is crown. In some embodiments, the chelator is DOTA. In some embodiments, the chelator is a chiral derivative of DOTA. Exemplary chiral DOTA chelators are described in Dai et al., Nature Communications (2018) 9:857. In some embodiments, the chelator is 2,2’,2",2’"- ((2S,5S,8S,11S)-2,5,8,11-tetramethyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic HO acid. In some embodiments, the chelator has a structur . In some embodiments, the chelator is 2,2’,2",2"‘-((2S,5S , , , , , , , , 0- tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic acid. In some embodiments, the chelator has a HO . HO R O N In some embodiments, the chelator has a structur , wherein each R is independently selected from hydroge , aminoalkyl, heteroalkyl, alkenyl, alkynyl, cycloalkyl, he , , , alkylcycloalkyl, alkylheterocycloalkyl, alkylaryl, alkylheteroaryl, or an amino acid side chain. In 35 Attorney Docket No.: A2219-7000WO OOHsome embodiments, the chelator has a structur , wherein each R is independently selected from hydrogen, alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, heteroalkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkylcycloalkyl, alkylheterocycloalkyl, alkylaryl, alkylheteroaryl, or an amino acid side chain. Exemplary chelators are further described in WO2012 / 174136; US20130183235A1; US20120219495A1; Ramogidaand et al., EJNMMI radiopharm. chem.4, 21 (2019); Thiele et al., Cancer Biotherapy and Radiopharmaceuticals 2018; Li et al., Bioconjugate Chem.2019, 30, 5, 1539-1553; and Baranyai et al., Eur. J. Inorg. Chem.36-56 (2020), each of which is incorporated by reference in its entirety. In an embodiment, the bifunctional compound of Formula (I) contains a chelator of Formula (II): 21aR20a R20bR Naa pharmaceutically acceptable salt, solvate, hydrate, tautom rein: R20aand R20bare independently selected from H, C1-6 alkyl, C 1-6 heteroalkyl, -C(O)OH, and -C(O)OR; each of R21a, R21b, and R21care selected from - CH2-C(O)OH, or -CH2-heteroaryl-C(O)OH; a is 1, 2, 3, 4, 5, or 6; b and b’ are independently selected from 0, 1, or 2; and c is 0, 1, or 2. In some embodiments, R20aand R20bare independently selected from H, C1-6 alkyl, C1-6 heteroalkyl, -C(O)OH, and -C(O)OR. In some embodiments, R20aand R20bare independently selected from H, C1-6 alkyl, C1-6 heteroalkyl, -C(O)OH, and -C(O)OR, wherein R is selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl. In some embodiments, R20aand R20bare independently selected from H, C1-6alkyl, C1-6heteroalkyl, and -C(O)OH. In some embodiments, R20aand R20bare independently selected from H and C1-636 Attorney Docket No.: A2219-7000WO alkyl. In an embodiment, each of R20aand R20bare independently H. In an embodiment, one of R20aand R20bis independently H. In an embodiment, one of R20aand R20bis independently - C(O)OH. In an embodiment, each of R21a, R21b, and R21care independently -CH2-C(O)OH. In an embodiment, a is selected from 1, 2 or 3. In an embodiment, a is 1. In an embodiment, a is 3. In an embodiment, b and b’ are each independently selected from 1 or 2. In an embodiment, both b and b’ are 1. In an embodiment, c is 0 or 1. In an embodiment, c is 1. In an embodiment, the bifunctional compound of Formula (I) contains a chelator of Formula (II-a): HOR20a R20ba pharmaceutically acceptable salt, solvate, hydrate, tautom R20aand R20bare independently selected from H, C1-6 alkyl, C1-6 heteroalkyl, -C(O)OH, -C(O)OR; a is 1, 2, 3, 4, 5, or 6; b and b’ are independently selected from 0, 1, or 2; c is 0, 1, or 2. In some embodiments, R20aand R20bare independently selected from H, C1-6alkyl, C1-6heteroalkyl, -C(O)OH, and -C(O)OR. In some embodiments, R20aand R20bare independently selected from H, C1-6alkyl, C1-6heteroalkyl, -C(O)OH, and -C(O)OR, wherein R is selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl. In some embodiments, R20aand R20bare independently selected from H, C1-6 alkyl, C1-6 heteroalkyl, and -C(O)OH. In some embodiments, R20aand R20bare independently selected from H and C1-6 alkyl. In an embodiment, each of R20aand R20bare independently H. In an embodiment, one of R20aand R20bis independently H. In an embodiment, one of R20aand R20bis independently - C(O)OH. In an embodiment, a is selected from 1, 2 or 3. In an embodiment, a is 1. In an embodiment, a is 3. In an embodiment, b and b’ are each independently selected from 1 or 2. In an embodiment, both b and b’ are 1. In an embodiment, c is 0 or 1. In an embodiment, c is 1. 37 Attorney Docket No.: A2219-7000WO In an embodiment, the chelator is selected from the following formulas: HO an DOTA-NOC, DOTA-TATE, DOTA-LAN, DOTA-VAP, DMSA, DTPA, NTA, NETA, EDTA, DO3A, DEPA, TRITA, or CB-TE2A. In some embodiments, the chelator binds to a radiometal ion. In some embodiments, the chelator binds to a radiometal ion selected from99Tc,64Cu,211At,123I,124I,131I,177Lu, or18F. In some embodiments, the chelator binds to a radiometal ion selected from99Tc,64Cu, or177Lu. Radiometal ions The radiometal ion is a radioisotope that may coordinate or chelate to the chelator. In an embodiment, the radiometal ion is selected from the group consisting of alpha radiation emitting isotopes, beta radiation emitting isotopes, gamma radiation emitting isotopes, Auger electron emitting isotopes, X-ray emitting isotopes, or fluorescence emitting isotopes. The radiometal ion may be useful in therapeutics / therapy or diagnostics / imaging. In an embodiment, the radiometal ion may be useful as therapeutic or therapy (e.g., in preparing a medicine for radiotherapy), or for imaging of disease states such as cancer, 38 Attorney Docket No.: A2219-7000WO inflammation, endometriosis, fibrosis, other diseases that involve tissue remodeling (e.g.,68Ga,67Ga,90Y,177Lu,225Ac,111In,161Tb,86Y, Al18F). In an embodiment, the radiometal ion may be useful in diagnostics or imaging (e.g.,68Ga,67Ga,90Y,177Lu,18F,111In,99Tc,86Y, Al18F). In an embodiment, the radiometal ion may comprise47Sc,51Cr,64Cu,67Cu,67Ga,68Ga,72As,88Y,90Y,97Ru,99Tc,101Rh,105Rh,109Pd,111In,119Sb,128Ba,139La,140La,142Pr,149Pm,151Eu,153Eu,153Sm,159Gd,165Dy,166Ho,169Er,175Yb,177Lu,186Re,188Re,197Hg,198Au,199Ag,201Tl,203Pb,212Pb,212Bi,213Bi,225Ac, or227Th. In an embodiment, the radiometal ion comprises64Cu,68Ga,90Y,99Tc,153Sm,177Lu, or188Re. In an embodiment, the radiometal ion may be useful in PET imaging (e.g.,68Ga,18F). In an embodiment, the radiometal ion may be useful in MRI imaging as a contrast agent (e.g., Gd). In an embodiment, the radiometal ion may be useful in β-radiotherapy (e.g.,177Lu,90Y,188Re), or alpha-radiotherapy (e.g.225Ac,212Pb), or combination of alpha- and beta-radiotherapy, or auger electron-based therapy. In an embodiment, the radiometal ion may be useful in SPECT imaging (e.g.,99Tc,203Pb,177Lu). In an embodiment, the radiometal ion is selected from99Tc,64Cu,211At,177Lu,212Pb,177Lu,111In. In an embodiment, the radiometal ion is an isotope useful in diagnostics and / or imaging (e.g.,68Ga,67Ga,90Y,177Lu,18F,111In,99Tc). In an embodiment, the radiometal ion is an isotope selected from68Ga,67Ga,90Y,177Lu,18F,111In, or99Tc. In an embodiment, the radiometal ion is an isotope useful in PET imaging (e.g.,68Ga,18F). In an embodiment, the radiometal ion is68Ga or18F. In an embodiment, the radiometal ion is an isotope useful in MRI imaging as a contrast agent (e.g., Gd). In an embodiment, the radiometal ion is Gd. In an embodiment, the radiometal ion is an isotope useful in β-radiotherapy (e.g.,177Lu,90Y,188Re,131I). In an embodiment, the radiometal ion is an isotope selected from177Lu,90Y,188Re or131I. In an embodiment, the radiometal ion is an isotope useful in alpha-radiotherapy (e.g.225Ac,212Pb). In an embodiment, the radiometal ion is an isotope selected from225Ac or212Pb. In an embodiment, the radiometal ion is an isotope useful in a combination of alpha- and beta-radiotherapy. In an embodiment, the radiometal ion is an isotope useful in auger electron-based therapy. In an embodiment, the radiometal ion is an isotope useful in SPECT imaging (e.g.,99Tc,203Pb,177Lu). In an embodiment, the radiometal ion is an isotope selected from99Tc,203Pb, or177Lu. 39 Attorney Docket No.: A2219-7000WO Linkers The present disclosure features bifunctional compounds comprising a FAP Ligand and a Chelator, separated by a linker (e.g., L1). In some embodiments, the linker is covalently bound to the FAP Ligand. In some embodiments, the linker is covalently bound to the Chelator. In some embodiments, the linker is covalently bound to both the FAP Ligand and the Chelator. In some embodiments, the linker is a non-cleavable linker. In some embodiments, the linker is not degraded or hydrolyzed at physiological conditions. In some embodiments, the linker comprises a bond that is not cleavable in a cell (e.g., a cell organelle) or the serum, e.g., of a sample or subject. In some embodiments, the linker comprises an alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, ether, amine, alkoxy, aryl, heteroaryl, cycloalkyl, or heterocyclyl. In some embodiments, the linker comprises an alkylene or heteroalkylene. In an embodiment, the linker (L1) is absent. In some embodiments, the linker (e.g., L1) has the structure of Formula (III): R10bR10aWr a pharmaceutically acceptable salt, hy wherein: R10a, R10b, R11a, R11b, R12a, and R12bare each independently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl-aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; Q is absent, N(R15), or heterocyclylene; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; R15is H or C1–6alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; 40 Attorney Docket No.: A2219-7000WO RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; denotes the point of attachment to the FAP Ligand in Formula(I); and * denotes the point of attachment to the Chelator in Formula (I).In some embodiments, each of R10a, R10b, R11a, and R11bis independently H. In some embodiments, each of R10aand R10bare independently H. In some embodiments, each of R11aand R11bare independently H. In some embodiments, each of R10aand R10bare taken together with the carbon atom to which they are attached form an oxo group. In some embodiments, each of R11aand R11bare taken together with the carbon atom to which they are attached form an oxo group. In some embodiments, each of R12aand R12bare taken together with the carbon atom to which they are attached form an oxo group. In some embodiments, one of R10aand R10bis -L2- [FAP Ligand]. In some embodiments, one of R11aand R11bis -L2-[FAP Ligand]. In some embodiments, one of R12aand R12bis -L2-[FAP Ligand]. In some embodiments, one of R10aand R10bis C1-6 alkyl-aryl. In some embodiments, one of R10aand R10bis NRBRC. In some embodiments, one of R10aand R10bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH. In some embodiments, one of R10aand R10bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or -OSO2F. In some embodiments, one of R10aand R10bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with -OH or -OSO2F. In some embodiments, R10ais -NH-C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with -OH or -OSO2F. In some embodiments, R10ais -NH-C(O)-C1-4 alkyl-aryl, wherein aryl is substituted with one of - OH or -OSO2F. In some embodiments, R10ais -NH-C(O)-C1-4 alkyl-aryl, wherein aryl is substituted with -OH. In some embodiments, R10ais -NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with -OSO2F. In some embodiments, one of R11aand R11bis NRBRCand the other is H. In some embodiments, one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH. In some embodiments, one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4 alkyl-aryl, wherein aryl is 41 Attorney Docket No.: A2219-7000WO optionally substituted with halo, -OH or -OSO2F. In some embodiments, one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with -OH or -OSO2F. In some embodiments, R11ais -NH-C(O)RH, wherein RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with - OH or -OSO2F. In some embodiments, R11ais -NH-C(O)-C1-4 alkyl-aryl, wherein aryl is substituted with one of -OH or -OSO2F. In some embodiments, R11ais -NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with -OH. In some embodiments, R11ais -NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with -OSO2F. As generally described herein, RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH. In some embodiments, both of RBand RCare H. In some embodiments, one of RBand RCis H, and the other of RBor RCis selected from C1-6 alkyl, or -C(O)RH. In some embodiments, one of RBand RCis H, and the other of RBor RCis C1-6 alkyl. In some embodiments, one of RBand RCis H, and the other of RBor RCis -C(O)RH. As generally described herein, RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with -OH, -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis C1-4alkyl-aryl, wherein aryl is substituted with one of -OH, -SO2F, -SO2- heteroaryl, or -OSO2F. In some embodiments, RHis C1-4 alkyl-aryl, wherein aryl is substituted with -OH. In some embodiments, RHis C1-4alkyl-aryl, wherein aryl is substituted with one of - SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis C1-4alkyl-aryl, wherein aryl is substituted with one of -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis C1-4 alkyl-aryl, wherein aryl is substituted with -SO2F. In some embodiments, RHis C1-4alkyl-aryl, wherein aryl is substituted with -SO2-heteroaryl. In some embodiments, RHis C1-4alkyl-aryl, wherein aryl is substituted with -OSO2F. In some embodiments, RHis C1-4 alkyl-phenyl, wherein phenyl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis C1-4alkyl- phenyl, wherein phenyl is optionally substituted with -OH, -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis C1-4 alkyl-phenyl, wherein phenyl is optionally substituted with - OH. In some embodiments, RHis C1-4alkyl-phenyl, wherein phenyl is optionally substituted with -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis C1-4alkyl-phenyl, wherein phenyl is optionally substituted with -OSO2F. 42 Attorney Docket No.: A2219-7000WO In some embodiments, RHis C1 alkyl-phenyl, wherein phenyl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis CH2-phenyl, wherein phenyl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis CH2-phenyl, wherein phenyl is optionally substituted with -OH, - SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis CH2-phenyl, wherein phenyl is optionally substituted with -OH. In some embodiments, RHis CH2-phenyl, wherein phenyl is optionally substituted with -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis CH2-phenyl, wherein phenyl is optionally substituted with -OSO2F. In some embodiments, RHis C2alkyl-phenyl, wherein phenyl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis CH2CH2- phenyl, wherein phenyl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or - OSO2F. In some embodiments, RHis C3 alkyl-phenyl, wherein phenyl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F. In some embodiments, RHis C4alkyl- phenyl, wherein phenyl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or - OSO2F. In some embodiments, the bifunctional compound of Formula (I) does not comprise x=1 (e.g., only one FAP Ligand) plus RHis C1-4alkyl-aryl, wherein aryl is substituted with -OH. In some embodiments, when RHis C1-4 alkyl-aryl, wherein aryl is substituted with -OH, the bifunctional compound of Formula (I) does not comprise x=1 (e.g., only one FAP Ligand). In some embodiments, RHis C1-4alkyl-aryl, and wherein when aryl is substituted with -OH, x is not 1 (e.g., x is 2, 3, or 4). In some embodiments, when RKis H, x is not 1 (e.g., x is 2, 3, or 4). In some embodiments, one of R11aand R11bis C1-6alkyl-aryl. In some embodiments, one of R12aand R12bis C1-6 alkyl-aryl. In some embodiments, Q is absent. In some embodiments, Q is N N N(R15). In some embodiments, Q is heterocyclylene In some embodiments, N N W is N(R14) (e.g., NH). In some embodiments, W is heterocyclylene (e.g ) In some 43 Attorney Docket No.: A2219-7000WO embodiments, W is heteroalkyl (e.g , O O , wherein RFand RGare each independently H, C1-6alkyl, C1-6 heteroalkyl or C1-6 haloalkyl). In an embodiment, M is absent. In an embodiment, M is NRE(e.g., NH, X2NCH3). In an embodiment, M is heteroalkylene (e.g2 , wherein X is NH, NCH3, or O). In some embodiments, M is NRE, wherein REis selected from H, C1-4 alkyl, or cycloalkyl. In some embodiments, M is NRE, wherein REis selected from H or C1-4alkyl. In some embodiments, M is NRE, wherein REis selected from H or CH3. In some embodiments, M is NRE, wherein REis H. In some embodiments, M is NRE, wherein REis CH3. In some embodiments, M is NH. In some embodiments, M is N(CH3). As generally described herein, REmay be H, C1-4alkyl, or cycloalkyl. In some embodiments, REis H or C1-4 alkyl. In some embodiments, REis H or C1-2 alkyl. In some embodiments, REis H or CH3. In some embodiments, REis H. In some embodiments, REis CH3. In an embodiment, L2is a linker (e.g., a linker of Formula (III)). In some embodiments, z is selected from 2, 3, 4, 5, and 6. In some embodiments, y is selected from 1, 2, and 3. In some embodiments, z is 0. In some embodiments, z is 3. In some embodiments, y is 0. In some embodiments, y is 1. In some embodiments, M is absent, y is 1 and z is 3. In some embodiments, M is absent, y is 1, z is 3 and R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRCand R11bis H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, R11bis H and W is C(R13a)(R13b) wherein R13aand R13bare H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15). In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with 44 Attorney Docket No.: A2219-7000WO the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, wherein one of RBand RCis H and the other of RBand RCis - C(O)RH, RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or -OSO2F, R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, RHis C1-2alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or -OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, RHis C1-2alkyl- aryl, wherein aryl is optionally substituted with -OH or -OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, RHis C1-2alkyl-aryl, wherein aryl is substituted with -OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, RHis C2alkyl-aryl, wherein aryl is substituted with - OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some 45 Attorney Docket No.: A2219-7000WO embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH- C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH-C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or - OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH-C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis C1-2alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or - OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH-C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis C1-2 alkyl-aryl, wherein aryl is optionally substituted with -OH or -OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH-C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis C1-2alkyl-aryl, wherein aryl is substituted with -OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH- C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis C1 alkyl-aryl, wherein aryl is substituted with -OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH-C(O)CH(RH)-, 46 Attorney Docket No.: A2219-7000WO wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis -CH2- aryl, wherein aryl is substituted with -OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH-C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis -CH2-aryl, wherein aryl is phenyl substituted with -OSO2F; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH-C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis C1-2 alkyl-aryl, wherein aryl is substituted with -OH; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH- C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis C1alkyl-aryl, wherein aryl is substituted with -OH; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH-C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis -CH2- aryl, wherein aryl is substituted with -OH; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -L2-[FAP Ligand], wherein L2 is *-NH-C(O)CH(RH)-, wherein * denotes the point of attachment of L2 to the compound of Formula (III), RHis -CH2-aryl, wherein aryl is phenyl substituted with -OH; R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is N(R15) wherein R15is H. 47 Attorney Docket No.: A2219-7000WO OZ3 Z2S N Z1 In some embodiments, -SO2-heteroaryl is ON, wherein Z1, Z2, and Z3are each independently selected from CH or N. In some embodiments, -SO2-heteroaryl is Z4, wherein Z4is selected from H, F, or -OCH3. In some embodiments, the linker (e.g., L1) has the structure of Formula (III-a): R15R10bR10aa pharmaceutically acceptable salt, reof, whe10a 10b 11a 11b 12a rein: R , R , R , R , R , and R12bare each independently selected from -L2-[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl-aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or - ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; denotes the point of attachment to the FAPLigand in Formula (I); and * denotes oint of attachment to the Chelator in Formula (I). In some embodiments, the linker (e.g., L1) has the structure of Formula (III-b): 48 Attorney Docket No.: A2219-7000WO 10b 10aa pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: R10a, R10b, R11a, and R11b, are each independently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl-aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2- heteroaryl; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, - SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; denotes the point of attachment to the FAP Ligand in Formula(I); and * denotes the nt of attachment to the Chelator in Formula (I).me embodiments, the linker (e.g., L1) has the structure of Formula (III-c): R15R10bR10a* N W O r a pharmaceutically acceptable wherein: R10a, R10b, R11a, R11b, and], H, C1–6 alkyl, C1–6 haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl-aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to 49 Attorney Docket No.: A2219-7000WO which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6 heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, - SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; denotes thepoint of attachment to the FAP Ligand in Formula (I); and * denotes the point of attachmentto the Chelator in Formula (I). In some embodiments, the linker (e.g., L1) has the structure of Formula (III-d): RBRCN a pharmaceutically acceptable salt, hydrate, solvate, f, wherein: RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; denotes the point of attachment to the FAPLigand in Formula (I); and * denotes the p t of attachment to the Chelator in Formula (I).In some embodime he linker (e.g., L1) has the structure of Formula (III-e): *NNMa pharmaceutically acceptable salt, hydrate, solvate, ereof, wherein: M is selected from absent, NRE, or heteroalkylene; denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes the point of attachment to the Chelator in Formula (I). 50 Attorney Docket No.: A2219-7000WO In some embodiments, the linker (e.g., L1) has the structure of Formula (III-f): O apharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: R12aand R12bare each independently selected from -L2-[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl-aryl; or each of R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; R15is H or C1–6alkyl; Q is absent, N(R15), or heterocyclyl; M is selected from absent, NRE, or heteroalkylene; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - SO2F, -SO2-heteroaryl, -OSO2F, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl- aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10;denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes the point ofattachment to the Chelator in Formula (I). In some embodiments, the linker (e.g., L1) has the structure of Formula (III-g): H O N a pharmaceutically acceptable salt, hydrate, solvate, ereof, wherein: R10aand R10bare each independently g , , C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, - ORA, -NRBRC, C1-6 alkyl-aryl; or each of R10aand R10bmay be taken together with the carbon atom to which they are attached to form an oxo group; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, -SO2-heteroaryl, – 51 Attorney Docket No.: A2219-7000WO C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; denotes the point ofattachment to the FAP Ligand in Formula (I); and * denotes the point of attachment to theChelator in Formula (I). In some embodiments, the linker (e.g., L1) has the structure of Formula (III-h): HOO O r a pharmaceutically , , , , , r thereof, wherein: R12ais selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, - ORA, -NRBRC, C1-6alkyl-aryl; M is selected from absent, NRE, or heteroalkylene; RAis H, C1–6alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, - SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes the point of attachment to the Chelator in Formula (I). In some embodiments, the linker (e.g., L1) has the structure of Formula (III-i): HOO O N W M a pharmaceutically acceptable salt, hydrate, wherein: W is selected from C(R13a)(R13b), herein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or 52 Attorney Docket No.: A2219-7000WO heteroalkylene; R13aand R13bare each independently H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, - SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; L2is a linker; denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes thepoint of attachment to the Chelator in Formula (I). In some embodiments, the linker (e.g., L1) has the structure of Formula (III-j): HOO O N O O r a utomer thereof, wherein: RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or - OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; denotes the point of attachment to the FAPLigand in Formula (I); and * denote e point of attachment to the Chelator in Formula (I).In an embodiment, nker (e.g., L2) has the Formula (III-k): HO OO O N O O N r N N r a thereof, RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or - 53 Attorney Docket No.: A2219-7000WO OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker denotes the point of attachment to the FAPLigand in Formula (I); and denotes the point of attachment to the Chelator in Formula(I). In an embodiment, the linker (e.g., L2) has the Formula (III-l): RBRCra pharmaceutically , y , , g, , of, wherein: RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; denotes the point of attachment to the FAP Ligand in Formula (I); and ** denotes the point of attachment to the Chelator in Formula(I). In some embodiments, the linker (e.g., L1) has the structure of Formula (III-m): HOO O N XaN N M r a pharmaceutically of, wherein: Xais -O-, - N H-, or -CH2-; Rais selected from -L -[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl-aryl; M is selected from absent, NRE, or heteroalkylene; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; denotes the point of attachment to 54 Attorney Docket No.: A2219-7000WOthe FAP Ligand in Formula (I); an denotes the point of attachment to the Chelator inFormula (I). * In an embodiment, the Linker is selected fro , H O O O , or -L2-[FAP Ligand]; RK helator. ORKIn an embodiment, the Linker is selected from , H O * O N O NH NH nd 55 Attorney Docket No.: A2219-7000WO * ORKRK, wherein * denotes where the l inker connects to the Chelator, and wherein R is H, -SO2F, or -SO2-heteroaryl. ORKIn an embodiment, the Linker is selected from , * H O N O RKRK, wherein * denotes where the linker . 56 Attorney Docket No.: A2219-7000WO FAP Ligand The FAP Ligand is a moiety capable of binding to the fibroblast activation protein (FAP). In an embodiment, the FAP Ligand is capable of forming a covalent bond with FAP (e.g., a covalent bond with an amino acid residue within the FAP protein sequence). In an embodiment, the FAP Ligand is capable of forming a covalent bond with a tyrosine residue. In an embodiment, the FAP Ligand is capable of forming a covalent bond with a cysteine, lysine, serine, and / or tyrosine residue. In an embodiment, the FAP Ligand is capable of forming a covalent bond with a cysteine, lysine, and / or tyrosine residue. In an embodiment, the FAP Ligand is capable of forming a covalent bond with a cysteine residue. In an embodiment, the FAP Ligand is capable of forming a covalent bond with a lysine residue. In an embodiment, the FAP Ligand is capable of forming a covalent bond with a serine residue. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV): O R3aR3bm r a pharmaceutically acceptable salt, : Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-657 Attorney Docket No.: A2219-7000WO alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, Ring A is a monocyclic aryl or monocyclic or bicyclic heteroaryl, optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is aryl (e.g., phenyl), optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is heteroaryl (e.g., pyridinyl or quinolinyl), optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is selected from phenyl, pyridinyl, or quinolinyl, optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is selected from phenyl, pyridinyl, or quinolinyl and is not substituted. In an embodiment, Ring A is phenyl and is not substituted. In an embodiment, each R1is selected from H, halo, -B(OR2b)(OR2c), -CN, and C1-6heteroalkyl. In an embodiment, R1is halo. In an embodiment, R1is -CN. In an embodiment, R1is - B(OR2b)(OR2c). In an embodiment, both R2band R2care H. In an embodiment, R3aand R3bare independently selected from H and C1-6alkyl. In an embodiment, R3aand R3bare independently selected from H and CH3. In an embodiment, both R3aand R3bare H. In an embodiment, one of R3aand R3bis H and the other is CH3. In an embodiment, R4is selected from H and C1-6 alkyl. In an embodiment, R4is selected from H and CH3. In an embodiment, R4is H. In an embodiment, each R5is selected from halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, aryl, and heteroaryl, wherein each aryl, and heteroaryl are optionally further substituted. In an embodiment, R5is - OH, -OSO2F, -SO2F, -SO2-heteroaryl, or aryl, wherein each aryl and heteroaryl is optionally further substituted. In an embodiment, R5is -OH. In an embodiment, R5is -OSO2F. In an embodiment, R5is -SO2F. In an embodiment, R5is -SO2-heteroaryl. In an embodiment, R5is aryl, which is optionally further substituted. In an embodiment, R6aand R6bare each independently selected from H and C1-6alkyl. In an embodiment, both R6aand R6bare H. In an embodiment, X is absent. In an embodiment, X is -N(R7)-. In an embodiment, X is -O-. In an embodiment, R7is H or C1-6 alkyl. In an embodiment, R7is H. In an embodiment, R7is CH3. In an embodiment, m is 1 or 2. In an embodiment, m is 1. In an embodiment, n is 1. In an embodiment, o is 0 or 1. In an embodiment, o is 0. In an embodiment, o is 1. In an embodiment, p is 1, 2, 3, or 4. In an embodiment, p is 1, 2, or 3. In an embodiment, p is 1. In an embodiment, p is 3. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-a): 58 Attorney Docket No.: A2219-7000WO r a pharmaceutically acceptable salt, s olvate, hydrate, tautomer, or stereoisomer thereof, wherein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-b): O R3aR3bm N a pharmaceutically acceptable salt, : Ring A is selected from monocyclic th 1-5 occurrences of R5; each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R1ais selected from - OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each 59 Attorney Docket No.: A2219-7000WO independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-c): R5aO R3aR3bm r a pharmaceutically acceptable salt, Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; each R5a, R5a’, R5b, and R5b’are independently selected from H, halo, -OH, - OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, R5a, R5a’, R5b, and R5b’are all H. 60 Attorney Docket No.: A2219-7000WO In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-d): r a pharmaceutically acceptable salt, s o va e, y ra e, au omer, or s ereo somer ereo , w ere n: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5k, R5l, R5m, and R5nare independently selected from H, halo, -OH, - OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-e): R6a R6bR5cO R3aR3bm N r a pharmaceutically acceptable ein: Each R1is independently 2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-661 Attorney Docket No.: A2219-7000WO alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5c, R5d, and R5eare independently selected from H, halo, -OH, - OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-f): m 6aa pharmaceutically acceptable salt, rein: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5f, R5g, R5h, and R5iare independently selected from H, halo, -OH, - OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. 62 Attorney Docket No.: A2219-7000WO In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-g): 1 a pharmaceutically acceptable salt, s o vate, y rate, tautomer, or stereo somer t ereo , w erein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R1ais selected from - OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-h): R1bR1b'O R3aR3ba pharmaceutically acceptable salt, solvate, in: Ring A is selected from monocyclic or uted with 1-5 occurrenc5 1 es of R ; Each R is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, 63 Attorney Docket No.: A2219-7000WO C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R1ais selected from - OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R1band R1b’are independently selected from H, halo, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-i): m R6a 1a pharmaceutically acceptable salt, solvate, n: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R1ais selected from -OR2a, -B(OR2b)(OR2c), - OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and 64 Attorney Docket No.: A2219-7000WO C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-j): FF), wherein each of R5f, R5g, R5h, and R5iare each , , 2F, -SO2F, -SO2-heteroaryl, optionally substituted aryl, or heteroalkyl. In an embodiment, one of R5f, R5g, R5h, and R5imust not be H. In an embodiment, a bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV-k): FF), wherein R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 , C1-6 alkyl, or C1-6 heteroalkyl (e.g., -CH2-S(O)2- CH3). In an embodiment, the FAP Ligand of Formula (IV) is selected from: O N O N H H N AP Attorney Docket No.: A2219-7000WO O the ted 66 Attorney Docket No.: A2219-7000WO O n embodiment, the FAP Ligand of Formula (IV) is: O is: is: s: CN n some embodiments, the bifunctional compound of Formula (I) is mpound in Table 1, or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof. Table 1. Exemplary Bifunctional compounds of Formula (I) Cmpd No.Structure 67 Attorney Docket No.: A2219-7000WO H 68 Attorney Docket No.: A2219-7000WO 69 Attorney Docket No.: A2219-7000WO HO F 70 Attorney Docket No.: A2219-7000WO FO SO OHNF 71 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO H 73 Attorney Docket No.: A2219-7000WO H NF 74 Attorney Docket No.: A2219-7000WO HONF 75 Attorney Docket No.: A2219-7000WO H 76 Attorney Docket No.: A2219-7000WO H 77 Attorney Docket No.: A2219-7000WO 78 Attorney Docket No.: A2219-7000WO 79 Attorney Docket No.: A2219-7000WO 80 Attorney Docket No.: A2219-7000WO 81 Attorney Docket No.: A2219-7000WO 82 Attorney Docket No.: A2219-7000WO 83 Attorney Docket No.: A2219-7000WO H 84 Attorney Docket No.: A2219-7000WO HONFNFNF Attorney Docket No.: A2219-7000WO HONFOHOH 86 Attorney Docket No.: A2219-7000WO FO SO HOHOH 87 Attorney Docket No.: A2219-7000WO HONFNFNFNF 88 Attorney Docket No.: A2219-7000WO F 89 Attorney Docket No.: A2219-7000WO 90 Attorney Docket No.: A2219-7000WO 91 Attorney Docket No.: A2219-7000WO 92 Attorney Docket No.: A2219-7000WO 93 Attorney Docket No.: A2219-7000WO 94 Attorney Docket No.: A2219-7000WO 95 Attorney Docket No.: A2219-7000WO 96 Attorney Docket No.: A2219-7000WO 97 Attorney Docket No.: A2219-7000WO FF Attorney Docket No.: A2219-7000WO NFFFF 99 Attorney Docket No.: A2219-7000WO 100 Attorney Docket No.: A2219-7000WO 101 Attorney Docket No.: A2219-7000WO 102 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO 104 Attorney Docket No.: A2219-7000WO NF 105 Attorney Docket No.: A2219-7000WO HO H O HO CNO N O O O N O N N O NH O N O NH H O O N O N HF FN O NH HO N N O HN O OH OOSO2FO 551 O HO CNO N O NH O N O O N HF FO NH N OSO2F HO OO CN Attorney Docket No.: A2219-7000WO HOCNF The compounds described herein, e.g., provided in Table 1, may be administered as drawn, or may be complexed with (i.e., radiolabeled with) a metal (e.g., a radioactive metal, e.g., a radiometal ion). For example, but not limited to, gallium, yttrium, actinium, technetium, copper, astatine, lead, scandium, indium, lutetium, dysprosium, gadolinium, samarium, lanthanum. In an embodiment, the metal is useful in therapeutics or diagnostics and imaging. In an embodiment, the metal is useful in therapeutics. In an embodiment, the metal is useful in diagnostics and imaging. In an embodiment, the metal is selected from gallium, yttrium, lutetium, actinium, or indium. In an embodiment, the metal is gallium, lutetium, or yttrium. In an embodiment, the metal is gallium. In an embodiment, the metal is yttrium. In an embodiment, the metal is actinium. In an embodiment, the metal is lutetium. The compounds described herein, e.g., provided in Table 1, may be administered as a complex with a metal isotope (i.e., a metal ion), for example, a radioactive metal isotope (i.e., a radioisotope, i.e., a radiometal ion, i.e., a radionuclide). For example,47Sc,51Cr,64Cu,67Cu, 107 Attorney Docket No.: A2219-7000WO67Ga,68Ga,72As,88Y,90Y,97Ru,99Tc,101Rh,105Rh,109Pd,111In,119Sb,128Ba,139La,140La,142Pr,149Pm,151Eu,153Eu,153Sm,159Gd,165Dy,166Ho,169Er,175Yb,177Lu,186Re,188Re,197Hg,198Au,199Ag,201Tl,203Pb,212Pb,212Bi,213Bi,225Ac, or227Th. In some embodiments, the metal isotope is a radioactive metal isotope or a fluorescent isotope. In some embodiments, the metal isotope is a radioactive metal isotope. In some embodiments, the metal isotope is a fluorescent isotope. In some embodiments, the radioisotope is selected from the group consisting of alpha radiation emitting isotopes, beta radiation emitting isotopes, gamma radiation emitting isotopes, Auger electron emitting isotopes, X-ray emitting isotopes, or fluorescence emitting isotopes. In some embodiments, the radioactive metal isotope (i.e., radioisotope) is an ion (e.g., a positively charged ion, e.g., a cation). In some embodiments, the radioactive metal isotope (i.e., radioisotope) is a positively charged ion. In some embodiments, the radioactive metal isotope (i.e., radioisotope) is a cation. In some embodiments, the radioactive metal isotope (i.e. radioisotope) is selected from47Sc,51Cr,64Cu,67Cu,67Ga,68Ga,72As,88Y,90Y,97Ru,99Tc,101Rh,105Rh,109Pd,111In,119Sb,128Ba,139 40La,142Pr,149Pm,151Eu153 153 159 165 166 , Eu, Sm, Gd, Dy, Ho,169Er,175Yb,177Lu,186Re,188Re,197Hg,198Au,199Ag,201Tl,203Pb,212Pb,212Bi,213Bi,225Ac, or227Th. In some embodiments, the radiometal isotope is selected from47Sc,51Cr,64Cu,67Cu,67Ga,68Ga,72As,88Y,90Y,97Ru,99Tc,101Rh,105Rh,109Pd,111In,119Sb,128Ba,139La,140La,142Pr,149Pm,151Eu,153Eu,153Sm,159Gd,165Dy,166Ho,169Er,175Yb,177Lu,186Re,188Re,197Hg,198Au,199Ag,201Tl,203Pb,212Pb,212Bi,213Bi,225Ac, or227Th. In some embodiments, the bifunctional compound of Formula (I) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-a) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-a) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-a) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-b) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-b) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-b) is complexed with a radioactive metal isotope (e.g., a radiometal ion). 108 Attorney Docket No.: A2219-7000WO In some embodiments, the bifunctional compound of Formula (I-c) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-c) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-c) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-d) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-d) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-d) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-e) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-e) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-e) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-f) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-f) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-f) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-g) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-g) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-g) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-h) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-h) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-h) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-i) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-i) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-i) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-j) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-j) is complexed with a 109 Attorney Docket No.: A2219-7000WO radioactive metal. In some embodiments, the bifunctional compound of Formula (I-j) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-k) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-k) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-k) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-l) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-l) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-l) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-m) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-m) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-m) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-n) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-n) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-n) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-o) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-o) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-o) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound of Formula (I-p) is complexed with a metal. In some embodiments, the bifunctional compound of Formula (I-p) is complexed with a radioactive metal. In some embodiments, the bifunctional compound of Formula (I-p) is complexed with a radioactive metal isotope (e.g., a radiometal ion). In some embodiments, the bifunctional compound is Compound 101 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 102 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 103 or a pharmaceutically acceptable 110 Attorney Docket No.: A2219-7000WO salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 104 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 105 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 106 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 107 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 108 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 109 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 110 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 111 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 112 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 113 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 114 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 115 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 116 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 117 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 118 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 119 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 120 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or 111 Attorney Docket No.: A2219-7000WO tautomer thereof. In some embodiments, the bifunctional compound is Compound 121 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 122 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 123 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 124 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 125 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 126 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 127 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 128 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 129 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 130 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 131 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 132 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 133 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 134 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 135 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 136 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 137 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or 112 Attorney Docket No.: A2219-7000WO tautomer thereof. In some embodiments, the bifunctional compound is Compound 138 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 139 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 140 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 141 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 142 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 143 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 144 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 145 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 146 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 147 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 148 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 149 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 150 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 151 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 152 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 153 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 154 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some 113 Attorney Docket No.: A2219-7000WO embodiments, the bifunctional compound is Compound 155 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 156 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 157 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 158 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 159 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 160 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 161 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 162 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 163 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 164 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 165 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 166 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 167 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 168 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 169 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 170 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 171 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is 114 Attorney Docket No.: A2219-7000WO Compound 172 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 173 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 174 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 175 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 176 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 177 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 178 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 179 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 180 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 181 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 182 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 183 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 184 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 185 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 186 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 187 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 188 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 189 or a pharmaceutically 115 Attorney Docket No.: A2219-7000WO acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 190 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 191 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 192 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 193 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 194 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 195 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 196 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 197 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 198 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 199 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 200 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 501 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 502 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 503 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 504 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 505 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 506 or a pharmaceutically acceptable salt, hydrate, solvate, 116 Attorney Docket No.: A2219-7000WO prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 507 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 508 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 509 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 510 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 511 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 512 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 513 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 514 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 515 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 516 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 517 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 518 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 519 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 520 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 521 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 522 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 523 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In 117 Attorney Docket No.: A2219-7000WO some embodiments, the bifunctional compound is Compound 524 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 525 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 526 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 527 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 528 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 529 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 530 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 531 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 532 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 533 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 534 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 535 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 536 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 537 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 538 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 539 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 540 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the 118 Attorney Docket No.: A2219-7000WO bifunctional compound is Compound 541 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 542 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 543 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 544 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 545 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 546 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 547 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 548 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 549 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 550 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 551 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 552 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 553 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound is Compound 554 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, the bifunctional compound of Formula (I) is not Compound 120 or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. FAP Ligand-Linker Compounds In one aspect, the present disclosure provides radiolabeled and compounds of Formula (V): 119 Attorney Docket No.: A2219-7000WO x (V), or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein (i) L1 comprises a linker; (ii) the FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP); and x is 1, 2, 3, or 4. Linker The present disclosure features FAP Ligand-Linker compounds comprising a FAP Ligand and a linker (e.g., L1). In some embodiments, the linker is covalently bound to the FAP Ligand. In some embodiments, the linker is a non-cleavable linker. In some embodiments, the linker is not degraded or hydrolyzed at physiological conditions. In some embodiments, the linker comprises a bond that is not cleavable in a cell (e.g., a cell organelle) or the serum, e.g., of a sample or subject. In some embodiments, the linker comprises an alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, ether, amine, alkoxy, aryl, heteroaryl, cycloalkyl, or heterocyclyl. In some embodiments, the linker comprises an alkylene or heteroalkylene. In an embodiment, the linker (L1) is absent. In some embodiments, the linker (e.g., L1) has the structure of Formula (VI): R10bR10aQWa pharmaceutically acceptable salt, hydrat of, wherein: R10a, R10b, R11a, R11b, R12a, and R1 are eac ndependent y se ected rom - -[ Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl-aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; Q is absent, NH(R15), or heterocyclyl; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom 120 Attorney Docket No.: A2219-7000WO to which they are attached to form an oxo group; R14is H or C1–6 alkyl; R15is H or C1–6 alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl- aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V). In some embodiments, each of R10a, R10b, R11a, and R11bis independently H. In some embodiments, each of R10aand R10bare independently H. In some embodiments, each of R11aand R11bare independently H. In some embodiments, each of R10aand R10bare taken together with the carbon atom to which they are attached form an oxo group. In some embodiments, each of R11aand R11bare taken together with the carbon atom to which they are attached form an oxo group. In some embodiments, each of R12aand R12bare taken together with the carbon atom to which they are attached form an oxo group. In some embodiments, one of R10aand R10bis -L2- [FAP Ligand]. In some embodiments, one of R11aand R11bis -NRBRCand the other is H. In some embodiments, one of R11aand R11bis -L2-[FAP Ligand]. In some embodiments, one of R12aand R12bis -L2-[FAP Ligand]. In some embodiments, one of R10aand R10bis C1-6 alkyl-aryl. In some embodiments, one of R11aand R11bis C1-6alkyl-aryl. In some embodiments, one of R12aand R12bis C1-6 alkyl-aryl. In some embodiments, Q is absent. In some embodiments, Q is NH(R15). In HN N some embodiments, Q is heterocyclyl (e.g., ). In some embodiments, W is N(R14) (e.g., NH). In some embodiments, W is C(R13a)(R13b) wherein R13aand R13bare each H. In some N N embodiments, W is heterocyclylen In some embodiments, W is heteroalkyl O N O O rN N N DRRFrRE F RG, wherein RFand RGare In an embodiment, M is 121 Attorney Docket No.: A2219-7000WO absent. In an embodiment, M is NRE(e.g., NH, NCH3). In an embodiment, M is heteroalkylene X2(e.g., , wherein X2is NH, NCH3, or O). In some embodiments, M is NRE, wherein REis selected from H, C1-4alkyl, or cycloalkyl. In some embodiments, M is NRE, wherein REis selected from H or C1-4 alkyl. In some embodiments, M is NRE, wherein REis selected from H or CH3. In some embodiments, M is NRE, wherein REis H. In some embodiments, M is NRE, wherein REis CH3. In some embodiments, M is NH. In some embodiments, M is N(CH3). As generally described herein, REmay be H, C1-4 alkyl, or cycloalkyl. In some embodiments, REis H or C1-4alkyl. In some embodiments, REis H or C1-2alkyl. In some embodiments, REis H or CH3. In some embodiments, REis H. In some embodiments, REis CH3. In an embodiment, L2is a linker (e.g., a linker of Formula (III)). In some embodiments, z is selected from 2, 3, 4, 5, and 6. In some embodiments, y is selected from 1, 2, and 3. In some embodiments, z is 0. In some embodiments, z is 3. In some embodiments, y is 0. In some embodiments, y is 1. In some embodiments, y is 2. As generally described herein, R15is H or C1–6alkyl. In some embodiments, R15is H or C1–4alkyl. In some embodiments, R15is H or C1–2alkyl. In some embodiments, R15is H or CH3. In some embodiments, R15is H. In some embodiments, R15is C1–6 alkyl. In some embodiments, R15is C1–4 alkyl. In some embodiments, R15is C1–2 alkyl. In some embodiments, R15is CH3. In some embodiments, one of R11aand R11bis NRBRCand the other is H. In some embodiments, one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH. In some embodiments, one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or -OSO2F. In some embodiments, one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with -OH or -OSO2F. In some embodiments, R11ais -NH-C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with - OH or -OSO2F. In some embodiments, R11ais -NH-C(O)-C1-4 alkyl-aryl, wherein aryl is substituted with one of -OH or -OSO2F. In some embodiments, R11ais -NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with -OH. In some embodiments, R11ais -NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with -OSO2F. 122 Attorney Docket No.: A2219-7000WO In some embodiments, M is absent, y is 1 and z is 3. In some embodiments, M is absent, y is 1, z is 3 and R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRCand R11bis H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, R11bis H and W is C(R13a)(R13b) wherein R13aand R13bare H. In some embodiments, M is absent, y is 1, z is 3, R10aand R10bare taken together with the carbon atom to which they are attached to form an oxo group, R11ais -NRBRC, R11bis H, W is C(R13a)(R13b) wherein R13aand R13bare H and Q is NH(R15) wherein R15is H. In some embodiments, the linker (e.g., L1) has the structure of Formula (VI-a): R15R10bR10aa pharmaceutically acceptable salt, hydrate, f, wherein: R10a, R10b,11a 11b 12a 12b R , R , R , and R are each independently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl-aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2- heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, - SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an 123 Attorney Docket No.: A2219-7000WO integer between 0 and 10; an denotes the point of attachment to the FAP Ligand in Formula (V). In some embodiments, the linker (e.g., L1) has the structure of Formula (VI-b): R10bR10aa pharmaceutically acceptable salt, hydrate, solvate, prodrug, s ereo somer, or au omer ereo , wherein: R10a, R10b, R11a, and R11b, are each independently selected from -L2-[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, - ORA, -NRBRC, C1-6 alkyl-aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from CH(R13a)(R13b), OH, NH(R14), S, heterocyclyl, or heteroalkyl, wherein each heteroalkyl and heterocyclyl is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl- aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V). In some embodiments, the linker (e.g., L1) has the structure of Formula (VI-c): R15R10bR10aHNWO r a pharmaceutically acceptable salt, , wherein: R10a, R10b, R11a, R11b, R12a, and], H, C1–6alkyl, C1–6haloalkyl, 124 Attorney Docket No.: A2219-7000WO C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl-aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; R13aand R13bare each independently H, C1–6 alkyl, C1–6 haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, - SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V). In some embodiments, the linker (e.g., L1) has the structure of Formula (VI-d): RBRCN a pharmaceutically acceptable salt, hydrate, solvate, eof, wherein: RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; and denotes the point of attachment to the FAP Ligand in Formula (V). me embodiments, one of RB In so and RCis H and the other of RBand RCis -C(O)RH. In some embodiments, one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or -OSO2F. In some embodiments, one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with -OH or -OSO2F. In some one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4 alkyl-aryl, wherein aryl is 125 Attorney Docket No.: A2219-7000WO substituted with -OH. In some embodiments, one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4 alkyl-aryl, wherein aryl is substituted with -OSO2F. In some embodiments, the linker (e.g., L1) has the structure of Formula (VI-e): HN (VI-e), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: M is selected from absent, NRE, or heteroalkylene; and denotes the point of attachment to the FAP Ligand in Formula (V). In some embodiments, the linker (e.g., L1) has the structure of Formula (VI-f): O apharmaceutically acceptable salt, hydrate,solvate, wherein:12a 12b R and R are each independently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl-aryl; or each of R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; Q is absent, N(R15), or heterocyclyl; M is selected from absent, NRE, or heteroalkylene; R15is H or C1–6alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4alkyl- aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V). I i h li k L1 h h f Formula (VI-g): H2N a pharmaceutically acceptable salt, hydrate, solvate, prodrug, 126 Attorney Docket No.: A2219-7000WO stereoisomer, or tautomer thereof, wherein: R10aand R10bare each independently selected from - L2-[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl-aryl; or each of R10aand R10bmay be taken together with the carbon atom to which they are attached to form an oxo group; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2- heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, - SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V). In some embodiments, the linker (e.g., L1) has the structure of Formula (VI-h): O O O H N O r a pharmaceutically e12a reof, wherein: R is selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, - ORA, -NRBRC, C1-6 alkyl-aryl; M is selected from absent, NRE, or heteroalkylene; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, - SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; and denotes the point of attachment to the FAP Ligand in Formula (V). In some embodi nts, the linker (e.g., L1) has the structure of Formula (VI-i): 127 Attorney Docket No.: A2219-7000WO O O O a pharmaceutically acceptable salt, hydrate, s olvate, prodrug, stereoisomer, or tautomer thereof, wherein: W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, -OSO2F, -SO2F, - SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; L2is a linker; and denotes the point of attachment to the FAP Ligand in Formula (V). n some embodiments, the linker (e.g., L1) has the structure of Formula (VI-j): O O O H2N O O N r N N r a pharmaceutically r thereof, wherein: RBand RC p y ,-6y , ; is C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; and denotes the point of attachment to the FAP Ligand in Formula (V). In an embodiment the linker (e.g., L2) has the Formula (VI-k): 128 Attorney Docket No.: A2219-7000WO O r a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or - OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker denotes the point of attachment to the FAP Ligand in Formula (I); and ** denotes the point of attachment to the Chelator in Formula(I). In an embodiment, the linker (e.g., L2) has the Formula (VI-l): RBRCOO Nr a pharmaceutically acceptable wherein: RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2-heteroaryl, or - OSO2F; r is 0, 1, 2, 3, or 4; denotes the point of attachment to the FAP Ligand in Formula(V); and ** denotes th int of attachment to the Chelator in Formula (I).I embodiments, the linker (e.g., L1) has the structure of Formula (VI-m): O O O H2N XaO N r N N H H H (VI-m), or a pharmaceutically automer thereof, wherein: Xais , , dependently selected from H, C1-6 alkyl, or -C(O)RH; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, - 129 Attorney Docket No.: A2219-7000WO SO2F, -SO2-heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; a denotes the point of attachment to the FAP Ligand in Formula (V). HN In an embodiment, the Linker is selected fro , O O d], ORKIn an embodiment, the Linker is selected from , O H2N O O NH nd Attorney Docket No.: A2219-7000WO ORKK, wherein RKis H or -SO2F. FAP Ligand The FAP Ligand is a moiety capable of binding to the fibroblast activation protein (FAP). In an embodiment, the FAP Ligand is capable of forming a covalent bond with FAP (e.g., a covalent bond with an amino acid residue within the FAP protein sequence). In an embodiment, the FAP Ligand is capable of forming a covalent bond with a tyrosine residue. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV): O R3aR3bm r a pharmaceutically acceptable salt, : Ring A is selected from monocyclic o r bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and 131 Attorney Docket No.: A2219-7000WO heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, Ring A is a monocyclic aryl or monocyclic or bicyclic heteroaryl, optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is aryl (e.g., phenyl), optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is heteroaryl (e.g., pyridinyl or quinolinyl), optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is selected from phenyl, pyridinyl, or quinolinyl, optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is selected from phenyl, pyridinyl, or quinolinyl and is not substituted. In an embodiment, Ring A is phenyl and is not substituted. In an embodiment, each R1is selected from H, halo, -B(OR2b)(OR2c), -CN, and C1-6heteroalkyl. In an embodiment, R1is halo. In an embodiment, R1is -CN. In an embodiment, R1is - B(OR2b)(OR2c). In an embodiment, both R2band R2care H. In an embodiment, R3aand R3bare independently selected from H and C1-6alkyl. In an embodiment, R3aand R3bare independently selected from H and CH3. In an embodiment, both R3aand R3bare H. In an embodiment, one of R3aand R3bis H and the other is CH3. In an embodiment, R4is selected from H and C1-6 alkyl. In an embodiment, R4is selected from H and CH3. In an embodiment, R4is H. In an embodiment, each R5is selected from halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, aryl, and heteroaryl, wherein each aryl, and heteroaryl are optionally further substituted. In an embodiment, R5is - OH, -OSO2F, -SO2F, -SO2-heteroaryl, or aryl, wherein aryl is optionally further substituted. In an embodiment, R5is -OH. In an embodiment, R5is -OSO2F. In an embodiment, R5is aryl, which is optionally further substituted. In an embodiment, R6aand R6bare each independently selected from H and C1-6 alkyl. In an embodiment, both R6aand R6bare H. In an embodiment, X is absent. In an embodiment, X is -N(R7)-. In an embodiment, X is -O-. In an embodiment, R7is H or C1-6alkyl. In an embodiment, R7is H. In an embodiment, R7is CH3. In an embodiment, m is 1 or 2. In an embodiment, m is 1. In an embodiment, n is 1. In an embodiment, o is 0 or 1. In an embodiment, o is 0. In an embodiment, o is 1. In an embodiment, p is 1, 2, 3, or 4. In an embodiment, p is 1, 2, or 3. In an embodiment, p is 1. In an embodiment, p is 3. 132 Attorney Docket No.: A2219-7000WO In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- a): r a pharmaceutically acceptable salt, s o va e, y ra e, au omer, or s ereo somer ereo , w ere n: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- b): O R3aR3bm N1a pharmaceutically acceptable salt, : Ring A is selected from monocyclic th 1-5 occurrences of R5;1 Each R is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, 133 Attorney Docket No.: A2219-7000WO C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R1ais selected from - OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- c): R5aO R3aR3bm r a pharmaceutically acceptable salt, ach R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5a, R5a’, R5b, and R5b’are independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6134 Attorney Docket No.: A2219-7000WO alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- d): r a pharmaceutically accepta , , , , , wherein each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5k, R5l, R5m, and R5nare independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV-e): R6a R6bR5cOR3a R3bm N r a pharmaceutically acceptable ein each R1is independently 2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each 135 Attorney Docket No.: A2219-7000WO independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; Each R5c, R5d, and R5eare independently selected from H, halo, -OH, - OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- f): m R6aa pharmaceutically acceptable salt, rein: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; Each R5f, R5g, R5h, and R5iare independently selected from H, halo, -OH, - OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 136 Attorney Docket No.: A2219-7000WO alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- g): a pharmaceutically acceptable salt, , , , , ein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R1ais selected from - OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- h): R1bR1b'a pharmaceutically acceptable salt, solvate, n: Ring A is selected from monocyclic or 137 Attorney Docket No.: A2219-7000WO bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R1ais selected from - OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R1band R1b’are independently selected from H, halo, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- i): a pharmaceutically acceptable salt, solvate, n: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R1ais selected from -OR2a, -B(OR2b)(OR2c), - OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; 138 Attorney Docket No.: A2219-7000WO X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- j): ), wherein each of R5f, R5g, R5h, and R5iare selected aryl, optionally substituted aryl, or heteroalkyl. In an embodiment, one of R5f, R5g, R5h, and R5imust not be H. In an embodiment, a compound of Formula (V) comprises a FAP Ligand of Formula (IV- k): ), wherein R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 l, or C1-6 heteroalkyl (e.g., -CH2-S(O)2-CH3). n an em o ment, t e gan o ormula (IV) is selected from: O N O N H H N N B N N nd 139 Attorney Docket No.: A2219-7000WO OHN , wherein R5is as defined herein. In an embodiment, the FAP O ted is: ound of Formula (V) is selected from a compound in Table 2, or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof. Table 2. Exemplary compounds of Formula (V) 140 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO F 142 Attorney Docket No.: A2219-7000WO 143 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO NH 145 Attorney Docket No.: A2219-7000WO 146 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO 148 Attorney Docket No.: A2219-7000WO 149 Attorney Docket No.: A2219-7000WO 150 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO 152 Attorney Docket No.: A2219-7000WO 153 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO 155 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO 157 Attorney Docket No.: A2219-7000WO 158 Attorney Docket No.: A2219-7000WO F 159 Attorney Docket No.: A2219-7000WO F Attorney Docket No.: A2219-7000WO 161 Attorney Docket No.: A2219-7000WO 162 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO g p In one aspect, the present disclosure provides radiolabeled and compounds of Formula (VIII): O R3aR3bm N N n (R1) a pharmaceutically acceptable salt, solvate, erein: Ring A is selected from monocyclic or stituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and 164 Attorney Docket No.: A2219-7000WO R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -NH(R7), or -OH; R7is selected from H, C1-6 alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, Ring A is a monocyclic aryl or monocyclic or bicyclic heteroaryl, optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is aryl (e.g., phenyl), optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is heteroaryl (e.g., pyridinyl or quinolinyl), optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is selected from phenyl, pyridinyl, or quinolinyl, optionally substituted with 1-5 occurrences of R5. In an embodiment, Ring A is selected from phenyl, pyridinyl, or quinolinyl and is not substituted. In an embodiment, Ring A is phenyl and is not substituted. In an embodiment, each R1is selected from H, halo, -B(OR2b)(OR2c), -CN, and C1-6 heteroalkyl. In an embodiment, R1is halo. In an embodiment, R1is -CN. In an embodiment, R1is - B(OR2b)(OR2c). In an embodiment, both R2band R2care H. In an embodiment, R3aand R3bare independently selected from H and C1-6 alkyl. In an embodiment, R3aand R3bare independently selected from H and CH3. In an embodiment, both R3aand R3bare H. In an embodiment, one of R3aand R3bis H and the other is CH3. In an embodiment, R4is selected from H and C1-6alkyl. In an embodiment, R4is selected from H and CH3. In an embodiment, R4is H. In an embodiment, each R5is selected from halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, aryl, and heteroaryl, wherein each aryl, and heteroaryl are optionally further substituted. In an embodiment, R5is - OH, -OSO2F, -SO2F, -SO2-heteroaryl, or aryl, wherein aryl is optionally further substituted. In an embodiment, R5is -OH. In an embodiment, R5is -OSO2F. In an embodiment, R5is aryl, which is optionally further substituted. In an embodiment, R6aand R6bare each independently selected from H and C1-6alkyl. In an embodiment, both R6aand R6bare H. In an embodiment, X is absent. In an embodiment, X is -NH(R7). In an embodiment, X is -OH. In an embodiment, R7is H or C1- 165 Attorney Docket No.: A2219-7000WO 6 alkyl. In an embodiment, R7is H. In an embodiment, R7is CH3. In an embodiment, m is 1 or 2. In an embodiment, m is 1. In an embodiment, n is 1. In an embodiment, o is 0 or 1. In an embodiment, o is 0. In an embodiment, o is 1. In an embodiment, p is 1, 2, 3, or 4. In an embodiment, p is 1, 2, or 3. In an embodiment, p is 1. In an embodiment, p is 3. In an embodiment, a compound of Formula (VIII) has the structure of Formula (VIII-a): O R3aR3b)p (VIII-a), or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- b): O R3aR3bm )p (VIII-b), or a pharmaceutically acceptable salt, solvate, of, wherein: Ring A is selected from monocyclic or 166 Attorney Docket No.: A2219-7000WO bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R1ais selected from - OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- c): R5aO R3aR3bm R5bN a pharmaceutically acceptable salt, solvate, in: Each R1is independently selected from H, halo, -ORa, -B(ORb)(ORc), -OP(O)(ORd)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5a, R5a’, R5b, and R5b’are independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -NH(R7), or -OH; R7is selected from H, C1-6 167 Attorney Docket No.: A2219-7000WO alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, R5a, R5a’, R5b, and R5b’are all H. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- d): a pharmaceutically acceptable salt, , y , , , erein: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5c, R5d, and R5eare independently selected from H, halo, -OH, - OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -NH(R7), or -OH; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- e): m R6a3b (R1R6bR3aRN )p X (VIII-e), or a pharmaceutically acceptable salt, solvate, ereof, wherein: Each R1is independently selected from H, 168 Attorney Docket No.: A2219-7000WO halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5f, R5g, R5h, and R5iare independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2- heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -NH(R7), or -OH; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII-f): O R3a 1R3b(R )pa pharmaceutically acceptable salt, solvate, Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R1ais selected from - OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; and p is 1, 2, 3, 4, 5, or 6. 169 Attorney Docket No.: A2219-7000WO In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- g): R1b')p (VIII-g), or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R1ais selected from -OR2a, - B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R1band R1b’are independently selected from H, halo, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- h): m R6a3b1R6bR3aRN (R )p a pharmaceutically acceptable salt, solvate, : Each R1is independently selected from H, )OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R1ais selected from -OR2a, -B(OR2b)(OR2c), - OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected 170 Attorney Docket No.: A2219-7000WO from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -NH(R7), or -OH; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII-i): FF), wherein each of R5f, R5g, R5h, and R5iare selected aryl, optionally substituted aryl, or heteroalkyl. In an embodiment, one of R5f, R5g, R5h, and R5imust not be H. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII-j): FF8(VIII-j), wherein R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 is H, C1-6alkyl, or C1-6heteroalkyl (e.g., -CH2-S(O)2-CH3). In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- k): 171 Attorney Docket No.: A2219-7000WO O3a 3bapharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; n is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. In an embodiment, p is 1 and R1is H. In an embodiment, p is 1, R1is H, n is 1, R3ais methyl and R3bis H. In an embodiment, p is 1, R1is H, n is 1, R3ais methyl, R3bis H and R4is H. In an embodiment, p is 1, R1is H, n is 1, R3ais methyl, R3bis H, R4is H and A is unsubstituted phenyl. In an embodiment, R2band R2care both H. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- m): NX5X4X1NX3 X2a pharmaceutically acceptable salt, solvate, hydrate n: each of X1, X2, X3, X4, and X5are selected from C, , , , H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6 heteroalkyl; Ryis selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- m’): 172 Attorney Docket No.: A2219-7000WO a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: X1and X4are independently selected from C and N; each of X2, X3, and X5are independently selected from C, C(Rx), N, N(Ry), or O; Rxis H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Ryis selected from H, C1-6 alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- n): (R1)0-7 (VIII-n), or a pharmaceutically acceptable salt, solvate, hydrate , , er thereof, wherein: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; each of X6, X7, and X8are selected from absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- n’): 173 Attorney Docket No.: A2219-7000WO 1 a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; Each of X6, X7, and X8are selected from absent, -CH-, -C(O)-, CH2, -N(R7)-, N, or -O-; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl. In some embodiments, X6is -C(O)- and X7is -N(R7)-. In an embodiment, the compound of Formula (VIII) has the structure of Formula (VIII- o): Y1O H O2N Y N a pharmaceutically acceptable salt, solvate, hydrate erein: Each R1is independently selected from H, halo, -O R , -B(OR )(OR ), -OP(O)(OR )2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; each of Y1and Y2are independently selected from CH or NH; and q is 1 or 2. 174 Attorney Docket No.: A2219-7000WO In an embodiment, the compound of Formula (VIII) is selected from: O om: OH. in thereof. Table 3. Exemplary compounds of Formula (VIII) 175 Attorney Docket No.: A2219-7000WO 176 Attorney Docket No.: A2219-7000WO 177 Attorney Docket No.: A2219-7000WO 178 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO 181 Attorney Docket No.: A2219-7000WO 182 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO 184 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO 186 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO 189 Attorney Docket No.: A2219-7000WO 190 Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO Attorney Docket No.: A2219-7000WO Methods of Use In another aspect, the disclosure provides a method of treating or preventing a disorder in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In another aspect, the disclosure provides a method of treating or preventing a disorder in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a bifunctional compound of Formula (I) which is complexed with (i.e., radiolabeled with) a metal (e.g., a radioactive metal, e.g., a radiometal ion), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. For use as a medicament, the bifunctional compound of Formula (I) is suitably complexed with (i.e., radiolabeled with) a metal (e.g., a radioactive metal, e.g., a radiometal ion). In another aspect, the disclosure provides a method of treating or preventing a cancer in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In another aspect, the disclosure provides a method of treating a cancer associated with an overexpression of FAP (Fibroblast Activation Protein-α), in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof. In some embodiments, a bifunctional compound of Formula (I) may be used to treat cancer associated with overexpression of FAP (Fibroblast Activation Protein-α). FAP (e.g., FAP protein) as referred to herein is a serine protease, which is specifically expressed in activated fibroblasts and is overexpressed in cancer-associated fibroblasts. The FAP protein is a transmembrane glycoprotein comprising 760 amino acids. The FAP protein comprises a short 195 Attorney Docket No.: A2219-7000WO cytoplasmic N-terminal region (residues 1-6), a transmembrane region (residues 7-26), and a large extracellular region with an α / β-hydrolase domain (residues 27-53 and 493-760) and an eight- bladed β-propeller domain (residues 54-492). The FAP protein comprises an active site that is localized in the extracellular part of the protein and comprises active site residues “catalytic triad” of Ser624, Asp702, and His734in humans and mice. The FAP protein is catalytically active as a 170- kda homodimer with two N-terminal glycosylated subunits. In some embodiments, a bifunctional compound of Formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, described herein interacts with (e.g., binds to) a FAP active site residue (e.g., Ser624, Asp702, and His734). FAP has been reported to cleave several bioactive peptides and structural proteins, including neuropeptide Y (NPY), Peptide YY, Substance P (SP), and B- type natriuretic peptide (BNP), human fibroblast growth factor 21 (FGF-21), human alpha2 antiplasmin and denatured collagen I and III. NPY, FGF-21 and alpha2 antiplasmin are considered to be physiological FAP substrates. In some embodiments, a bifunctional compound of Formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof described herein interacts with (e.g., binds to, inhibits) the FAP protein. In some embodiments, a bifunctional compound of Formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof binds to the FAP protein, delivering a radioactive metal atom to the cancer cell. The present disclosure also provides methods for the treatment or prevention of a disease, disorder, or condition. In an embodiment, the disease, disorder, or condition is related to (e.g., associated with) the overexpression of FAP protein. In an embodiment, the disease, disorder, or condition comprises a proliferative disease (e.g., cancer). Such methods comprise the step of administering to the subject in need thereof an effective amount of a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, stereoisomer thereof, or a pharmaceutical composition thereof. In certain embodiments, the methods described herein include administering to a subject an effective amount of a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof. In an embodiment, the disease, disorder, or condition comprises an inflammatory condition or fibrotic condition. Such methods comprise the step of administering to the subject in need thereof an effective amount of a bifunctional compound of Formula (I), or a pharmaceutically 196 Attorney Docket No.: A2219-7000WO acceptable salt, solvate, hydrate, tautomer, stereoisomer thereof, or a pharmaceutical composition thereof. In certain embodiments, the methods described herein include administering to a subject an effective amount of a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof. In an embodiment, the disease, disorder, or condition comprises an inflammatory or fibrotic condition. In an embodiment, the disease, disorder, or condition comprises an inflammatory condition. In an embodiment, the disease, disorder, or condition comprises a fibrotic condition. In an embodiment, the disease, disorder, or condition comprises psoriasis, dermal hypersensitivity, eczema, burns, atopic dermatitis, fibrosis (e.g., kidney or lung fibrosis), endometriosis, metabolic dysfunction-associated steatohepatitis (MASH), allergic rhinitis, respiratory distress syndrome, asthma, bronchitis, tendinitis, bursitis, fever, migraine headaches, inflammatory bowel disease, Crohn's disease, gastritis, irritable bowel syndrome, colitis and colorectal cancer, atherosclerosis, thyroiditis, aplastic anemia, Hodgkin's Disease, rheumatic fever, osteoarthritis, type I diabetes, myasthenia gravis, rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis, sarcoidosis, nephrotic syndrome, renal failure, Behcet's Syndrome, polymyositis, gingivitis, graft and transplant rejection, graft versus host disease (GVHD), conjunctivitis, swelling occurring after injury, myocardial ischemia, and endotoxin shock syndrome. In an embodiment, the disease, disorder, or condition comprises endometriosis, metabolic dysfunction-associated steatohepatitis (MASH), or fibrotic diseases. In certain embodiments, the subject being treated is a mammal. In certain embodiments, the subject is a human. In certain embodiments, the subject is a domesticated animal, such as a dog, cat, cow, pig, horse, sheep, or goat. In certain embodiments, the subject is a companion animal such as a dog or cat. In certain embodiments, the subject is a livestock animal such as a cow, pig, horse, sheep, or goat. In certain embodiments, the subject is a zoo animal. In another embodiment, the subject is a research animal such as a rodent, dog, or non-human primate. In certain embodiments, the subject is a non-human transgenic animal such as a transgenic mouse or transgenic pig. A proliferative disease may also be associated with inhibition of apoptosis of a cell in a biological sample or subject. All types of biological samples described herein or known in the art are contemplated as being within the scope of the disclosure. The bifunctional compounds of 197 Attorney Docket No.: A2219-7000WO Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, and compositions thereof, may induce apoptosis, and therefore, be useful in treating and / or preventing proliferative diseases. In certain embodiments, the proliferative disease to be treated or prevented using the bifunctional compounds of Formula (I) is cancer. As used herein, the term “cancer” refers to a malignant neoplasm (Stedman’s Medical Dictionary, 25th ed.; Hensyl ed.; Williams & Wilkins: Philadelphia, 1990). All types of cancers disclosed herein or known in the art are contemplated as being within the scope of the disclosure. Exemplary cancers include, but are not limited to, acoustic neuroma; adenocarcinoma; adrenal gland cancer; anal cancer; angiosarcoma (e.g., lymphangiosarcoma, lymphangioendotheliosarcoma, hemangiosarcoma); appendix cancer; benign monoclonal gammopathy; biliary cancer (e.g., cholangiocarcinoma); bladder cancer; breast cancer (e.g., adenocarcinoma of the breast, papillary carcinoma of the breast, mammary cancer, medullary carcinoma of the breast); brain cancer (e.g., meningioma, glioblastomas, glioma (e.g., astrocytoma, oligodendroglioma), medulloblastoma); bronchus cancer; carcinoid tumor; cervical cancer (e.g., cervical adenocarcinoma); choriocarcinoma; chordoma; craniopharyngioma; colorectal cancer (e.g., colon cancer, rectal cancer, colorectal adenocarcinoma); connective tissue cancer; epithelial carcinoma; ependymoma; endotheliosarcoma (e.g., Kaposi’s sarcoma, multiple idiopathic hemorrhagic sarcoma); endometrial cancer (e.g., uterine cancer, uterine sarcoma); esophageal cancer (e.g., adenocarcinoma of the esophagus, Barrett’s adenocarcinoma); Ewing’s sarcoma; eye cancer (e.g., intraocular melanoma, retinoblastoma); familiar hypereosinophilia; gall bladder cancer; gastric cancer (e.g., stomach adenocarcinoma); gastrointestinal stromal tumor (GIST); germ cell cancer; head and neck cancer (e.g., head and neck squamous cell carcinoma, oral cancer (e.g., oral squamous cell carcinoma), throat cancer (e.g., laryngeal cancer, pharyngeal cancer, nasopharyngeal cancer, oropharyngeal cancer), e.g., adenoid cystic carcinoma (ACC)); hematopoietic cancers (e.g., leukemia such as acute lymphocytic leukemia (ALL) (e.g., B-cell ALL, T-cell ALL), acute myelocytic leukemia (AML) (e.g., B-cell AML, T-cell AML), chronic myelocytic leukemia (CML) (e.g., B-cell CML, T-cell CML), and chronic lymphocytic leukemia (CLL) (e.g., B-cell CLL, T-cell CLL)); lymphoma such as Hodgkin lymphoma (HL) (e.g., B-cell HL, T-cell HL) and non-Hodgkin lymphoma (NHL) (e.g., B-cell NHL such as diffuse large cell lymphoma (DLCL) (e.g., diffuse large B-cell lymphoma), follicular lymphoma, chronic lymphocytic leukemia / small lymphocytic lymphoma (CLL / SLL), mantle cell lymphoma (MCL), 198 Attorney Docket No.: A2219-7000WO marginal zone B-cell lymphomas (e.g., mucosa-associated lymphoid tissue (MALT) lymphomas, nodal marginal zone B-cell lymphoma, splenic marginal zone B-cell lymphoma), primary mediastinal B-cell lymphoma, Burkitt lymphoma, lymphoplasmacytic lymphoma (i.e., Waldenström’s macroglobulinemia), hairy cell leukemia (HCL), immunoblastic large cell lymphoma, precursor B-lymphoblastic lymphoma and primary central nervous system (CNS) lymphoma; and T-cell NHL such as precursor T-lymphoblastic lymphoma / leukemia, peripheral T-cell lymphoma (PTCL) (e.g., cutaneous T-cell lymphoma (CTCL) (e.g., mycosis fungoides, Sezary syndrome), angioimmunoblastic T-cell lymphoma, extranodal natural killer T-cell lymphoma, enteropathy type T-cell lymphoma, subcutaneous panniculitis-like T-cell lymphoma, and anaplastic large cell lymphoma); a mixture of one or more leukemia / lymphoma as described above; and multiple myeloma (MM)), heavy chain disease (e.g., alpha chain disease, gamma chain disease, mu chain disease); hemangioblastoma; hypopharynx cancer; inflammatory myofibroblastic tumors; immunocytic amyloidosis; kidney cancer (e.g., nephroblastoma a.k.a. Wilms’ tumor, renal cell carcinoma); liver cancer (e.g., hepatocellular cancer (HCC), malignant hepatoma); lung cancer (e.g., bronchogenic carcinoma, small cell lung cancer (SCLC), non-small cell lung cancer (NSCLC), adenocarcinoma of the lung); leiomyosarcoma (LMS); mastocytosis (e.g., systemic mastocytosis); muscle cancer; myelodysplastic syndrome (MDS); mesothelioma; myeloproliferative disorder (MPD) (e.g., polycythemia vera (PV), essential thrombocytosis (ET), agnogenic myeloid metaplasia (AMM) a.k.a. myelofibrosis (MF), chronic idiopathic myelofibrosis, chronic myelocytic leukemia (CML), chronic neutrophilic leukemia (CNL), hypereosinophilic syndrome (HES)); neuroblastoma; neurofibroma (e.g., neurofibromatosis (NF) type 1 or type 2, schwannomatosis); neuroendocrine cancer (e.g., gastroenteropancreatic neuroendocrine tumor (GEP-NET), carcinoid tumor); osteosarcoma (e.g., bone cancer); ovarian cancer (e.g., cystadenocarcinoma, ovarian embryonal carcinoma, ovarian adenocarcinoma); papillary adenocarcinoma; pancreatic cancer (e.g., pancreatic adenocarcinoma, intraductal papillary mucinous neoplasm (IPMN), Islet cell tumors); penile cancer (e.g., Paget’s disease of the penis and scrotum); pinealoma; primitive neuroectodermal tumor (PNT); plasma cell neoplasia; paraneoplastic syndromes; intraepithelial neoplasms; prostate cancer (e.g., prostate adenocarcinoma); rectal cancer; rhabdomyosarcoma; salivary gland cancer; skin cancer (e.g., squamous cell carcinoma (SCC), keratoacanthoma (KA), melanoma, basal cell carcinoma (BCC)); small bowel cancer (e.g., appendix cancer); soft tissue sarcoma (e.g., malignant fibrous 199 Attorney Docket No.: A2219-7000WO histiocytoma (MFH), liposarcoma, malignant peripheral nerve sheath tumor (MPNST), chondrosarcoma, fibrosarcoma, myxosarcoma); sebaceous gland carcinoma; small intestine cancer; sweat gland carcinoma; synovioma; testicular cancer (e.g., seminoma, testicular embryonal carcinoma); thyroid cancer (e.g., papillary carcinoma of the thyroid, papillary thyroid carcinoma (PTC), medullary thyroid cancer); urethral cancer; vaginal cancer; and vulvar cancer (e.g., Paget’s disease of the vulva). In some embodiments, the cancer is selected from adenoid cystic carcinoma (ACC), acute myelocytic leukemia (AML) (e.g., B-cell AML, T-cell AML), chronic myelocytic leukemia (CML) (e.g., B-cell CML, T-cell CML), non-Hodgkin lymphoma (NHL), Burkitt lymphoma, colorectal cancer (e.g., colon cancer, rectal cancer, colorectal adenocarcinoma), prostate cancer (e.g., prostate adenocarcinoma), ovarian cancer (e.g., cystadenocarcinoma, ovarian embryonal carcinoma, ovarian adenocarcinoma), and myelodysplastic syndrome (MDS). In some embodiments, the cancer is selected from breast cancer, colorectal cancer, pancreatic cancer, lung cancer, brain cancer, intrahepatic bile duct cancer, or ovarian cancer. In an embodiment, the cancer is a cancer derived from non-epithelial tissues (e.g., melanoma and myeloma). In an embodiment, the cancer is selected from the group consisting of breast cancer, pancreatic cancer, small intestine cancer, colon cancer, multi-drug resistant colon cancer, rectal cancer, colorectal cancer, metastatic colorectal cancer, lung cancer, non-small cell lung cancer, head and neck cancer, ovarian cancer, hepatocellular cancer, esophageal cancer, hypopharynx cancer, nasopharynx cancer, larynx cancer, myeloma cells, bladder cancer, cholangiocarcinoma, clear cell renal carcinoma, neuroendocrine tumor, oncogenic osteomalacia, sarcoma, CUP (carcinoma of unknown primary), thymus cancer, desmoid tumors, glioma, astrocytoma, cervix cancer, skin cancer, kidney cancer and prostate cancer. The cell described herein may be an abnormal cell. The cell may be in vitro or in vivo. In certain embodiments, the cell is a proliferative cell. In certain embodiments, the cell is a cancer cell. In certain embodiments, the cell is a blood cell. In certain embodiments, the cell is a lymphocyte. In certain embodiments, the cell is a benign neoplastic cell. In certain embodiments, the cell is an endothelial cell. In certain embodiments, the cell is an immune cell. In certain embodiments, the cell is a neuronal cell. In certain embodiments, the cell is a glial cell. In certain embodiments, the cell is a brain cell. In certain embodiments, the cell is a fibroblast. In certain 200 Attorney Docket No.: A2219-7000WO embodiments, the cell is a primary cell, e.g., a cell isolated from a subject (e.g., a human subject). In some embodiments, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, has improved cell permeability over a reference compound, e.g., in a standard assay for measuring cell permeability. Cell permeability may be investigated, for example, using a standard assay run in either Madin-Darby Canine Kidney (MDCK) cells expressing Breast Cancer Resistance Protein (BCRP) or subclone MDCKII cells expressing Multidrug Resistance Protein 1 (MDR1); see, e.g., Drug Metabolism and Disposition 36, 268-275 (2008) and Journal of Pharmaceutical Sciences 107 2225-2235 (2018). In an embodiment, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, has a cell permeability measurement (Papp) of < 2×10-6cm s-1. In an embodiment, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, has a cell permeability measurement (Papp) of between 2-6×10-6cm s-1. In an embodiment, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, has a cell permeability measurement (Papp) of Papp greater than 6×10-6cm s-1. In an embodiment, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, has a cell permeability greater than 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, 99% or more, e.g., compared with a reference compound. The bifunctional compounds of Formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, described herein, at least in some embodiments, may exhibit one or more of the following properties: (i) increased uptake by a cancer cell (e.g., a tumor), relative to a non-cancer cell; (ii) prolonged retention at a target site, e.g., a cancer cell (e.g., a tumor); (iii) increased concentration at a cancer cell or tissue (e.g., tumor) relative to, for example, a non-cancer cell or tissue; (iv) ability to decrease the size or volume of a cancer tissue (e.g., a tumor); (v) ability for rapid elimination from the subject, e.g., through renal clearance; (vi) minimal uptake by a non-cancer cell or tissue (e.g., normal cell or tissue, e.g., kidney cell or tissue); and / or (vii) increased delivery of radiation to a cancer cell or tissue (e.g., tumor), e.g., relative to a non-cancer cell or tissue. In an embodiment, the increase or decrease observed for a certain property (e.g., (i)-(vii)) is relative to a corresponding reference. In some embodiments, a bifunctional compound of Formula (I) exhibits increased uptake by a cancer cell (e.g., a tumor). In some embodiments, a bifunctional compound of Formula (I) exhibits prolonged 201 Attorney Docket No.: A2219-7000WO retention at cancer cell (e.g., tumor). In some embodiments, a bifunctional compound of Formula (I) is present at a cancer cell or tissue (e.g., tumor) at an increased concentration relative to, for example, a non-cancer tissue / cell. In some embodiments, a bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., a tumor). In some embodiments, a bifunctional compound of Formula (I) exhibits rapid elimination from the subject, e.g., through renal clearance. In some embodiments, a bifunctional compound of Formula (I) exhibits minimal uptake by non- cancer cells or tissues (e.g., normal cells or tissues, e.g., kidney cells or tissues). In some embodiments, a bifunctional compound of Formula (I) exhibits delivery of high dose of radiation to cancer cell or tissue (e.g., tumor). In some embodiments, the bifunctional compounds of the disclosure exhibit effective tumor uptake. For example, the bifunctional compounds described herein may exhibit effective uptake by a cancer cell or tissue (e.g., tumor), e.g., relative to a reference, e.g., relative to a non- cancer cell or tissue (e.g., a “normal” cell or tissue, e.g., a “healthy” cell or tissue). In some embodiments, the bifunctional compound of Formula (I) has an increased cellular uptake, e.g., relative to a reference, e.g., relative to a non-cancer cell or tissue. In some embodiments, the bifunctional compound of Formula (I) has an increased cellular uptake, e.g., by about 5%, 10% 15%, 20%, 25%, 30%, 40%, 50%, 60%, 70%, 75%, 80%, 90%, 95%, 99% or more, by a cancer cell or tissue (e.g., tumor), e.g., relative to a reference, e.g., relative to a non-cancer cell or tissue. In some embodiments, the bifunctional compound of Formula (I) has a high, selective uptake in FAP-expressing tumors and a low uptake in non-cancer cells and tissues. In some embodiments, the bifunctional compound of Formula (I) has an increased tumor-to-kidney, tumor-to-spleen, and / or tumor-to-intestine uptake ratio. In an embodiment, a bifunctional compound of Formula (I) exhibits an injected dose per gram of tissue (%ID / g) of greater than 1%, 2%, 3%, 4%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, or greater, e.g., as shown in FIGS.1A-1B. In an embodiment, a bifunctional compound of Formula (I) exhibits an injected dose per gram of tissue (%ID / g) of greater than 5%. In an embodiment, a bifunctional compound of Formula (I) exhibits an injected dose per gram of tissue (%ID / g) of greater than 10%. In an embodiment, a bifunctional compound of Formula (I) exhibits an injected dose per gram of tissue (%ID / g) of greater than 15%. In an embodiment, a bifunctional compound of Formula (I) exhibits an injected dose per gram of tissue (%ID / g) of greater than 20%. In an embodiment, a bifunctional compound of Formula (I) exhibits an injected dose per gram of tissue 202 Attorney Docket No.: A2219-7000WO (%ID / g) of greater than 25%. In some embodiments, the bifunctional compounds of the disclosure exhibit prolonged retention at the cancer cell (e.g., tumor). For example, the bifunctional compounds described herein may be retained by a cancer cell (e.g., tumor) for a prolonged period of time, e.g., relative to a reference, e.g., a non-cancer cell or tissue. In some embodiments, the bifunctional compound of Formula (I) has a prolonged retention at the cancer cell (e.g., tumor), at a therapeutically or diagnostically relevant level e.g., at least 1 hour post-injection. In some embodiments, the bifunctional compound of Formula (I) has a prolonged retention at the cancer cell (e.g., tumor), at a therapeutically or diagnostically relevant level e.g., at least 5 min, 10 min, 20 min, 30 min, 45 min, 1 h, 2 h, 3 h, 4 h, 5 h, 6 h, 8 h, 10 h, 12 h, 16 h, 20 h, 24 h, 36 h, 48 h, 60 h, 72 h, or longer post-injection. In an embodiment, a bifunctional compound of Formula (I) exhibits a prolonged retention at the cancer cell (e.g., tumor), greater than 1 h, 6 h, 12 h, 24 h, 36 h, 48 h, or longer, e.g., as shown in FIGS. 2A-2B, 3A-3B, 4A-4B, and 5A-5B. In an embodiment, a bifunctional compound of Formula (I) exhibits a prolonged retention at the cancer cell (e.g., tumor), e.g., greater than 6 h post-injection. In an embodiment, a bifunctional compound of Formula (I) exhibits a prolonged retention at the cancer cell (e.g., tumor), e.g., greater than 12 h post-injection. In an embodiment, a bifunctional compound of Formula (I) exhibits a prolonged retention at the cancer cell (e.g., tumor), e.g., greater than 24 h post-injection. In an embodiment, a bifunctional compound of Formula (I) exhibits a prolonged retention at the cancer cell (e.g., tumor), e.g., greater than 48 h post-injection. In some embodiments, the bifunctional compounds of the disclosure exhibit an increased concentration in a cancer cell or tissue (e.g., a tumor) relative to, for example, a non-cancer tissue or cell. For example, the bifunctional compounds described herein may exhibit a high concentration ratio in a cancer cell or tissue (e.g., tumor) relative to a normal cell or tissue (e.g., non-cancer cell or tissue), e.g., a ratio of greater than 1.1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 15, 20, 25, 30, 40, 45, 50, 75, 90, or 100. In some embodiments, the bifunctional compound of Formula (I) exhibits a high concentration ratio in a cancer cell or tissue (e.g., tumor) relative to a non-cancer cell or tissue (e.g., normal cell or tissue), e.g., a ratio of greater than 1.1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 15, 20, 25, 30, 40, 45, 50, 75, 90, or 100. In some embodiments, the bifunctional compound of Formula (I) exhibits a high concentration ratio, e.g., a ratio of greater than 1.1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 15, 20, 25, 30, 40, 45, 50, 75, 90, or 100, in a cancer cell or tissue (e.g., tumor) relative to 203 Attorney Docket No.: A2219-7000WO a non-cancer cell or tissue (e.g., normal cell or tissue). In some embodiments, the bifunctional compound of Formula (I) exhibits a high concentration ratio, e.g., a ratio of greater than 5, 6, 7, 8, 9, 10, 15, 20, 25, 30, 40, 45, 50, 75, 90, or 100, in a cancer cell or tissue (e.g., tumor) relative to a non-cancer cell or tissue (e.g., normal cell or tissue). In some embodiments, the bifunctional compound of Formula (I) exhibits a high concentration ratio, e.g., a ratio of greater than 10, 15, 20, 25, 30, 40, 45, 50, 75, 90, or 100, in a cancer cell or tissue (e.g., tumor) relative to a non-cancer cell or tissue (e.g., normal cell or tissue). In some embodiments, the bifunctional compound of Formula (I) exhibits a 3-fold greater concentration in a cancer cell or tissue (e.g., tumor) relative to a non-cancer cell or tissue (e.g., normal cell or tissue). In some embodiments, the bifunctional compound of Formula (I) exhibits a 10-fold greater concentration in a cancer cell or tissue (e.g., tumor) relative to a non-cancer cell or tissue (e.g., normal cell or tissue). In some embodiments, the bifunctional compound of the disclosure is capable of reducing the size or volume of a cancer tissue (e.g., tumor). For example, the bifunctional compounds described herein may reduce the size or volume of a tumor. In some embodiments, the bifunctional compound of Formula (I) results in a reduction in the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell. In some embodiments, the bifunctional compound of Formula (I) results in a reduction in the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by about 1%, 2%, 5%, 10%, 15%, 20%, 25%, 30%, 40%, 50%, 60%, 70%, 75%, 80%, 90%, 95%, 99%, or more. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 10% (e.g., at least 15%, 20%, 25%, 30%, 40%, 50%, 60%, 70%, 75%, 80%, 90%, 95%, 99%, or more). In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor) between about 10% and 50%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 15%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 20%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 25%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer 204 Attorney Docket No.: A2219-7000WO tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 30%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 40%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 50%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 60%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 70%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type- matched cancer cell, by at least 75%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 80%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 90%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 95%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by at least 99%. In some embodiments, the bifunctional compound of Formula (I) reduces the size or volume of a cancer tissue (e.g., tumor), e.g., relative to a reference, e.g., a type-matched cancer cell, by more than 99%. In some embodiments, the bifunctional compound of Formula (I) results in the death of a cancer cell. In some embodiments, the bifunctional compounds of the disclosure exhibit rapid systemic elimination from the subject, e.g., through renal clearance. For example, the bifunctional compounds described herein may be rapidly eliminated from the subject, e.g., through systemic elimination, e.g., through renal clearance. In some embodiments, the bifunctional compound of Formula (I) exhibits rapid elimination from the subject, e.g., through systemic elimination, e.g., through renal clearance. In some embodiments, the bifunctional compound of Formula (I) exhibits rapid elimination from the subject through the kidney and bladder. 205 Attorney Docket No.: A2219-7000WO In some embodiments, the bifunctional compounds of the disclosure exhibit minimal uptake by non-cancer cells or tissues. For example, the bifunctional compounds described herein may have minimal off-target uptake (e.g., minimal uptake by non-target cells, e.g., non-cancer cells). In some embodiments, the bifunctional compound of Formula (I) exhibits minimal uptake by non-cancer cells or tissues, e.g., less than about 0.01%, 0.02%, 0.03%, 0.05%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1%, 1.5%, 2%, 3%, 4%, or 5%. In some embodiments, the bifunctional compound of Formula (I) exhibits minimal uptake by non-cancer cells or tissues, e.g., less than about 0.01%, 0.02%, 0.03%, 0.05%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1%, 1.5%, 2%, or 3%. In some embodiments, the bifunctional compound of Formula (I) exhibits minimal uptake, e.g., less than 1%, by non-cancer cells or tissues. In some embodiments, the bifunctional compounds of the disclosure exhibits delivery of high doses of radiation to cancer cells or tissues (e.g., tumor). For example, the bifunctional compounds described herein may selectively deliver high dose radiation to target cells or tissues e.g., cancer cells or tissues (e.g., tumor), e.g., relative to non-target cells or tissues (e.g., non-cancer cells or tissues, e.g., normal cells or tissues). In some embodiments, the bifunctional compound of Formula (I) exhibits delivery of high doses of radiation to cancer cells or tissues (e.g., tumor). In some embodiments, the bifunctional compound of Formula (I) selectively delivers high-dose radiation to target cells or tissues e.g., cancer cells or tissues (e.g., tumor), e.g., relative to non- target cells or tissues (e.g., non-cancer cells or tissues, e.g., normal cells or tissues). In some embodiments, the bifunctional compound of Formula (I) selectively delivers high-dose radiation to cancer cells or tissues (e.g., tumor), e.g., relative to non-cancer cells or tissues (e.g., normal cells or tissues). In some embodiments, the bifunctional compound of Formula (I) selectively delivers high-dose radiation to cancer cells or tissues (e.g., tumor) relative to non-cancer cells or tissues (e.g., normal cells or tissues). In some embodiments, the bifunctional compound of Formula (I) selectively delivers high-dose radiation to FAP-expressing cancer cells or tissues (e.g., tumor) relative to non-cancer cells or tissues (e.g., normal cells or tissues). In some embodiments, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, exhibits decreased cell efflux, e.g., over a reference compound, e.g., in a standard assay for measuring cell efflux. Cell efflux may be investigated, for example, using a standard assay run in either Madin-Darby Canine Kidney (MDCK) cells expressing Breast Cancer Resistance Protein (BCRP) or subclone MDCKII cells 206 Attorney Docket No.: A2219-7000WO expressing Multidrug Resistance Protein 1 (MDR1); see, e.g., Drug Metabolism and Disposition 36, 268-275 (2008) and Journal of Pharmaceutical Sciences 107 2225-2235 (2018). In an embodiment, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, has a cell efflux ratio of less than 1.5. In an embodiment, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, has a cell efflux ratio of between 1.5 and 5. In an embodiment, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, has a cell efflux ratio greater than 5. In an embodiment, a bifunctional compound of Formula (I), or a pharmaceutically acceptable salt thereof, e.g., as described herein, has a cell efflux ratio less than 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%, 45%, 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, 99% or more, e.g., compared with a reference compound. In certain embodiments, the methods described herein comprise the additional step of administering one or more additional pharmaceutical agents in combination with the bifunctional compound of Formula (I), a pharmaceutically acceptable salt thereof, or compositions comprising such bifunctional compound or pharmaceutically acceptable salt thereof. Such additional pharmaceutical agents include, but are not limited to, anti-proliferative agents, anti-cancer agents, anti-inflammatory agents, immunosuppressant agents, and a pain-relieving agent. Boron Neutron Capture Therapy In another aspect, the disclosure provides bifunctional compounds for the use in boron neutron capture therapy (BNCT) for the targeted treatment of cancer. In BNCT, a boron-containing compound (e.g., a boron-containing compound described herein, e.g., a boron-containing compound of Formula (I)) is administered to a subject and selectively delivered to tumor cells. The boron-containing compound accumulates preferentially in cancer cells while sparing healthy tissue. The subject is exposed to a beam of low-energy neutrons (e.g., neutrons from a nuclear reactor or accelerator), which initiates a chemical reaction in cells which have accumulated boron- 10 (e.g., boron-10 from the boron-containing compounds described herein), releasing high-energy particles (alpha particles and lithium ions) which travel approximately 5-9 micrometers, destroying the tumor cell from inside while minimizing damage to surrounding healthy tissue. The effectiveness of BNCT may depend on the boron-containing compound’s ability to selectively target tumor cells and the precise delivery of neutrons to the subject. In some embodiments, the compound comprises a boron entity for the use in boron neutron 207 Attorney Docket No.: A2219-7000WO capture therapy. In some embodiments, the boron entity is a natural boron isotope (e.g.,11B,10B). In some embodiments, the boron entity is10B. In some embodiments, the bifunctional compounds of Formula (I) described herein comprises boron-11 or boron-10. In some embodiments, the bifunctional compounds of Formula (I) described herein comprises boron-10. In some embodiments, the bifunctional compounds of Formula (I) described herein comprises boron-10, for the use in BNCT-related purposes. Advantages of this approach may include cell-level targeting, minimally invasive, and the ability to treat diffuse or inoperable tumors, including, but not limited to, glioblastomas or head and neck cancers. Use of BNCT is highly selective and may only targets cancer cells where the boron-containing molecule is located. The targeted neutron irradiation is minimally invasive and does not require a surgical approach. ENUMERATED EMBODIMENTS 1. A bifunctional compound of Formula (I): hl L1 FAP LiI), or a ph mer, or tautomer thereof, wherein: (i) the Chelator comprises a moiety capable of binding to a positively charged ion (e.g., a cation) (e.g., a radiometal ion); (ii) L1 comprises a linker; (iii) the FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP); and x is 1, 2, 3, 4, 5, or 6. 2. The bifunctional compound of embodiment 1, wherein the FAP Ligand is capable of forming a covalent bond with Fibroblast Activation Protein-α (FAP) (e.g., a covalent bond with an amino acid residue within the FAP protein sequence). 208 Attorney Docket No.: A2219-7000WO 3. The bifunctional compound of any one of the preceding embodiments, wherein the FAP ligand is capable of forming a covalent bond with a cysteine, lysine, serine, and / or tyrosine residue. 4. The bifunctional compound of any one of the preceding embodiments, wherein x is 1. 5. The bifunctional compound of any one of the preceding embodiments, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-a): Chelator L1 FAP Ligand(I-a), or a pharmaceutically acceptable salt, s olvate, hydrate, tautomer, or stereoisomer thereof, wherein: (i) the Chelator comprises a moiety capable of binding to a positively-charged ion (e.g., a cation) (e.g., a radiometal ion); (ii) L1 comprises a linker; and (iii) the FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP). 6. The bifunctional compound of any one of the preceding embodiments, wherein the bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV): O R3aR3bm r a pharmaceutically acceptable salt, sol g y y y teroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; Attorney Docket No.: A2219-7000WO R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. 7. The bifunctional compound of any one of the preceding embodiments, wherein Ring A is a monocyclic aryl or monocyclic or bicyclic heteroaryl, optionally substituted with 1-5 occurrences of R5. 8. The bifunctional compound of any one of the preceding embodiments, wherein Ring A is aryl (e.g., phenyl), optionally substituted with 1-5 occurrences of R5. 9. The bifunctional compound of any one of the preceding embodiments, wherein Ring A is heteroaryl (e.g., pyridinyl or quinolinyl), optionally substituted with 1-5 occurrences of R5. 10. The bifunctional compound of any one of the preceding embodiments, wherein Ring A is selected from phenyl, pyridinyl, or quinolinyl, optionally substituted with 1-5 occurrences of R5. 210 Attorney Docket No.: A2219-7000WO 11. The bifunctional compound of any one of the preceding embodiments, wherein Ring A is R5j5a’, R5b, R5b, R5c, R5d, R5e, R5, R5g, R5, R5, and R5jare independently selected from H, halo, -OH, - OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted. 12. The bifunctional compound of any one of the preceding embodiments, wherein Ring A is R5aR5cR5bR5f5gselected from , wherein each of R5a, R5a’, R5b, R5b’, R5c, lected from H, halo, -OH, - OSO2F, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted. 13. The bifunctional compound of any one of the preceding embodiments, wherein X is absent. 14. The bifunctional compound of any one of the preceding embodiments, wherein X is - N(R7)- or -O-. 15. The bifunctional compound of any one of the preceding embodiments, wherein X is - N(R7)- (e.g., -NH-, e.g., -N(CH3)-) 16. The bifunctional compound of any one of the preceding embodiments, wherein R7is H or C1-6 alkyl. 211 Attorney Docket No.: A2219-7000WO 17. The bifunctional compound of any one of the preceding embodiments, wherein X is -NH- or -N(CH3)-. 18. The bifunctional compound of any one of the preceding embodiments, wherein X is -O-. 19. The bifunctional compound of any one of the preceding embodiments, wherein each R1is independently selected from H, halo, -B(OR2b)(OR2c), -CN, and C1-6heteroalkyl. 20. The bifunctional compound of any one of the preceding embodiments, wherein R2band R2care each independently selected from H and C1-6alkyl. 21. The bifunctional compound of any one of the preceding embodiments, wherein both R2band R2care H. 22. The bifunctional compound of any one of the preceding embodiments, wherein R3aand R3bare independently selected from H and C1-6alkyl. 23. The bifunctional compound of any one of the preceding embodiments, wherein both R3aand R3bare H. 24. The bifunctional compound of any one of the preceding embodiments, wherein one of R3aand R3bis H and the other is CH3. 25. The bifunctional compound of any one of the preceding embodiments, wherein R4is selected from H and C1-6 alkyl. 26. The bifunctional compound of any one of the preceding embodiments, wherein R4is H. 27. The bifunctional compound of any one of the preceding embodiments, wherein each R5is selected from halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, aryl, and heteroaryl, wherein each aryl, and heteroaryl are optionally further substituted. 212 Attorney Docket No.: A2219-7000WO 28. The bifunctional compound of any one of the preceding embodiments, wherein R5is - OH, -OSO2F, -SO2F, -SO2-heteroaryl, or aryl, wherein each aryl and heteroaryl is optionally further substituted. 29. The bifunctional compound of any one of the preceding embodiments, wherein R5is - OH. 30. The bifunctional compound of any one of the preceding embodiments, wherein o is 0 or 1. 31. The bifunctional compound of any one of the preceding embodiments, wherein o is 0. 32. The bifunctional compound of any one of the preceding embodiments, wherein o is 1. 33. The bifunctional compound of any one of the preceding embodiments, wherein each R6aand R6bare independently selected from H and C1-6alkyl. 34. The bifunctional compound of any one of the preceding embodiments, wherein both R6aand R6bare H. 35. The bifunctional compound of any one of the preceding embodiments, wherein m is 1 or 2. 36. The bifunctional compound of any one of the preceding embodiments, wherein m is 1. 37. The bifunctional compound of any one of the preceding embodiments, wherein n is 1. 38. The bifunctional compound of any one of the preceding embodiments, wherein p is 1, 2, or 3. 213 Attorney Docket No.: A2219-7000WO 39. The bifunctional compound of any one of the preceding embodiments, wherein p is 1 or 2. 40. The bifunctional compound of any one of the preceding embodiments, wherein p is 1. 41. The bifunctional compound of any one of the preceding embodiments, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-c): 3aR3bO R m c), wherein: ged ion (e.g., a cation) (e.g., a radiometal ion); (ii) L1 comprises a linker; Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6 heteroalkyl C2-6 alkenyl C2-6 alkynyl and C1-6 haloalkyl; Raand R are independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, heteroaryl, and aryl are optionally further substituted; R6aand R6bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; 214 Attorney Docket No.: A2219-7000WO R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. 42. The bifunctional compound of any one of the preceding embodiments, wherein the bifunctional compound of Formula (I) comprises a Chelator of Formula (II-a): HOR20a R20ba pharmaceutically acceptable salt, solvate, hydrate, tautom R20aand R20bare independently selected from H, C1-6 alkyl, C1-6 heteroalkyl, -C(O)OH, and -C(O)OR; a is 1, 2, 3, 4, 5, or 6; b and b’ are independently selected from 0, 1, or 2; and c is 0, 1, or 2. 43. The bifunctional compound of any one of the preceding embodiments, wherein one of R20aand R20bis independently H. 44. The bifunctional compound of any one of the preceding embodiments, wherein each of R20aand R20bare independently H. 45. The bifunctional compound of any one of the preceding embodiments, wherein a is selected from 1, 2, or 3. 46. The bifunctional compound of any one of the preceding embodiments, wherein a is 1. 215 Attorney Docket No.: A2219-7000WO 47. The bifunctional compound of any one of the preceding embodiments, wherein b and b’ are both 1. 48. The bifunctional compound of any one of the preceding embodiments, wherein c is 0 or 1. 49. The bifunctional compound of any one of the preceding embodiments, wherein c is 1. 50. The bifunctional compound of any one of the preceding embodiments, wherein the chelator is selected from 1,4,7,10-tetraazacyclododecane-N,N’,N,N’-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), triethylenetetramine (TETA), 1,4,7,10- tetraazacyclododecane-1-(glutamic acid)-4,7,10-triacetic acid (DOTAGA), or ethylenediaminetetraacetic acid (EDTA). 51. The bifunctional compound of any one of the preceding embodiments, wherein the chelator is selected from 1,4,7,10-tetraazacyclododecane-N,N’,N,N’-tetraacetic acid (DOTA) or 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA). 52. The bifunctional compound of any one of the preceding embodiments, wherein the chelator is 1,4,7,10-tetraazacyclododecane-N,N’,N,N’-tetraacetic acid (DOTA). 53. The bifunctional compound of any one of the preceding embodiments, wherein the HO N O NOchelatorH. 216 Attorney Docket No.: A2219-7000WO 54. The bifunctional compound of any one of the preceding embodiments, wherein the OH H 55. The bifunctional compound of any one of the preceding embodiments, wherein the bifunctional compound of Formula (I) comprises an L1 having the structure of Formula (III): R10bR10a*QWr a pharmaceutically acceptable salt, hy of, wherein: R 0a, R0b, Ra, Rb, Ra, and Rbare each independently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl- aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; Q is absent, N(R15), or heterocyclylene; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; 217 Attorney Docket No.: A2219-7000WO R13aand R13bare each independently H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; R15is H or C1–6 alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; denotes the point of attachment to the FAP Ligand in Formula (I); and denotes the point of attachment to the Chelator in Formula (I).56. The bifunctional compound of any one of the preceding claims, wherein each of R10aand R10bare independently selected from -L2-[FAP Ligand] or H. 57. The bifunctional compound of any one of the preceding embodiments, wherein each of R10aand R10bare independently H. 58. The bifunctional compound of any one of the preceding embodiments, wherein each of R10aand R10bare taken together with the carbon atom to which they are attached form an oxo group. 59. The bifunctional compound of any one of the preceding embodiments, wherein one of R10aand R10bis -L2-[FAP Ligand]. 218 Attorney Docket No.: A2219-7000WO 60. The bifunctional compound of any one of the preceding embodiments, wherein L2 is a linker (e.g., a linker of Formula (III)). 61. The bifunctional compound of any one of the preceding embodiments, wherein one of R11aand R11bis NRBRC, wherein RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; and RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or - OSO2F. 62. The bifunctional compound of any one of the preceding embodiments, wherein one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or -OSO2F. 63. The bifunctional compound of any one of the preceding embodiments, wherein one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with -OH or -OSO2F. 64. The bifunctional compound of any one of the preceding embodiments, wherein R11ais - NH-C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with -OH or - OSO2F. 65. The bifunctional compound of any one of the preceding embodiments, wherein R11ais - NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with one of -OH or -OSO2F. 66. The bifunctional compound of any one of the preceding embodiments, wherein R11ais - NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with -OH. 67. The bifunctional compound of any one of the preceding embodiments, wherein R11ais - NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with -OSO2F. 219 Attorney Docket No.: A2219-7000WO 68. The bifunctional compound of any one of the preceding embodiments, wherein each of R11aand R11bare independently H. 69. The bifunctional compound of any one of the preceding embodiments, wherein each of R11aand R11bare taken together with the carbon atom to which they are attached form an oxo group. 70. The bifunctional compound of any one of the preceding embodiments, wherein each of R10a, R10b, R11a, and R11bis independently H. 71. The bifunctional compound of any one of the preceding embodiments, wherein Q is absent. 72. The bifunctional compound of any one of the preceding embodiments, wherein Q is N(R15). 73. The bifunctional compound of any one of the preceding embodiments, wherein Q is N N heterocyclylene ). 74. The bifunctional compound of any one of the preceding embodiments, wherein W is selected from N(R14), heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD. 75. The bifunctional compound of any one of the preceding embodiments, wherein W is N(R14) (e.g., NH). 76. The bifunctional compound of any one of the preceding embodiments, wherein W is N N heterocyclylene (e.g. ). 220 Attorney Docket No.: A2219-7000WO 77. The bifunctional compound of any one of the preceding embodiments, wherein W is . 78. The bifunctional compound of any one of the preceding embodiments, wherein W is O heteroalkyG, wherein RFand RGare , - , - - . 79. The bifunctional compound of any one of the preceding embodiments, wherein M is absent. 80. The bifunctional compound of any one of the preceding embodiments, wherein M is X2N heteroalkylene (e.g. , wherein X2is NH, NCH3, or O). 81. The bifunctional compound of any one of the preceding embodiments, wherein y is selected from 1, 2, 3, 4, or 5 82. The bifunctional compound of any one of the preceding embodiments, wherein y is 0. 83. The bifunctional compound of any one of the preceding embodiments, wherein y is 4. 84. The bifunctional compound of any one of the preceding embodiments, wherein z is selected from 2, 3, 4, 5, and 6. 85. The bifunctional compound of any one of the preceding embodiments, wherein z is 0. 221 Attorney Docket No.: A2219-7000WO 86. The bifunctional compound of any one of the preceding embodiments, wherein L1 has the structure of Formula (III-a): R15 10b 10ar a pharmaceutically acceptable salt, hyd rate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: R10a, R10b, R11a, R11b, R12a, and R12bare each independently selected from -L2-[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl- aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2 is a linker; y and z are each independently an integer between 0 and 10; denotes the point of attachment to the FAP Ligand in Formula (I); and denotes the point of attachment to the Chelator in Formula (I).222 Attorney Docket No.: A2219-7000WO 87. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-b): R10bR10aa pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereosomer, or tautomer t ereof, wherein: R10a, R10b, R11a, R11b, W, M, R13a, R13b, R14, RA, RB, RC, RD, RH, r, L2, y and z are as described in embodiment 55 denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes the point of attachmentto the Chelator in Formula (I). 88. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-c): R15R10bR10aN W r a pharmaceutically acceptable salt, hy wherein: R10a, R10b, R11a, R11b, R12a, R12b, W, R15, y and z are as defined in embodiment 55; denotes the point of attachmentto the FAP Ligand in Formula (I); and * denotes the po of attachment to the Chelator inFormula (I). 89. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-d): RBRCN * a pharmaceutically acceptable salt, hydrate, solvate, reof, wherein: RBand RCare as defined in 223 Attorney Docket No.: A2219-7000WO embodiment 55 denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes the point of attachment to the Chelator in Formula (I). 90. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-e): * a pharmaceutically acceptable salt, hydrate, solvate, g, , eof, wherein: M is as defined in embodiment 55; denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes thepoint of attachment to the Chelator in Formula (I). 91. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-f): O Q ra pharmaceutically acceptable salt,hydrate wherein: R12a, R12b, Q, M, and z are as defined in embodiment 55; denotes the point of attachment to the FAP Ligand inFormula (I); and * denot e point of attachment to the Chelator in Formula (I). 92. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-g): 224 Attorney Docket No.: A2219-7000WO O ate, prodrug , stereoisomer, or tautomer thereof, wherein: R0aand R0bare as defined in embodiment55; denotes the point of attachment to the FAP Ligand in Formula (I); an denotes the point of attachment to the Chelator in Formula (I). 93. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-h): HOO O N O r a pharma automer thereof, wherein: R12a, M, RB, RC, and r are as defined in embodiment 55; denotes the point ofattachment to the FAP Ligand in Formula (I); and * denotes the point of attachment to theChelator in Formula (I). 94. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-i): HOO O N W M r a pharmaceutically acceptable salt, hydrate wherein: W, M, RB, RC, and L2 are 225 Attorney Docket No.: A2219-7000WO as defined in embodiment 55 denotes the point of attachment to the FAP Ligand inFormula (I); and * denotes the point of attachment to the Chelator in Formula (I).95. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-j): HOO O (III-j), or a pharmaceuticall y eptable sal t, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: RB, RC, r, and L2are as defined in embodiment 55; denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes the point of attachment to the Chelator inFormula (I). 96. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-k): HO OO O N O O N r N N r a pharma er thereof, wherein: RB, RC, RH, and r are as defined in embodiment 55; denotes the point ofattachment to the FAP Ligand in Formula (I); and ** tes the point of attachment to theChelator in Formula (I). 97. The bifunctional compound of any one of the preceding embodiments, wherein L1 is selected from Formula (III-l): 226 Attorney Docket No.: A2219-7000WO RB Clly acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: RB, RC, and r are as defined in embodiment 55 denotes the point of attachment to the FAP Ligand in Formula (I); and ** denotes the point of attachment to the Chelator in Formula (I). 98. The bifunctional compound of any one of the preceding embodiments, wherein L1 is O , Attorney Docket No.: A2219-7000WO O RKRK, wherein RKis H or -SO2F; RB enotes where L1 connects to the Chelator. 99. The bifunctional compound of any one of the preceding embodiments, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-f): O R3aR3b(R1)p N f), wherein R1ais -B(O g A, R1, R2a, R2b, R2 , , , , , , , , , 1. 100. The bifunctional compound of any one of the preceding embodiments, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-i): 228 Attorney Docket No.: A2219-7000WO R21a-i), wherei n: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; R10a, R10b, R11a, R11b, R12a, and R12bare each independently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl- aryl; or each of ...
Claims
1. Attorney Docket No.: A2219-7000WO CLAIMS 1. A bifunctional compound of Formula (I): x (I), or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or tautomer thereof, wherein: (i) the Chelator comprises a moiety capable of binding to a positively charged ion (e.g., a cation) (e.g., a radiometal ion); (ii) L1 comprises a linker; (iii) the FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP); and x is 1, 2, 3, 4, 5, or 6.
2. The bifunctional compound of claim 1, wherein the FAP Ligand is capable of forming a covalent bond with Fibroblast Activation Protein-α (FAP) (e.g., a covalent bond with an amino acid residue within the FAP protein sequence).
3. The bifunctional compound of claim 1, wherein the FAP ligand is capable of forming a covalent bond with a cysteine, lysine, serine, and / or tyrosine residue.
4. The bifunctional compound of claim 1, wherein x is 1.
5. The bifunctional compound of claim 1, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-a): Chelator L1 FAP Ligand(I-a), or a pharmaceutically acceptable salt, mer thereo , wherein: ( ) e e a or compr ses a moiety capable of binding to a positively charged ion (e.g., a cation) (e.g., a radiometal ion); (ii) L1 comprises a linker; and 335 Attorney Docket No.: A2219-7000WO (iii) the FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP).
6. The bifunctional compound of claim 5, wherein the bifunctional compound of Formula (I) comprises a FAP Ligand of Formula (IV): r a pharmaceutically acceptable salt, sol , , , , Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR2c), -OP(O)(OR2d)2, -C(O)OR2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6. 336 Attorney Docket No.: A2219-7000WO 7. The bifunctional compound of claim 6, wherein Ring A is a monocyclic aryl or monocyclic or bicyclic heteroaryl, optionally substituted with 1-5 occurrences of R5.
8. The bifunctional compound of claim 6, wherein Ring A is aryl (e.g., phenyl), optionally substituted with 1-5 occurrences of R5.
9. The bifunctional compound of claim 6, wherein Ring A is heteroaryl (e.g., pyridinyl or quinolinyl), optionally substituted with 1-5 occurrences of R5.
10. The bifunctional compound of claim 6, wherein Ring A is selected from phenyl, pyridinyl, or quinolinyl, optionally substituted with 1-5 occurrences of R5. R5aR5bR5a'11. The bifunctional compound of claim 6, wherein Ring A is selected fro , 5 R5jRc R5fN R5dR5iN R5gR5e, or R5h, wherein each of R5a, R5a’, R5b, R5b’, R5c, R5d, R5e, R5f, R5g, R5h, R5i, and R5jare independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted. 337 Attorney Docket No.: A2219-7000WO R5aR<sup>5a'12. The bifunctional compound of claim 6, wherein Ring A is selected fro , R5cfg, wherein each of R5a, R5a’, R5b, R5b’, R5c, R5d, R5e, R5f, R5g, , an are n epen en y se ected from H, halo, -OH, -OSO2F, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted.
13. The bifunctional compound of claim 6, wherein X is absent.
14. The bifunctional compound of claim 6, wherein X is -N(R7< / sup>)- or -O-.
15. The bifunctional compound of claim 6, wherein X is -N(R7)- (e.g., -NH-, e.g., -N(CH3)-).
16. The bifunctional compound of claim 6, wherein R7is H or C1-6 alkyl.
17. The bifunctional compound of claim 6, wherein X is -NH- or -N(CH<sub>3)-.
18. The bifunctional compound of claim 6, wherein X is -O-.
19. The bifunctional compound of claim 6, wherein each R1is independently selected from H, halo, -B(OR2b)(OR<sup>2c), -CN, and C1-6 heteroalkyl.
20. The bifunctional compound of claim 6, wherein R2band R2care each independently selected from H and C1-6 alkyl.
21. The bifunctional compound of claim 6, wherein both R2band R2c< / sup>are H. 338 Attorney Docket No.: A2219-7000WO 22. The bifunctional compound of claim 6, wherein R3aand R3bare independently selected from H and C1-6 alkyl.
23. The bifunctional compound of claim 6, wherein both R3aand R3b< / sup>are H.
24. The bifunctional compound of claim 6, wherein one of R3aand R3bis H and the other is CH<sub>3.
25. The bifunctional compound of claim 6, wherein R4is selected from H and C1-6< / sub>alkyl.
26. The bifunctional compound of claim 6, wherein R4is H.
27. The bifunctional compound of claim 6, wherein each R5is selected from halo, -OH, - OSO2F, -SO2F, -SO2-heteroaryl, aryl, and heteroaryl, wherein each aryl, and heteroaryl are optionally further substituted.
28. The bifunctional compound of claim 6, wherein R5is -OH, -OSO2F, -SO2F, -SO2- heteroaryl, or aryl, wherein each aryl and heteroaryl is optionally further substituted.
29. The bifunctional compound of claim 6, wherein R5< / sup>is -OH.
30. The bifunctional compound of claim 6, wherein o is 0 or 1.
31. The bifunctional compound of claim 6, wherein o is 0.
32. The bifunctional compound of claim 6, wherein o is 1.
33. The bifunctional compound of claim 6, wherein each R6aand R6bare independently selected from H and C1-6< / sub>alkyl.
34. The bifunctional compound of claim 6, wherein both R6aand R6b< / sup>are H. 339 Attorney Docket No.: A2219-7000WO 35. The bifunctional compound of claim 6, wherein m is 1 or 2.
36. The bifunctional compound of claim 6, wherein m is 1.
37. The bifunctional compound of claim 6, wherein n is 1.
38. The bifunctional compound of claim 6, wherein p is 1, 2, or 3.
39. The bifunctional compound of claim 6, wherein p is 1 or 2.
40. The bifunctional compound of claim 6, wherein p is 1.
41. The bifunctional compound of claim 6, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-c): O R3aR3bm c), wherein: ged ion (e.g., a cation) (e.g., a radiometal ion); (ii) L1 comprises a linker; Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; 340 Attorney Docket No.: A2219-7000WO R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, heteroaryl, and aryl are optionally further substituted; R6aand R6bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.
42. The bifunctional compound of claim 5, wherein the bifunctional compound of Formula (I) comprises a Chelator of Formula (II-a): HOR20a R20bN a pharmaceutically acceptable salt, solvate, hydrate erein: Raand R are independently selected from H, C1-6alkyl, C1-6heteroalkyl, -C(O)OH, or -C(O)OR; a is 1, 2, 3, 4, 5, or 6; b and b’ are independently selected from 0, 1, or 2; and c is 0, 1, or 2.
43. The bifunctional compound of claim 42, wherein one of R20aand R20bis independently H. 341 Attorney Docket No.: A2219-7000WO 44. The bifunctional compound of claim 42, wherein each of R20aand R20bare independently H.
45. The bifunctional compound of claim 42, wherein a is 1, 2, or 3.
46. The bifunctional compound of claim 42, wherein a is 1.
47. The bifunctional compound of claim 42, wherein b and b’ are both 1.
48. The bifunctional compound of claim 42, wherein c is 0 or 1.
49. The bifunctional compound of claim 42, wherein c is 1.
50. The bifunctional compound of claim 42, wherein the chelator is selected from 1,4,7,10- tetraazacyclododecane-N,N’,N,N’-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-1,4,7- triacetic acid (NOTA), triethylenetetramine (TETA), 1,4,7,10-tetraazacyclododecane-1-(glutamic acid)-4,7,10-triacetic acid (DOTAGA), ethylenediaminetetraacetic acid (EDTA), or macropa.
51. The bifunctional compound of claim 42, wherein the chelator is selected from 1,4,7,10- tetraazacyclododecane-N,N’,N,N’-tetraacetic acid (DOTA) or 1,4,7-triazacyclononane-1,4,7- triacetic acid (NOTA).
52. The bifunctional compound of claim 42, wherein the chelator is 1,4,7,10- tetraazacyclododecane-N,N’,N,N’-tetraacetic acid (DOTA).
53. The bifunctional compound of claim 42, wherein the chelator is HO N O NOH . 342 Attorney Docket No.: A2219-7000WO 54. The bifunctional compound of claim 42, wherein the chelator is selected from or<img src='' class="img-anchor img-center" img-id="IMGF000344_0001" / > 55. The bifunctional compound of claim 5, wherein the bifunctional compound of Formula (I) comprises an L1 having the structure of Formula (III): R10bR10a*QWr a pharmaceutically acceptable salt, hy of, wherein: R10a, R10b, R11a, R11b, R12a, and R12bare each independently selected from -L2-[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl- aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; Q is absent, N(R15), or heterocyclylene; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; 343 Attorney Docket No.: A2219-7000WO R13aand R13bare each independently H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; R15is H or C1–6 alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; denotes the point of attachment to the FAP Ligand in Formula (I); and denotes the point of attachment to the Chelator in Formula (I).
56. The bifunctional compound of claim 55, wherein each of R10aand R10bare independently selected from -L2-[FAP Ligand] or H.
57. The bifunctional compound of claim 55, wherein each of R10aand R10bare independently H.
58. The bifunctional compound of claim 55, wherein each of R10aand R10bare taken together with the carbon atom to which they are attached form an oxo group.
59. The bifunctional compound of claim 55, wherein one of R10aand R10bis -L2-[FAP Ligand]. 344 Attorney Docket No.: A2219-7000WO 60. The bifunctional compound of claim 55, wherein L2 is a linker (e.g., a linker of Formula (III)).
61. The bifunctional compound of claim 55, wherein one of R11aand R11bis NRBRC, wherein RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; and RHis C1-4 alkyl- aryl, wherein aryl is optionally substituted with halo, -OH or -OSO<sub>2F.
62. The bifunctional compound of claim 55, wherein one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH or -OSO<sub>2F.
63. The bifunctional compound of claim 55, wherein one of R11aand R11bis NRBRC, wherein one of RBand RCis H and the other of RBand RCis -C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with -OH or -OSO2F.
64. The bifunctional compound of claim 55, wherein R11ais -NH-C(O)RH, wherein RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with -OH or -OSO<sub>2F.
65. The bifunctional compound of claim 55, wherein R11ais -NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with one of -OH or -OSO<sub>2F.
66. The bifunctional compound of claim 55, wherein R11ais -NH-C(O)-C1-4alkyl-aryl, wherein aryl is substituted with -OH.
67. The bifunctional compound of claim 55, wherein R11ais -NH-C(O)-C1-4 alkyl-aryl, wherein aryl is substituted with -OSO<sub>2F.
68. The bifunctional compound of claim 55, wherein each of R11aand R11bare independently H. 345 Attorney Docket No.: A2219-7000WO 69. The bifunctional compound of claim 55, wherein each of R11aand R11bare taken together with the carbon atom to which they are attached form an oxo group.
70. The bifunctional compound of claim 55, wherein each of R10a, R10b, R11a, and R11bis independently H.
71. The bifunctional compound of claim 55, wherein Q is absent.
72. The bifunctional compound of claim 55, wherein Q is N(R15). N 73. The bifunctional compound of claim 55, wherein Q is heterocyclylene (e. ).<img src='' class="img-anchor img-center" img-id="IMGF000347_0001" / > 74. The bifunctional compound of claim 55, wherein W is selected from N(R14), heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of R<sup>D.
75. The bifunctional compound of claim 55, wherein W is N(R14) (e.g., NH). N N 76. The bifunctional compound of claim 55, wherein W is heterocyclyle ).<img src='' class="img-anchor img-center" img-id="IMGF000347_0002" / > N N 77. The bifunctional compound of claim 55, wherein W . 346 Attorney Docket No.: A2219-7000WO 78. The bifunctional compound of claim 55, wherein W is heteroalkyl (e.g., O , wherein RFand RGare each independently H, C1-6alkyl, C1-6heteroalkyl or C1-6haloalkyl).
79. The bifunctional compound of claim 55, wherein M is absent.
80. The bifunctional compound of claim 55, wherein M is heteroalkylene (e.g., X2, wherein X2is NH, NCH3, or O).<img src='' class="img-anchor img-center" img-id="IMGF000348_0002" / > 81. The bifunctional compound of claim 55, wherein y is selected from 1, 2, 3, 4, or 5 82. The bifunctional compound of claim 55, wherein y is 0.
83. The bifunctional compound of claim 55, wherein y is 4.
84. The bifunctional compound of claim 55, wherein z is selected from 2, 3, 4, 5, and 6.
85. The bifunctional compound of claim 55, wherein z is 0.
86. The bifunctional compound of claim 55, wherein L1 has the structure of Formula (III-a): R15R10bR10a* N W r a pharmaceutically acceptable salt, hy of, wherein: ntly selected from -L2-[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl- 347 Attorney Docket No.: A2219-7000WO aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2 is a linker; y and z are each independently an integer between 0 and 10; denotes the point of attachment to the FAP Ligand in Formula (I); and denotes the point of attachment to the Chelator in Formula (I).
87. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-b): R10bR10a* W M a pharmaceutically acceptable salt, hydrate, solvate, f, wherein: R10a, R10b, R11a, R11b, W, M, and y are as described in claim 55; denotes the point of attachment to the FAP Ligand in Formula(I); and * denotes the point of attachment to the Chelator in Formula (I).348 Attorney Docket No.: A2219-7000WO 88. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-c): R15r a pharmaceutically acceptable salt, hyd rate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: R10a, R10b, R11a, R11b, R12a, R12b, W, R15, y and z are as defined in claim 55 denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes the point of attachment to the Chelator inFormula (I).<img src='' class="img-anchor img-center" img-id="IMGF000350_0003" / > 89. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-d): RBRCN a pharmaceutically acceptable salt, hydrate, solvate, reof, wherein: RBand RCare as defined in claim 55; denotes the point of attachment to the FAP Ligand in Formula (I); and * denotesthe t of attachment to the Chelator in Formula (I).<img src='' class="img-anchor img-center" img-id="IMGF000350_0005" / > 90. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-e): *NNMa pharmaceutically acceptable salt, hydrate, solvate, eof, wherein: M is as defined in claim 55; denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes t int ofattachment to the Chelator in Formula (I).<img src='' class="img-anchor img-center" img-id="IMGF000350_0008" / > 91. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-f): 349 Attorney Docket No.: A2219-7000WO O ra pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: R12a, R12b, Q, M, and z are as defined in claim 55; denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes the point of attachment to the Chelator in Formula (I).
92. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-g): H O N a pharmaceutically acceptable salt, hydrate, solvate, prodrug wherein: R10aand R10bare as defined in claim 55; denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes thepoint of attachment to the Chelator in Formula (I).<img src='' class="img-anchor img-center" img-id="IMGF000351_0004" / > 93. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-h): HOO O N O N r N M r a pharma automer thereof, wherein: R12a, M, RB, RC, and r are as defined in claim 55; denotes the point of attachmentto the FAP Ligand in Formula (I); and * denotes the t of attachment to the Chelator inFormula (I).<img src='' class="img-anchor img-center" img-id="IMGF000351_0007" / > 94. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-i): 350 Attorney Docket No.: A2219-7000WO O O O r a pharmaceutically acceptable salt, hydrate , solvate, prodrug, stereoisomer, or tautomer thereof, wherein: W, M, RB, RC, and L2are as defined in claim 55 denotes the point of attachment to the FAP Ligand in Formula (I); and * denotes the point of attachment to the Chelator in Formula (I).
95. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-j): HOO O N O O (III-j), or a pharma r, or tautomer thereof, wherein: RB, RC, r, and L2are as defined in claim 55; denotes the point of attachment to theFAP Ligand in Formula (I); and * denotes the p of attachment to the Chelator inFormula (I).<img src='' class="img-anchor img-center" img-id="IMGF000352_0005" / > 96. Th*e * bifunctional compound of claim 55, wherein L1 is selected from Formula (III-k): HO OO O N O O N N N H r H H r a pharma er thereof, wherein: RB, RC, and r are as defined in claim 55; denotes the point of attachment to the 351 Attorney Docket No.: A2219-7000WO FAP Ligand in Formula (I); an denotes the point of attachment to the Chelator inFormula (I).
97. The bifunctional compound of claim 55, wherein L1 is selected from Formula (III-l): RBRCra pharmaceuticallyaccepta , y , , p g, , f, wherein: RB, RC, and r are as defined in claim 55; denotes the point of attachment to the FAP Ligand in Formula (I); and ** denotes the point of attachment to the Chelator in Formula (I).<img src='' class="img-anchor img-center" img-id="IMGF000353_0004" / > 98. The bifunctional compound of claim 55, wherein L1 is selected from O K , 352 Attorney Docket No.: A2219-7000WO O , r - connects to t e e ator.
99. The bifunctional compound of claim 1, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-f): 353 Attorney Docket No.: A2219-7000WO 1 -f), wherein R1a is -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR2e, or -CN; and the Chelator, L1, Ring A, R1, R2a, R2b, R2c, R2d, R2e, R3a, R3b, R4, R6a, R6b, R7, and p are as defined in claim 41.
100. The bifunctional compound of claim 1, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-i): R21a2 10b 10OR3a 3b-i), wherei Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; 354 Attorney Docket No.: A2219-7000WO R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R10a, R10b, R11a, R11b, R12a, and R12bare each independently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl- aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6alkyl; R15is H or C1–6alkyl; R20aand R20bare independently selected from H, C1-6 alkyl, C1-6 heteroalkyl, -C(O)OH, and -C(O)OR; each of R21a, R21b, R21cis selected from -CH2-C(O)OH, or -CH2-heteroaryl-C(O)OH; Q is absent, N(R15), or heterocyclyl; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; L2is a linker; a is 1, 2, 3, 4, 5, or 6; b and b’ are independently selected from 0, 1, or 2; c is 0, 1, or 2; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; 355 Attorney Docket No.: A2219-7000WO p is 1, 2, 3, 4, 5, or 6; r is 0, 1, 2, 3, or 4; and y and z are each independently an integer between 0 and 10.
101. The bifunctional compound of claim 1, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-j): OH r a pharma herein: M is N(R16) or O; and Each of R13f, R13g, R13h, R13i, and R13jare independently selected from H, C1-4 alkyl, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, and substituted aryl, wherein at least one of R13f, R13h, or R13imust not be H; and R16is H or C1-4< / sub>alkyl.
102. The bifunctional compound of claim 1, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-k): OH N O r a pharma herein: R13jis halo or C1-4alkyl; and 356 Attorney Docket No.: A2219-7000WO Each of R13f, R13g, R13h, and R13iare independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, and substituted aryl, wherein at least one of R13f, R13h, or R13imust not be H.
103. The bifunctional compound of claim 1, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-l): OH r a pharma herein: M is N(CH3) or O; and Each of R13f, R13h, and R13iare independently selected from H, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, and substituted aryl, wherein one of R13f, R13h, or R13imust not be H.
104. The bifunctional compound of claim 1, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-m): R11bR11aH O Chelator N M FAP Ligand m), wherein: arged ion (e.g., a (ii) L2 comprises a linker; (iii) each FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP); 357 Attorney Docket No.: A2219-7000WO R10a, R10b, R11a, and R11bare each independently selected from H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl-aryl; or each of R10aand R10b, R11aand R11b, independently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclyl, or heteroalkylene, wherein each heteroalkyl and heterocyclyl is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; REis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; and y is an integer between 0 and 10.
105. The bifunctional compound of claim 104, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-n): O H Chelator N N H r a pharmaceutically wherein: RKis H or -SO2F; 358 Attorney Docket No.: A2219-7000WO and wherein the Chelator is as defined in claim 42 and the [FAP ligand] is a compound of formula (IV).
106. The bifunctional compound of claim 105, wherein the FAP ligand is O H .<img src='' class="img-anchor img-center" img-id="IMGF000360_0001" / > 107. The bifunctional compound of claim 104, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-o): H O Ch l t N lly is defined in claim 55 and RKis H or -SO<sub>2F.
108. The bifunctional compound of claim 104, wherein the bifunctional compound of Formula (I) is a compound of Formula (I-p): 359 Attorney Docket No.: A2219-7000WO HO O r a pharmaceutically : RKis H or -SO2F.
109. The bifunctional compound of claim 108, wherein RKis H.
110. The bifunctional compound of claim 108, wherein RK< / sup>is -SO2F.
111. The bifunctional compound of claim 1, wherein the bifunctional compound of Formula (I) is selected from any one of the compounds shown in Table 1, or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof.
112. The bifunctional compound of claim 1, wherein the bifunctional compound is complexed with a radiometal ion.
113. The bifunctional compound of claim 1, wherein the bifunctional compound comprises a radiometal ion.
114. The bifunctional compound of claim 1, wherein the bifunctional compound comprises a radiometal ion selected from47Sc,51Cr,64Cu,67Cu,67Ga,68Ga,72As,88Y,90Y,97Ru,99Tc,101Rh,105Rh,109Pd,111In,119Sb,128Ba,139La,140La,142Pr,149Pm,151Eu,153Eu,153Sm,159Gd,165Dy,166Ho, 360 Attorney Docket No.: A2219-7000WO169Er,175Yb,177Lu,186Re,188Re,197Hg,198Au,199Ag,201Tl,203Pb,212Pb,212Bi,213Bi,225Ac, or227Th.
115. The bifunctional compound of claim 1, wherein the compound comprises a radiometal ion selected from64Cu,68Ga,90Y,99Tc,153Sm,177Lu, or188Re.
116. The bifunctional compound of claim 1, wherein the compound comprises a radiometal ion selected from99Tc,64Cu,211At,177Lu,212Pb,177Lu,111In.
117. A compound of Formula (V): x (V), or a pharmaceutically acceptable salt, solvate, hydrate , au o e , o s e eo so e ereof, wherein: (i) L1 comprises a linker; (ii) the FAP Ligand comprises a moiety capable of binding to the fibroblast activation protein (FAP); and x is 1, 2, 3, or 4.
118. The compound of claim 117, wherein the compound of Formula (V) comprises an L1 of Formula (VI): R10bR10aQWa pharmaceutically acceptable salt, hydrate of, wherein: , , , , , pendently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl- aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; 361 Attorney Docket No.: A2219-7000WO Q is absent, NH(R15), or heterocyclyl; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6alkyl; R15is H or C1–6alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V).
119. The compound of claim 118, wherein the compound of Formula (V) comprises an L1 of Formula (VI-a): R15R10bR10aHN W a pharmaceutically acceptable salt, hydrate of, wherein: endently select2 ed from -L -[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl- 362 Attorney Docket No.: A2219-7000WO aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6alkyl; R15is H or C1–6alkyl; RAis H, C1–6 alkyl, C2–6 alkenyl, C2–6 alkynyl, C1–6 haloalkyl, C1–6 heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V).
120. The compound of claim 118, wherein the compound of Formula (V) comprises an L1 of Formula (VI-b): R10bR10aW M a pharmaceutically acceptable salt, hydrate, solvate, prodru , wherein: independently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl-aryl; or each of 363 Attorney Docket No.: A2219-7000WO R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from CH(R13a)(R13b), OH, NH(R14), S, heterocyclyl, or heteroalkyl, wherein each heteroalkyl and heterocyclyl is substituted with 0-4 occurrences of RD; M is selected from absent, NRE, or heteroalkylene; R13aand R13bare each independently H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V).
121. The compound of claim 118, wherein the compound of Formula (V) comprises an L1 of Formula (VI-c): R15R10bR10aHN W O r a pharmaceutically acceptable salt, hy , wherein: ly selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl- 364 Attorney Docket No.: A2219-7000WO aryl; or each of R10aand R10b, R11aand R11b, and R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; W is selected from C(R13a)(R13b), O, N(R14), S, heterocyclylene, or heteroalkylene, wherein each heteroalkylene and heterocyclylene is substituted with 0-4 occurrences of RD; R13aand R13bare each independently H, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, halo, cyano, or -ORA; or R13aand R13bmay be taken together with the carbon atom to which they are attached to form an oxo group; R14is H or C1–6 alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V).
122. The compound of claim 118, wherein the compound of Formula (V) comprises an L1 of Formula (VI-d): RBRCN a pharmaceutically acceptable salt, hydrate, solvate, reof, wherein: ted from H, C1-6alkyl, or -C(O)RH; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; and 365 Attorney Docket No.: A2219-7000WO denotes the point of attachment to the FAP Ligand in Formula (V).
123. The compound of claim 118, wherein the compound of Formula (V) comprises an L1 of Formula (VI-e): HN (VI-e), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: M is selected from absent, NRE, or heteroalkylene; and denotes the point of attachment to the FAP Ligand in Formula (V).
124. The compound of claim 118, wherein the compound of Formula (V) comprises an L1 of Formula (VI-f): O apharmaceutically acceptable salt,hydrate reof, wherein: R12aand R12bare each independently selected from -L2-[FAP Ligand], H, C1–6 alkyl, C1–6 haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6alkyl-aryl; or each of R12aand R12bindependently may be taken together with the carbon atom to which they are attached to form an oxo group; Q is absent, N(R15), or heterocyclyl; M is selected from absent, O, NRE, or heteroalkylene; R15is H or C1–6 alkyl; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6 alkyl, C1–6 haloalkyl, C1–6 heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; 366 Attorney Docket No.: A2219-7000WO RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V).
125. The compound of claim 118, wherein the compound of Formula (V) comprises an L1 of Formula (VI-g): O a pharmaceutically acceptable salt, hydrate, solvate, reof, wherein: R10aand R10bare each independently selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6 heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl-aryl; or each of R10aand R10bmay be taken together with the carbon atom to which they are attached to form an oxo group; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; y and z are each independently an integer between 0 and 10; and denotes the point of attachment to the FAP Ligand in Formula (V). 367 Attorney Docket No.: A2219-7000WO 126. The compound of claim 118, wherein the compound of Formula (V) comprises an L1 of Formula (VI-h): O O O r a pharma ceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein: R12ais selected from -L2-[FAP Ligand], H, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, halo, cyano, -ORA, -NRBRC, C1-6 alkyl-aryl; M is selected from absent, NRE, or heteroalkylene; RAis H, C1–6alkyl, C2–6alkenyl, C2–6alkynyl, C1–6haloalkyl, C1–6heteroalkyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl; RBand RCare each independently selected from H, C1-6 alkyl, or -C(O)RH; RDis selected from halo, C1–6alkyl, C1–6haloalkyl, C1–6heteroalkyl, cyano, -ORA, - OSO2F, -SO2F, -SO2-heteroaryl, –C(O)OCH2-aryl, and –C(O)OCH2-heteroaryl; RHis C1-4 alkyl-aryl, wherein aryl is optionally substituted with halo, -OH, -SO2F, -SO2- heteroaryl, or -OSO2F; r is 0, 1, 2, 3, or 4; L2is a linker; and denotes the point of attachment to the FAP Ligand in Formula (V).
127. The compound of claim 117, wherein the compound of Formula (V) comprises a FAP Ligand of Formula (IV): O R3aR3bm N1r a pharmaceutically acceptable salt, sol 368 Attorney Docket No.: A2219-7000WO Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; X is absent, -N(R7)-, or -O-; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.
128. The compound of claim 117, wherein the compound of Formula (V) is selected from any one of the compounds shown in Table 2, or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof.
129. A compound of Formula (VIII): 369 Attorney Docket No.: A2219-7000WO r a pharmaceutically acceptable salt, sol vate, hydrate, tautomer, or stereoisomer thereof, wherein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; X is absent, -NH(R7)-, or -OH; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.
130. The compound of claim 129, wherein the compound of Formula (VIII) has the structure of Formula (VIII-a): 370 Attorney Docket No.: A2219-7000WO )p (VIII-a), or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.
131. The compound of claim 129, wherein the compound of Formula (VIII) is a compound of Formula (VIII-b): 371 Attorney Docket No.: A2219-7000WO )p (VIII-b), or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R1ais selected from -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, 1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.
132. The compound of claim 129, wherein the compound of Formula (VIII) is a compound of Formula (VIII-c): 372 Attorney Docket No.: A2219-7000WO r a pharmaceutically acceptable salt, sol vate, hydrate, tautomer, or stereoisomer thereof, wherein: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5a, R5a’, R5b, and R5b’are independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; X is absent, -NH(R7), or -OH; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.
133. The compound of claim 129, wherein the compound of Formula (VIII) is a compound of Formula (VIII-d): 373 Attorney Docket No.: A2219-7000WO r a pharmaceutically accepta ble salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5c, R5d, and R5eare independently selected from H, halo, -OH, -OSO2F, -SO2F, - SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6heteroalkyl; X is absent, -NH(R7), or -OH; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.
134. The compound of claim 129, the compound of Formula (VIII) is a compound of Formula (VIII-e): 374 Attorney Docket No.: A2219-7000WO m ble ac s epe e y se ec e o , a o, - , - , - R2d)2, -C(O)OR2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5f, R5g, R5h, and R5iare independently selected from H, halo, -OH, -OSO2F, - SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; X is absent, -NH(R7), or -OH; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.
135. The compound of claim 129, wherein the compound of Formula (VIII) is a compound of Formula (VIII-f): 375 Attorney Docket No.: A2219-7000WO 1)p (VIII-f), or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R1ais selected from -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; R7is selected from H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; and p is 1, 2, 3, 4, 5, or 6.
136. The compound of claim 129, wherein the compound of Formula (VIII) is a compound of Formula (VIII-g): R1bR1b'O R3aR3b)p(VIII-g), or a pharmaceutically acceptable salt, solvate, hydrat reof, wherein: 376 Attorney Docket No.: A2219-7000WO Ring A is selected from monocyclic or bicyclic aryl or heteroaryl ring, optionally substituted with 1-5 occurrences of R5; Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C1-6 heteroalkyl; R1ais selected from -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R1band R1b’are independently selected from H, halo, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; R3aand R3bare independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6heteroalkyl; R4is H, C1-6 alkyl, C2-6 alkenyl, C1-6 haloalkyl, and C1-6 heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; and p is 1, 2, 3, 4, 5, or 6.
137. The compound of claim 129, wherein the compound of Formula (VIII) is a compound of Formula (VIII-h): m R6a3b (R1R6b 3aRN )p a pharmaceutically acceptable salt, solvate, n: p y , , -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R1ais selected from -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR2e, and -CN; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6heteroalkyl, C2-6alkenyl, C2-6alkynyl, and C1-6haloalkyl; 377 Attorney Docket No.: A2219-7000WO R3aand R3bare independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halo, and C1-6 heteroalkyl; R4is H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; Each R5is independently selected from H, halo, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 heteroalkyl, aryl, and heteroaryl, wherein each alkyl, alkenyl, alkynyl, heteroalkyl, aryl, and heteroaryl are optionally further substituted; R6aand R6bare each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halo, and C1-6 heteroalkyl; X is absent, -NH(R7), or -OH; R7is selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; m is selected from 0, 1, 2, or 3; n is 0, 1, or 2; o is 0, 1, or 2; and p is 1, 2, 3, 4, 5, or 6.
138. The compound of claim 129, wherein the compound of Formula (VIII) is a compound of Formula (VIII-i): FFN (VIII-i), or a pharmaceutically acceptable salt, solvate r thereof, wherein: each of R5f, R5g, R5h, and R5iare selected from H, -OH, -OSO2F, -SO2F, -SO2-heteroaryl, optionally substituted aryl, or heteroalkyl, wherein one of R5f, R5g, R5h, and R5imust not be H.
139. The compound of claim 129, wherein the compound of Formula (VIII) is a compound of Formula (VIII-m’): 378 Attorney Docket No.: A2219-7000WO a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof, wherein: X1and X4are independently selected from C and N; each of X2, X3, and X5are selected from C, C(Rx), N, N(Ry), or O; Rxis selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl; and Ryis selected from H, C1-6alkyl, C2-6alkenyl, C1-6haloalkyl, and C1-6heteroalkyl.
140. The compound of claim 129, wherein the compound of Formula (VIII) is a compound of Formula (VIII-o): Y1O H N a pharmaceutically acceptable salt, solvate, hydrate erein: Each R1is independently selected from H, halo, -OR2a, -B(OR2b)(OR<sup>2c), -OP(O)(OR2d)2, -C(O)OR<sup>2e, -CN, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl, and C1-6heteroalkyl; R2a, R2b, R2c, R2d, and R2eare each independently selected from H, halo, -SO2F, C1-6 alkyl, C1-6 heteroalkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl; each of Y1and Y2are independently selected from CH or NH; and q is 1 or 2.
141. The compound of claim 129, wherein the compound of Formula (VIII) is selected from any one of the compounds shown in Table 3 or a pharmaceutically acceptable salt, solvate, hydrate, tautomer, or stereoisomer thereof.
142. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable excipient. 379 Attorney Docket No.: A2219-7000WO 143. A composition for use in treating a disease or disorder in a subject comprising administering to the subject a compound of Formula (I), according to claim 1.
144. The composition for use of claim 143, wherein the disease or disorder comprises a proliferative disease (e.g., cancer, a benign neoplasm, or angiogenesis).
145. The composition for use of claim 144, wherein the disease or disorder comprises a neurological disease or disorder, autoimmune disease or disorder, immunodeficiency disease or disorder, lysosomal storage disease or disorder, cardiovascular disease or disorder, metabolic disease or disorder, respiratory disease or disorder, renal disease or disorder, or infectious disease.
146. The composition for use of claim 144, wherein the disease or disorder comprises cancer.
147. A composition for use in treating a disease or disorder in a subject comprising administering to the subject a compound of Formula (I), according to claim 1, wherein the compound of Formula (I) is complexed with a radiometal ion.
148. The composition for use of claim 147, wherein the disease or disorder comprises a proliferative disease (e.g., cancer, a benign neoplasm, or angiogenesis).
149. The composition for use of claim 148, wherein the disease or disorder comprises a neurological disease or disorder, autoimmune disease or disorder, immunodeficiency disease or disorder, lysosomal storage disease or disorder, cardiovascular disease or disorder, metabolic disease or disorder, respiratory disease or disorder, renal disease or disorder, or infectious disease.
150. The composition for use of claim 148, wherein the disease or disorder comprises cancer.
151. A method for treating a disease or disorder in a subject comprising administering to the subject a compound of Formula (I), according to claim 1. 380 Attorney Docket No.: A2219-7000WO 152. The method of claim 151, wherein the disease or disorder comprises a proliferative disease (e.g., cancer, a benign neoplasm, or angiogenesis).
153. The method of claim 151, wherein the disease or disorder comprises a neurological disease or disorder, autoimmune disease or disorder, immunodeficiency disease or disorder, lysosomal storage disease or disorder, cardiovascular disease or disorder, metabolic disease or disorder, respiratory disease or disorder, renal disease or disorder, or infectious disease.
154. The method of claim 152, wherein the disease or disorder comprises cancer.
155. A method for treating a disease or disorder in a subject comprising administering to the subject a compound of Formula (I), according to claim 1, wherein the compound of Formula (I) is complexed with a radiometal ion.
156. The method of claim 155, wherein the disease or disorder comprises a proliferative disease (e.g., cancer, a benign neoplasm, or angiogenesis).
157. The method of claim 155, wherein the disease or disorder comprises a neurological disease or disorder, autoimmune disease or disorder, immunodeficiency disease or disorder, lysosomal storage disease or disorder, cardiovascular disease or disorder, metabolic disease or disorder, respiratory disease or disorder, renal disease or disorder, or infectious disease.
158. The method of claim 156, wherein the disease or disorder comprises cancer.
159. The bifunctional compound of claim 1, wherein the bifunctional compound of Formula (I) complexed with a radiometal ion exhibits one or more of the following properties: (i) uptake by a cancer cell (e.g., a tumor); (ii) prolonged retention at cancer cell (e.g., tumor); (iii) is present at a cancer cell or tissue (e.g., tumor) at an increased concentration relative to, for example, a non-cancer tissue / cell; 381 Attorney Docket No.: A2219-7000WO (iv) reduces the size or volume of a cancer tissue (e.g., a tumor); (v) rapid elimination from the subject, e.g., through renal clearance; (vi) minimal uptake by non-cancer cells or tissues (e.g., normal cells or tissues, e.g., kidney cells or tissues); and / or (vii) delivery of high dose of radiation to a cancer cell or tissue (e.g., tumor). 382
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