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Androgen Receptor Signaling Pathway Map

Androgen Receptor Products

All (48)
Androgen Receptor Inhibitors (11)
Androgen Receptor Antagonists (19)
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New Androgen Receptor Products

Catalog No.	Product Name	Information	Product Use Citations
S0097	(S,R,S)-AHPC (MDK7526)	(S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC is potential useful for the targeted degradation of the androgen receptor. (S,R,S)-AHPC can be connected to the ligand for protein such as BCR-ABL1 by a linker to form PROTACs such as GMB-475. GMB-475 induces the degradation of BCR-ABL1 with IC50 of 1.11 μM in Ba/F3 cells.
S1123	Abiraterone (CB-7598)	Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.	Cancer Cell, 2021, S1535-6108(21)00659-0 Cancers (Basel), 2021, 13(16)3959 Sci Rep, 2021, 11(1):10765
S1195	TAK-700 (Orteronel)	TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3.	Drug Metab Dispos, 2017, 45(6):635-645 Biochem Biophys Res Commun, 2016, 477(4):1005-10
S1304	Megestrol Acetate	Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.	Hum Cell, 2022, 10.1007/s13577-022-00671-y Hum Cell, 2021, 34(6):1911-1918 Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1353	Ketoconazole (R 41400)	Ketoconazole (R 41400) inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4 Nat Commun, 2021, 12(1):652 Pharmacol Res, 2021, 169:105648
S2246	Abiraterone Acetate (CB7630)	Abiraterone Acetate (CB7630) is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor.	Clin Cancer Res, 2021, clincanres.4391.2020 Neoplasia, 2021, 23(12):1261-1274 J Biol Chem, 2021, 297(2):100969
S2840	Apalutamide (ARN-509)	Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.	Prostate, 2022, 82(3):314-322 J Pathol, 2021, 10.1002/path.5652 Nat Commun, 2020, 19;11(1):2508
S6885	Ailanthone	Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.
S6965^New	Bavdegalutamide (ARV-110)	Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR. ARV-110 completely degrades androgen receptor (AR) in all cell lines tested with DC50 of < 1 nM. ARV-110 can be used for the research of prostate cancer.
S7040	AZD3514	AZD3514 is a potent and oral androgen receptor downregulator with K_i of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
S9667	Inobrodib (CCS-1477)	Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
S1190	Bicalutamide (ICI-176334)	Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.	Cell Commun Signal, 2022, 20(1):31 Sci Adv, 2021, 7(27)eabg2564 Cell Rep, 2021, 36(10):109625
S1250	Enzalutamide (MDV3100)	Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.	Sci Adv, 2022, 8(17):eabh3635 Cancer Res, 2022, canres.1807.2021 NPJ Precis Oncol, 2022, 6(1):21
S1908	Flutamide	Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with K_i values of 55 nM, and primarily used to treat prostate cancer.	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cell Chem Biol, 2021, 28(6):788-801.e5 Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2042	Cyproterone Acetate	Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.	Sci Rep, 2021, 11(1):5457 Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332
S2604	Dehydroepiandrosterone (DHEA)	Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.	Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2 J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002 SSRN, 2021, 10.2139/ssrn.3886996
S2803	Galeterone	Galeterone (TOK-001) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.	ChemMedChem, 2022, e202200043 Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w Steroids, 2020, 153:108534
S4054	Spironolactone	Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.	Int J Mol Sci, 2021, 22(4)1638 J Biol Chem, 2021, S0021-9258(21)00252-0 J Environ Sci Health B, 2020, 55(2):91-102
S4593	Chlormadinone acetate	Chlormadinone acetate (Gestafortin) is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.
S4728	3,3'-Diindolylmethane	3,3'-Diindolylmethane(DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.	FASEB J, 2021, 35(5):e21502 Cell Death Dis, 2019, 10(2):38
S4836	Nilutamide	Nilutamide (RU23908) is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.
S5285	RU58841	RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
S5437	4,4'-DDE	4,4'-DDE (DDE, p,p'-DDE, p,p'-dichlorodiphenyldichloroethylene), a breakdown product of DDT, is an organochlorine pesticide and may behave as a potent androgen receptor antagonist.
S6896	Clascoterone	Clascoterone (Winlevi, Cortexolone 17 alpha-propionate, Cortexolone 17α-propionate, CB-03-01) is a topical and peripherally selective antagonist of androgen receptor (AR).
S7559	Darolutamide (ODM-201)	Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i of 11 nM. Phase 3.	Proc Natl Acad Sci U S A, 2020, 202021450 Mol Cancer Ther, 2020, molcanther.0417.2020 Mol Cancer Ther, 2020, 19;molcanther00152020
S7955	EPI-001	EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.	Prostate, 2019, 79(2):206-214
S8885	UT-34	UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer.
S9045	Triptophenolide	Triptophenolide (Hypolide), derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.
S9898^New	Proxalutamide (GT0918)	Proxalutamide (GT0918) is a second-generation androgen receptor antagonist that binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.
S9900^New	JNJ-63576253 (TRC-253)	JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.
S1140	Andarine	Andarine (GTx-007, S-4) is a selective non-steroidal androgen receptor (AR) agonist with K_i of 4 nM, tissue-selective for anabolic organs. Phase 3.	Anal Chem, 2021, 10.1021/acs.analchem.1c01083 Drug Test Anal, 2020, 10.1002/dta.2917 J Am Soc Mass Spectrom, 2020, 31(11):2243-2249
S2832	Epiandrosterone	Epiandrosterone (3β-androsterone, EpiA) is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.
S3715	Boldenone Undecylenate	Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.
S3717	Testosterone Enanthate	Testosterone Enanthate (Testosterone heptanoate, NSC-17591) is an androgen and anabolic steroid used in androgen replacement therapy.	Cancers (Basel), 2021, 13(19)4937 Onco Targets Ther, 2020, 8;13:2987-2995
S3830	Protodioscin	Protodioscin (Furostanol I), a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S3946	Mesterolone	Mesterolone (Androviron, Mesteranum, Proviron) is a synthetic steroid with anabolic and androgenic activities.
S4757	Dihydrotestosterone (DHT)	Dihydrotestosterone (DHT, androstanolone, stanolone, 5α-DHT) is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.	J Med Chem, 2022, 65(3):2507-2521 Life Sci Alliance, 2022, 5(4)e202101116 J Oncol, 2022, 2022:6085948
S4794	Drostanolone Propionate	Drostanolone Propionate (Dromostanolone propionate, NSC-12198, Drostanolone 17β-propionate) is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795	Trenbolone acetate	Trenbolone acetate (RU-1697, Trenbolone 17β), a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S5508	Dehydroepiandrosterone acetate	Dehydroepiandrosterone acetate (DHEA, Androstenolone) is a kind of dehydroepiandrosterone derivatives. DHEA is an endogenous steroid hormone, which is considered to be a natural product/dietary supplement with many proposed benefits to humans.	Br J Cancer, 2020, 10.1038/s41416-020-1007-3 Cancer Lett, 2016, 382(2):195-202
S6352	Androsterone	Androsterone (5alpha-Androsterone) is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.	Mediators Inflamm, 2019, 2019:7162976
S6407	Tulobuterol hydrochloride	Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities.
S0276	GSK-2881078	GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
S0839	ACP-105	ACP-105 is an orally available and potent selective androgen receptor modulator (SARM) with pEC50 of 9.0 and 9.4 for AR wild type and AR mutation T877A, respectively.	Drug Test Anal, 2020, 10.1002/dta.2917
S1174	Ostarine (GTx-024)	Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with K_i of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.	Int J Mol Sci, 2022, 23(8)4404 J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083
S5275	Testolone (RAD140)	Testolone (RAD140) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.	J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083
S6630	Dimethylcurcumin (ASC-J9)	Dimethylcurcumin (ASC-J9, Dimethyl curcumin, GO-Y025) is an androgen receptor (AR) degradation enhancer that suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
S8822	Ligandrol (LGD-4033)	Ligandrol (LGD-4033, VK-5211) is a novel nonsteroidal, oral selective androgen receptor modulator with high affinity (Ki of ∼1 nM) and selectivity.	J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083 Anal Bioanal Chem, 2021, 10.1007/s00216-021-03740-7
S0097	(S,R,S)-AHPC (MDK7526)	(S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC is potential useful for the targeted degradation of the androgen receptor. (S,R,S)-AHPC can be connected to the ligand for protein such as BCR-ABL1 by a linker to form PROTACs such as GMB-475. GMB-475 induces the degradation of BCR-ABL1 with IC50 of 1.11 μM in Ba/F3 cells.
S1123	Abiraterone (CB-7598)	Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.	Cancer Cell, 2021, S1535-6108(21)00659-0 Cancers (Basel), 2021, 13(16)3959 Sci Rep, 2021, 11(1):10765
S1195	TAK-700 (Orteronel)	TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). TAK-700 (Orteronel) is an androgen biosynthesis inhibitor. Phase 3.	Drug Metab Dispos, 2017, 45(6):635-645 Biochem Biophys Res Commun, 2016, 477(4):1005-10
S1304	Megestrol Acetate	Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.	Hum Cell, 2022, 10.1007/s13577-022-00671-y Hum Cell, 2021, 34(6):1911-1918 Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1353	Ketoconazole (R 41400)	Ketoconazole (R 41400) inhibits cyclosporine oxidase and testosterone 6 beta-hydroxylase with IC50 of 0.19 mM and 0.22 mM, respectively. Ketoconazole is an androgen biosynthesis inhibitor.	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4 Nat Commun, 2021, 12(1):652 Pharmacol Res, 2021, 169:105648
S2246	Abiraterone Acetate (CB7630)	Abiraterone Acetate (CB7630) is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM in a cell-free assay. Abiraterone acetate is an oral androgen biosynthesis inhibitor.	Clin Cancer Res, 2021, clincanres.4391.2020 Neoplasia, 2021, 23(12):1261-1274 J Biol Chem, 2021, 297(2):100969
S2840	Apalutamide (ARN-509)	Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.	Prostate, 2022, 82(3):314-322 J Pathol, 2021, 10.1002/path.5652 Nat Commun, 2020, 19;11(1):2508
S6885	Ailanthone	Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.
S6965^New	Bavdegalutamide (ARV-110)	Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR. ARV-110 completely degrades androgen receptor (AR) in all cell lines tested with DC50 of < 1 nM. ARV-110 can be used for the research of prostate cancer.
S7040	AZD3514	AZD3514 is a potent and oral androgen receptor downregulator with K_i of 2.2 μM and has ability of reducing AR protein expression.Phase 1.
S9667	Inobrodib (CCS-1477)	Inobrodib (CCS1477; CBP-IN-1; CBP/p300-IN-4）is a potent and selective inhibitor of p300/CBP bromodomain. CCS1477 works by inhibiting the expression and function of the androgen receptor (AR), as well as inhibiting c-Myc.
S1190	Bicalutamide (ICI-176334)	Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.	Cell Commun Signal, 2022, 20(1):31 Sci Adv, 2021, 7(27)eabg2564 Cell Rep, 2021, 36(10):109625
S1250	Enzalutamide (MDV3100)	Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.	Sci Adv, 2022, 8(17):eabh3635 Cancer Res, 2022, canres.1807.2021 NPJ Precis Oncol, 2022, 6(1):21
S1908	Flutamide	Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with K_i values of 55 nM, and primarily used to treat prostate cancer.	Hum Cell, 2022, 10.1007/s13577-022-00671-y Cell Chem Biol, 2021, 28(6):788-801.e5 Hum Cell, 2021, 10.1007/s13577-021-00639-4
S2042	Cyproterone Acetate	Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.	Sci Rep, 2021, 11(1):5457 Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332
S2604	Dehydroepiandrosterone (DHEA)	Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.	Stem Cell Rev Rep, 2021, 10.1007/s12015-021-10239-2 J Chromatogr B Analyt Technol Biomed Life Sci, 2021, 1186:123002 SSRN, 2021, 10.2139/ssrn.3886996
S2803	Galeterone	Galeterone (TOK-001) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.	ChemMedChem, 2022, e202200043 Cancer Chemother Pharmacol, 2020, 10.1007/s00280-020-04195-w Steroids, 2020, 153:108534
S4054	Spironolactone	Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.	Int J Mol Sci, 2021, 22(4)1638 J Biol Chem, 2021, S0021-9258(21)00252-0 J Environ Sci Health B, 2020, 55(2):91-102
S4593	Chlormadinone acetate	Chlormadinone acetate (Gestafortin) is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.
S4728	3,3'-Diindolylmethane	3,3'-Diindolylmethane(DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.	FASEB J, 2021, 35(5):e21502 Cell Death Dis, 2019, 10(2):38
S4836	Nilutamide	Nilutamide (RU23908) is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.
S5285	RU58841	RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
S5437	4,4'-DDE	4,4'-DDE (DDE, p,p'-DDE, p,p'-dichlorodiphenyldichloroethylene), a breakdown product of DDT, is an organochlorine pesticide and may behave as a potent androgen receptor antagonist.
S6896	Clascoterone	Clascoterone (Winlevi, Cortexolone 17 alpha-propionate, Cortexolone 17α-propionate, CB-03-01) is a topical and peripherally selective antagonist of androgen receptor (AR).
S7559	Darolutamide (ODM-201)	Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K_i of 11 nM. Phase 3.	Proc Natl Acad Sci U S A, 2020, 202021450 Mol Cancer Ther, 2020, molcanther.0417.2020 Mol Cancer Ther, 2020, 19;molcanther00152020
S7955	EPI-001	EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.	Prostate, 2019, 79(2):206-214
S8885	UT-34	UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer.
S9045	Triptophenolide	Triptophenolide (Hypolide), derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.
S9898^New	Proxalutamide (GT0918)	Proxalutamide (GT0918) is a second-generation androgen receptor antagonist that binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.
S9900^New	JNJ-63576253 (TRC-253)	JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.
S1140	Andarine	Andarine (GTx-007, S-4) is a selective non-steroidal androgen receptor (AR) agonist with K_i of 4 nM, tissue-selective for anabolic organs. Phase 3.	Anal Chem, 2021, 10.1021/acs.analchem.1c01083 Drug Test Anal, 2020, 10.1002/dta.2917 J Am Soc Mass Spectrom, 2020, 31(11):2243-2249
S2832	Epiandrosterone	Epiandrosterone (3β-androsterone, EpiA) is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.
S3715	Boldenone Undecylenate	Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.
S3717	Testosterone Enanthate	Testosterone Enanthate (Testosterone heptanoate, NSC-17591) is an androgen and anabolic steroid used in androgen replacement therapy.	Cancers (Basel), 2021, 13(19)4937 Onco Targets Ther, 2020, 8;13:2987-2995
S3830	Protodioscin	Protodioscin (Furostanol I), a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.
S3946	Mesterolone	Mesterolone (Androviron, Mesteranum, Proviron) is a synthetic steroid with anabolic and androgenic activities.
S4757	Dihydrotestosterone (DHT)	Dihydrotestosterone (DHT, androstanolone, stanolone, 5α-DHT) is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.	J Med Chem, 2022, 65(3):2507-2521 Life Sci Alliance, 2022, 5(4)e202101116 J Oncol, 2022, 2022:6085948
S4794	Drostanolone Propionate	Drostanolone Propionate (Dromostanolone propionate, NSC-12198, Drostanolone 17β-propionate) is an anabolic androgenic steroid with strong anti-estrogenic properties.
S4795	Trenbolone acetate	Trenbolone acetate (RU-1697, Trenbolone 17β), a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.
S5508	Dehydroepiandrosterone acetate	Dehydroepiandrosterone acetate (DHEA, Androstenolone) is a kind of dehydroepiandrosterone derivatives. DHEA is an endogenous steroid hormone, which is considered to be a natural product/dietary supplement with many proposed benefits to humans.	Br J Cancer, 2020, 10.1038/s41416-020-1007-3 Cancer Lett, 2016, 382(2):195-202
S6352	Androsterone	Androsterone (5alpha-Androsterone) is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.	Mediators Inflamm, 2019, 2019:7162976
S6407	Tulobuterol hydrochloride	Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities.
S0276	GSK-2881078	GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
S0839	ACP-105	ACP-105 is an orally available and potent selective androgen receptor modulator (SARM) with pEC50 of 9.0 and 9.4 for AR wild type and AR mutation T877A, respectively.	Drug Test Anal, 2020, 10.1002/dta.2917
S1174	Ostarine (GTx-024)	Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with K_i of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.	Int J Mol Sci, 2022, 23(8)4404 J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083
S5275	Testolone (RAD140)	Testolone (RAD140) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.	J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083
S6630	Dimethylcurcumin (ASC-J9)	Dimethylcurcumin (ASC-J9, Dimethyl curcumin, GO-Y025) is an androgen receptor (AR) degradation enhancer that suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
S8822	Ligandrol (LGD-4033)	Ligandrol (LGD-4033, VK-5211) is a novel nonsteroidal, oral selective androgen receptor modulator with high affinity (Ki of ∼1 nM) and selectivity.	J Clin Invest, 2021, 131(10)146777 Anal Chem, 2021, 10.1021/acs.analchem.1c01083 Anal Bioanal Chem, 2021, 10.1007/s00216-021-03740-7
S6965^New	Bavdegalutamide (ARV-110)	Bavdegalutamide (ARV-110) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR. ARV-110 completely degrades androgen receptor (AR) in all cell lines tested with DC50 of < 1 nM. ARV-110 can be used for the research of prostate cancer.
S9898^New	Proxalutamide (GT0918)	Proxalutamide (GT0918) is a second-generation androgen receptor antagonist that binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.
S9900^New	JNJ-63576253 (TRC-253)	JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.