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Androgen Receptor

Androgen Receptor Products

All (41)
Androgen Receptor Inhibitors (16)
Androgen Receptor Antagonists (22)
Androgen Receptor Modulators (3)
New Androgen Receptor Products

Catalog No.	Product Name	Information	Product Use Citations
S1250	Enzalutamide	Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.	Theranostics, 2025, 15(12):5572-5591 Clin Cancer Res, 2025, 10.1158/1078-0432.CCR-24-1812 Cancer Res, 2025, 85(2):342-359
S1190	Bicalutamide	Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.	J Control Release, 2025, 380:417-432 iScience, 2024, 27(3):109246 Cancers (Basel), 2024, 16(7)1303
S1123	Abiraterone	Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.	Cancer Res, 2023, 83(8):1361-1380 Cancer Cell, 2021, S1535-6108(21)00659-0 Cancers (Basel), 2021, 13(16)3959
S2246	Abiraterone Acetate	Abiraterone Acetate 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.	Cells, 2024, 13(19)1622 iScience, 2024, 27(10):110862 Cancer Res, 2023, 83(2):219-238
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.	J Control Release, 2025, 380:417-432 Nat Commun, 2024, 15(1):9755 Cell Death Dis, 2024, 15(8):617
S1353	Ketoconazole	Ketoconazole 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.	Mol Oncol, 2025, 10.1002/1878-0261.13799 Discov Oncol, 2024, 15(1):709 J Med Virol, 2023, 95(6):e28856
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.	iScience, 2024, 27(10):110862 Zool Res, 2024, 45(2):355-366 Dis Model Mech, 2024, 17(10)dmm050900
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.	Clin Cancer Res, 2025, 10.1158/1078-0432.CCR-24-1812 Nat Commun, 2024, 15(1):9755 Int J Biol Sci, 2024, 20(12):4635-4653
S1304	Megestrol Acetate	Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.	iScience, 2024, 27(10):110862 J Pers Med, 2022, 12(2)258 Hum Cell, 2022, 10.1007/s13577-022-00671-y
S4054	Spironolactone	Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.	Cancer Cell, 2025, 43(4):776-796.e14 Biomed Pharmacother, 2024, 180:117523 iScience, 2024, 27(2):108839
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
S7955	EPI-001	EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.	Int J Biol Macromol, 2024, 278(Pt 3):134844 Nat Struct Mol Biol, 2023, 30(12):1958-1969 Int J Mol Sci, 2023, 24(4)3823
S1195	Orteronel	Orteronel(TAK-700) 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.	Toxicol Appl Pharmacol, 2023, 475:116638 Drug Metab Dispos, 2017, 45(6):635-645 Biochem Biophys Res Commun, 2016, 477(4):1005-10
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.	iScience, 2024, 27(10):110862 Sci Rep, 2021, 11(1):5457 Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332
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
S6965	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.	BMC Biol, 2025, 23(1):51 Cell Mol Life Sci, 2024, 81(1):324 Nucleic Acids Res, 2023, gkad642
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
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.
E1502	Deutenzalutamide	Deutenzalutamide (HC-1119, MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. It can be used in a treatment of advanced prostate cancer.
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.
S0276	GSK-2881078	GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
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.
E8277^New	GDC-2992	GDC-2992 (RO7656594, Compound 28A) is an orally active degrader of androgen receptor (AR) with a DC50 of 2.7 nM. It binds to AR and cereblon (CRBN), inducing AR ubiquitination and degradation. GDC-2992 also inhibits cell proliferation in VCaP cells and exhibits potential to reduce treatment resistance and disease relapse in prostate cancer.
S9900	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.
E8283^New	ID11916	ID11916 is an orally available antagonist of Androgen receptor (AR) that blocks androgen binding, AR nuclear translocation, and transcriptional activity. It also inhibits PDE5 and exhibits anti-proliferative activity. ID11916 inhibits tumor growth in the MDA-MB-453 xenograft model.
E8305^New	ATC-324	ATC-324 is a potent AUTOphagy-TArgeting Chimera (AUTOTAC) degrader of androgen receptor (AR) with a DC50 of 2.05 µM. It induces autophagy–lysosomal degradation of AR, reduces nuclear AR and AR-V7 activity, and causes cytotoxicity in AR-positive prostate cancer cells, making it useful for prostate cancer research.
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 -resistant prostate cancer.
S5285	RU58841	RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
E0377	CLP-3094	CLP-3094, a potent inhibitor targeting the binding function 3 (BF3) site of androgen receptor (AR), inhibits AR transcriptional activity with IC50 of 4 μM, also is a selective, potent GPR142 antagonist.
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.
E1964^New	BMS-986365	BMS-986365 (CC-94676) is a potent and selective, heterobifunctional ligand-directed degrader (LDD) and antagonist of androgen receptor (AR), that effectively targets both wildtype and mutant forms of the androgen receptor (AR) in the cytoplasm and nucleus. It rapidly degrades AR, suppresses AR signaling, and shows promising clinical activity in inhibiting tumor growth in patients with metastatic castration-resistant prostate cancer (mCRPC).
E0608	Pyrilutamide(KX-826)	Pyrilutamide (KX-826) is an antagonist of androgen receptor (AR) and a potential first-in-class topical drug for the treatment of androgenetic alopecia (AGA) and acne vulgaris.
S3542	N-desMethyl EnzalutaMide	N-desMethyl EnzalutaMide (N-desmethyl MDV 3100) is the active metabolite of Enzalutamide, which is an oral androgen receptor inhibitor for treatment of castration-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.
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.	Theranostics, 2024, 14(4):1371-1389
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.	Nat Commun, 2025, 16(1):4133 bioRxiv, 2024, 2024.03.29.587346 PLoS Pathog, 2023, 19(8):e1011598
E2850	ORM-15341	ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 value of 38 nM and the inhibition constant (Ki) value of 8 nM.
S9898	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.	CNS Neurosci Ther, 2024, 30(6):e14822
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).
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.
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.
S1123	Abiraterone	Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM in a cell-free assay. Abiraterone (CB-7598) is an androgen biosynthesis inhibitor.	Cancer Res, 2023, 83(8):1361-1380 Cancer Cell, 2021, S1535-6108(21)00659-0 Cancers (Basel), 2021, 13(16)3959
S2246	Abiraterone Acetate	Abiraterone Acetate 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.	Cells, 2024, 13(19)1622 iScience, 2024, 27(10):110862 Cancer Res, 2023, 83(2):219-238
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.	J Control Release, 2025, 380:417-432 Nat Commun, 2024, 15(1):9755 Cell Death Dis, 2024, 15(8):617
S1353	Ketoconazole	Ketoconazole 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.	Mol Oncol, 2025, 10.1002/1878-0261.13799 Discov Oncol, 2024, 15(1):709 J Med Virol, 2023, 95(6):e28856
S1304	Megestrol Acetate	Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.	iScience, 2024, 27(10):110862 J Pers Med, 2022, 12(2)258 Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1195	Orteronel	Orteronel(TAK-700) 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.	Toxicol Appl Pharmacol, 2023, 475:116638 Drug Metab Dispos, 2017, 45(6):635-645 Biochem Biophys Res Commun, 2016, 477(4):1005-10
S6965	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.	BMC Biol, 2025, 23(1):51 Cell Mol Life Sci, 2024, 81(1):324 Nucleic Acids Res, 2023, gkad642
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.
E8277^New	GDC-2992	GDC-2992 (RO7656594, Compound 28A) is an orally active degrader of androgen receptor (AR) with a DC50 of 2.7 nM. It binds to AR and cereblon (CRBN), inducing AR ubiquitination and degradation. GDC-2992 also inhibits cell proliferation in VCaP cells and exhibits potential to reduce treatment resistance and disease relapse in prostate cancer.
E8283^New	ID11916	ID11916 is an orally available antagonist of Androgen receptor (AR) that blocks androgen binding, AR nuclear translocation, and transcriptional activity. It also inhibits PDE5 and exhibits anti-proliferative activity. ID11916 inhibits tumor growth in the MDA-MB-453 xenograft model.
E8305^New	ATC-324	ATC-324 is a potent AUTOphagy-TArgeting Chimera (AUTOTAC) degrader of androgen receptor (AR) with a DC50 of 2.05 µM. It induces autophagy–lysosomal degradation of AR, reduces nuclear AR and AR-V7 activity, and causes cytotoxicity in AR-positive prostate cancer cells, making it useful for prostate cancer research.
E0377	CLP-3094	CLP-3094, a potent inhibitor targeting the binding function 3 (BF3) site of androgen receptor (AR), inhibits AR transcriptional activity with IC50 of 4 μM, also is a selective, potent GPR142 antagonist.
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.
S3542	N-desMethyl EnzalutaMide	N-desMethyl EnzalutaMide (N-desmethyl MDV 3100) is the active metabolite of Enzalutamide, which is an oral androgen receptor inhibitor for treatment of castration-resistant prostate cancer.
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.	Theranostics, 2024, 14(4):1371-1389
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.	Nat Commun, 2025, 16(1):4133 bioRxiv, 2024, 2024.03.29.587346 PLoS Pathog, 2023, 19(8):e1011598
S1250	Enzalutamide	Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.	Theranostics, 2025, 15(12):5572-5591 Clin Cancer Res, 2025, 10.1158/1078-0432.CCR-24-1812 Cancer Res, 2025, 85(2):342-359
S1190	Bicalutamide	Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.	J Control Release, 2025, 380:417-432 iScience, 2024, 27(3):109246 Cancers (Basel), 2024, 16(7)1303
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.	iScience, 2024, 27(10):110862 Zool Res, 2024, 45(2):355-366 Dis Model Mech, 2024, 17(10)dmm050900
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.	Clin Cancer Res, 2025, 10.1158/1078-0432.CCR-24-1812 Nat Commun, 2024, 15(1):9755 Int J Biol Sci, 2024, 20(12):4635-4653
S4054	Spironolactone	Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.	Cancer Cell, 2025, 43(4):776-796.e14 Biomed Pharmacother, 2024, 180:117523 iScience, 2024, 27(2):108839
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
S7955	EPI-001	EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.	Int J Biol Macromol, 2024, 278(Pt 3):134844 Nat Struct Mol Biol, 2023, 30(12):1958-1969 Int J Mol Sci, 2023, 24(4)3823
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.	iScience, 2024, 27(10):110862 Sci Rep, 2021, 11(1):5457 Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2319-2332
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
E1502	Deutenzalutamide	Deutenzalutamide (HC-1119, MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. It can be used in a treatment of advanced prostate cancer.
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.
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.
S9900	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.
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 -resistant prostate cancer.
S5285	RU58841	RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
E1964^New	BMS-986365	BMS-986365 (CC-94676) is a potent and selective, heterobifunctional ligand-directed degrader (LDD) and antagonist of androgen receptor (AR), that effectively targets both wildtype and mutant forms of the androgen receptor (AR) in the cytoplasm and nucleus. It rapidly degrades AR, suppresses AR signaling, and shows promising clinical activity in inhibiting tumor growth in patients with metastatic castration-resistant prostate cancer (mCRPC).
E0608	Pyrilutamide(KX-826)	Pyrilutamide (KX-826) is an antagonist of androgen receptor (AR) and a potential first-in-class topical drug for the treatment of androgenetic alopecia (AGA) and acne vulgaris.
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.
E2850	ORM-15341	ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 value of 38 nM and the inhibition constant (Ki) value of 8 nM.
S9898	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.	CNS Neurosci Ther, 2024, 30(6):e14822
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).
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.
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
S0276	GSK-2881078	GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
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.
E8277^New	GDC-2992	GDC-2992 (RO7656594, Compound 28A) is an orally active degrader of androgen receptor (AR) with a DC50 of 2.7 nM. It binds to AR and cereblon (CRBN), inducing AR ubiquitination and degradation. GDC-2992 also inhibits cell proliferation in VCaP cells and exhibits potential to reduce treatment resistance and disease relapse in prostate cancer.
E8283^New	ID11916	ID11916 is an orally available antagonist of Androgen receptor (AR) that blocks androgen binding, AR nuclear translocation, and transcriptional activity. It also inhibits PDE5 and exhibits anti-proliferative activity. ID11916 inhibits tumor growth in the MDA-MB-453 xenograft model.
E8305^New	ATC-324	ATC-324 is a potent AUTOphagy-TArgeting Chimera (AUTOTAC) degrader of androgen receptor (AR) with a DC50 of 2.05 µM. It induces autophagy–lysosomal degradation of AR, reduces nuclear AR and AR-V7 activity, and causes cytotoxicity in AR-positive prostate cancer cells, making it useful for prostate cancer research.
E1964^New	BMS-986365	BMS-986365 (CC-94676) is a potent and selective, heterobifunctional ligand-directed degrader (LDD) and antagonist of androgen receptor (AR), that effectively targets both wildtype and mutant forms of the androgen receptor (AR) in the cytoplasm and nucleus. It rapidly degrades AR, suppresses AR signaling, and shows promising clinical activity in inhibiting tumor growth in patients with metastatic castration-resistant prostate cancer (mCRPC).

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Androgen ReceptorSignaling Pathway