S1250 |
Enzalutamide
|
Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy. |
-
Cell Rep Med, 2024, 5(2):101388
-
Cancer Lett, 2024, 597:217068
-
Cancer Lett, 2024, 604:217219
|
|
S1190 |
Bicalutamide
|
Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy. |
-
iScience, 2024, 27(3):109246
-
Cancers (Basel), 2024, 16(7)1303
-
Cancers (Basel), 2024, 16(2)296
|
|
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
-
Cancer Res, 2023, 83(2):219-238
-
J Immunother Cancer, 2023, 11(5)e006581
|
|
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. |
-
Cell Death Dis, 2024, 15(8):617
-
Oncogene, 2024, 43(4):235-247
-
Mol Oncol, 2024, 10.1002/1878-0261.13634
|
|
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. |
-
J Med Virol, 2023, 95(6):e28856
-
J Med Virol, 2023, 95(6):e28856
-
Cell Death Dis, 2023, 14(1):64
|
|
S1908 |
Flutamide
|
Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer. |
-
Zool Res, 2024, 45(2):355-366
-
Dis Model Mech, 2024, 17(10)dmm050900
-
Int J Mol Sci, 2022, 23-169390
|
|
S7559 |
Darolutamide (ODM-201)
|
Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
|
-
Int J Biol Sci, 2024, 20(12):4635-4653
-
Nat Commun, 2023, 14(1):5253
-
Nat Commun, 2023, 14(1):5253
|
|
S1304 |
Megestrol Acetate
|
Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite. |
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
-
Hum Cell, 2021, 34(6):1911-1918
|
|
S4054 |
Spironolactone
|
Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM. |
-
Biomed Pharmacother, 2024, 180:117523
-
iScience, 2024, 27(2):108839
-
Toxics, 2024, 12(4)247
|
|
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. |
-
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. |
-
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 Ki 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. |
|
|
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. |
|
|
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. |
|
|
E1964New |
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, AR1-651) 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. |
-
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
- Cancer Res, 2023, 83(2):219-238
- J Immunother Cancer, 2023, 11(5)e006581
|
|
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. |
- Cell Death Dis, 2024, 15(8):617
- Oncogene, 2024, 43(4):235-247
- Mol Oncol, 2024, 10.1002/1878-0261.13634
|
|
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. |
- J Med Virol, 2023, 95(6):e28856
- J Med Virol, 2023, 95(6):e28856
- Cell Death Dis, 2023, 14(1):64
|
|
S1304 |
Megestrol Acetate
|
Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite. |
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
- Hum Cell, 2021, 34(6):1911-1918
|
|
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. |
- 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 Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1. |
|
|
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, AR1-651) 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. |
- 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. |
- Cell Rep Med, 2024, 5(2):101388
- Cancer Lett, 2024, 597:217068
- Cancer Lett, 2024, 604:217219
|
|
S1190 |
Bicalutamide
|
Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy. |
- iScience, 2024, 27(3):109246
- Cancers (Basel), 2024, 16(7)1303
- Cancers (Basel), 2024, 16(2)296
|
|
S1908 |
Flutamide
|
Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer. |
- Zool Res, 2024, 45(2):355-366
- Dis Model Mech, 2024, 17(10)dmm050900
- Int J Mol Sci, 2022, 23-169390
|
|
S7559 |
Darolutamide (ODM-201)
|
Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
|
- Int J Biol Sci, 2024, 20(12):4635-4653
- Nat Commun, 2023, 14(1):5253
- Nat Commun, 2023, 14(1):5253
|
|
S4054 |
Spironolactone
|
Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM. |
- Biomed Pharmacother, 2024, 180:117523
- iScience, 2024, 27(2):108839
- Toxics, 2024, 12(4)247
|
|
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. |
- 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. |
|
|
E1964New |
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. |
|
|