S1250 |
Enzalutamide
|
エンザルタミド (Enzalutamide (MDV3100)) は、アンドロゲン受容体 (androgen receptor, AR) アンタゴニストで LNCaP 細胞における IC50 は36 nM です。エンザルミドはオートファジー (autophagy) を増加させることが示されています。 |
-
Cancers (Basel), 2024, 16(2)296
-
bioRxiv, 2024, 10.1101/2024.01.16.575611
-
bioRxiv, 2024, 10.1101/2023.12.01.569685
|
|
S1190 |
Bicalutamide
|
Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy. |
-
Cancers (Basel), 2024, 16(2)296
-
Biomedicines, 2024, 12(1)181
-
J Exp Clin Cancer Res, 2023, 42(1):204
|
|
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. |
-
Cancer Res, 2023, 83(2):219-238
-
J Immunother Cancer, 2023, 11(5)e006581
-
Pharmacol Res, 2023, 189:106692
|
|
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. |
-
Oncogene, 2024, 43(4):235-247
-
Nat Commun, 2023, 14(1):5253
-
Nat Commun, 2023, 14(1):5253
|
|
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
-
Cell Death Dis, 2023, 14(1):64
-
Cell Death Dis, 2023, 14(8):488
|
|
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. |
-
Int J Mol Sci, 2022, 23-169390
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
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.
|
-
Nat Commun, 2023, 14(1):5253
-
Nat Commun, 2023, 14(1):5253
-
Cancer Res, 2023, 83(3):456-470
|
|
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. |
-
J Cell Mol Med, 2023, 27(8):1069-1082
-
ESC Heart Fail, 2022, 10.1002/ehf2.14186
-
Int J Mol Sci, 2021, 22(4)1638
|
|
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 Mol Sci, 2023, 24(4)3823
-
Cell Death Dis, 2022, 13(7):626
-
Mar Drugs, 2022, 20(6)378
|
|
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. |
-
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. |
|
|
E1502New |
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 enzalutamide-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. |
|
|
E0608New |
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. |
|
|
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. |
|
|
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. |
|
|
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. |
- Cancer Res, 2023, 83(2):219-238
- J Immunother Cancer, 2023, 11(5)e006581
- Pharmacol Res, 2023, 189:106692
|
|
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. |
- Oncogene, 2024, 43(4):235-247
- Nat Commun, 2023, 14(1):5253
- Nat Commun, 2023, 14(1):5253
|
|
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
- Cell Death Dis, 2023, 14(1):64
- Cell Death Dis, 2023, 14(8):488
|
|
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. |
- 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. |
|
|
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. |
|
|
S1250 |
Enzalutamide
|
エンザルタミド (Enzalutamide (MDV3100)) は、アンドロゲン受容体 (androgen receptor, AR) アンタゴニストで LNCaP 細胞における IC50 は36 nM です。エンザルミドはオートファジー (autophagy) を増加させることが示されています。 |
- Cancers (Basel), 2024, 16(2)296
- bioRxiv, 2024, 10.1101/2024.01.16.575611
- bioRxiv, 2024, 10.1101/2023.12.01.569685
|
|
S1190 |
Bicalutamide
|
Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy. |
- Cancers (Basel), 2024, 16(2)296
- Biomedicines, 2024, 12(1)181
- J Exp Clin Cancer Res, 2023, 42(1):204
|
|
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. |
- Int J Mol Sci, 2022, 23-169390
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
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.
|
- Nat Commun, 2023, 14(1):5253
- Nat Commun, 2023, 14(1):5253
- Cancer Res, 2023, 83(3):456-470
|
|
S4054 |
Spironolactone
|
Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM. |
- J Cell Mol Med, 2023, 27(8):1069-1082
- ESC Heart Fail, 2022, 10.1002/ehf2.14186
- Int J Mol Sci, 2021, 22(4)1638
|
|
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 Mol Sci, 2023, 24(4)3823
- Cell Death Dis, 2022, 13(7):626
- Mar Drugs, 2022, 20(6)378
|
|
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
|
|
E1502New |
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 enzalutamide-resistant prostate cancer. |
|
|
S5285 |
RU58841
|
RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen. |
|
|
E0608New |
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. |
|
|
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. |
|
|