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ChEMBL ligand: CHEMBL491 (2-hydroxyflutamide, .alpha.-hydroxyflutamide, Hydroxy-flutamide, Hydroxyflutamide) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
ChEMBL | Displacement of [3H]testosterone from wild type human androgen receptor | B | 6.37 | pKi | 430 | nM | Ki | Bioorg Med Chem (2008) 16: 6799-6812 [PMID:18571420] |
ChEMBL | Displacement of [3H]DHT from human androgen receptor in MDA453 cells | B | 7.37 | pKi | 43 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1910-1915 [PMID:18291644] |
ChEMBL | Inhibition of [3H]DHT binding to androgen receptor of MDA-453 cells | B | 7.37 | pKi | 43 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 389-393 [PMID:15603960] |
ChEMBL | Binding affinity for androgen receptor in human MDA-453 cells | B | 7.37 | pKi | 43 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 271-276 [PMID:15603938] |
ChEMBL | Binding affinity for human androgen receptor transfected into mammalian COS-1 cells | B | 7.47 | pKi | 34 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 411-414 [PMID:10743937] |
ChEMBL | Binding affinity for human androgen receptor in transiently-transfected COS-1 cells. | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
ChEMBL | Displacement of [3H]testosterone from human recombinant androgen receptor T877A mutant expressed in LNCaP cells | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem (2008) 16: 6799-6812 [PMID:18571420] |
ChEMBL | Binding affinity for mutant T877A Androgen receptor in human LNCaP cells | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 271-276 [PMID:15603938] |
ChEMBL | Inhibition of [3H]-DHT binding to T877A androgen receptor of LNCaP cells | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 389-393 [PMID:15603960] |
ChEMBL | Displacement of [3H]-DHT from human GST fused AR-LBD (627 to 919 amino acids) transfected in Escherichia coli HB 101 after 15 hrs by liquid scintillation counting assay | B | 5.11 | pIC50 | 7690 | nM | IC50 | Eur J Med Chem (2015) 102: 310-319 [PMID:26295173] |
ChEMBL | Displacement of [3H]-DHT from human GST-tagged androgen receptor LBD (627 to 919) expressed in Escherichia coli HB-101 after 15 hrs by liquid scintillation counting analysis | B | 5.15 | pIC50 | 7100 | nM | IC50 | ACS Med Chem Lett (2013) 4: 937-941 [PMID:24900588] |
ChEMBL | Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method | F | 6.46 | pIC50 | 350 | nM | IC50 | Bioorg Med Chem (2008) 16: 6799-6812 [PMID:18571420] |
ChEMBL | Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem (2013) 21: 1643-1651 [PMID:23462715] |
ChEMBL | Antagonistic activity at AR in human 22Rv1 cells assessed as reduction in cell number by CCK8 assay | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2020) 63: 10396-10411 [PMID:32847363] |
ChEMBL | Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation assay | B | 6.65 | pIC50 | 223.87 | nM | IC50 | J Med Chem (2012) 55: 6316-6327 [PMID:22746350] |
ChEMBL | Displacement of [3H]mibolerone from human androgen receptor expressed in CHOK1 cells | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5573-5576 [PMID:17804229] |
ChEMBL | Displacement of [3H]mibolerone from androgen receptor expressed in CHOK1 cells | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2007) 15: 174-185 [PMID:17064916] |
ChEMBL | Antagonist activity at wild type AR expressed in human SC cells assessed as inhibition of 1 nM DHT-induced cell proliferation after 3 days by WST-8 assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Eur J Med Chem (2015) 102: 310-319 [PMID:26295173] |
ChEMBL | Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay | F | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem (2008) 16: 8022-8028 [PMID:18707892] |
ChEMBL | Inhibitory concentration against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells | F | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 411-414 [PMID:10743937] |
ChEMBL | Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by reporter gene assay | F | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem (2007) 15: 174-185 [PMID:17064916] |
ChEMBL | Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay | F | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5573-5576 [PMID:17804229] |
ChEMBL | Inhibition of androgen receptor in human MDA-453 cells | B | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 271-276 [PMID:15603938] |
ChEMBL | Inhibition of human androgen receptor of breast carcinoma MDA-453 cells in reporter gene assay | F | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 389-393 [PMID:15603960] |
ChEMBL | Antagonist activity at human androgen receptor in MDA453 cells by alkaline phosphatase reporter gene assay | F | 7.59 | pIC50 | 26 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1910-1915 [PMID:18291644] |
ChEMBL | Antagonist activity at androgen receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay | B | 7.6 | pIC50 | 25 | nM | IC50 | J Nat Prod (2009) 72: 1944-1948 [PMID:19863083] |
ChEMBL | Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. | F | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
GtoPdb | - | - | 6.6 | pEC50 | 254 | nM | EC50 | Biochem Pharmacol (1998) 55: 1427-33 [PMID:10076535] |
Androgen receptor/Androgen Receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091] | ||||||||
ChEMBL | Antagonist activity at androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell growth after 3 days | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem (2013) 21: 1643-1651 [PMID:23462715] |
ChEMBL | Antagonist activity at androgen receptor in mouse SC3 cells assessed as inhibition of DHT-induced cell growth after 3 days by CCK-8/WST-8 assay | B | 6.43 | pIC50 | 370 | nM | IC50 | ACS Med Chem Lett (2013) 4: 937-941 [PMID:24900588] |
ChEMBL | In vitro inhibition of DHT (dihydrotestosterone) on proliferation of androgen-sensitive cancer Schionogi (SC-3) cells | F | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (1995) 38: 1158-1173 [PMID:7707319] |
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
ChEMBL | In vivo binding affinity for rat ventral prostate androgen receptor by displacement of [3H]R-1881 | B | 5.68 | pKi | 2100 | nM | Ki | J Med Chem (1992) 35: 1663-1670 [PMID:1588549] |
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
ChEMBL | Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. | F | 5.7 | pIC50 | 2013 | nM | IC50 | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]