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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]