hydroxyflutamide [Ligand Id: 2862] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL491 (2-hydroxyflutamide, .alpha.-hydroxyflutamide, Hydroxy-flutamide, Hydroxyflutamide)
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Mouse [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]