PF-03882845 [Ligand Id: 9061] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1215331 (PF-3882845)
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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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]
GtoPdb - - 5.05 pIC50 8910 nM IC50 J Med Chem (2014) 57: 4273-88 [PMID:24738581]
ChEMBL Antagonist activity at androgen receptor F 5.05 pIC50 >8910 nM IC50 J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Antagonist activity at androgen receptor (unknown origin) by Gal4-based cellular assay B 5.05 pIC50 >8910 nM IC50 J Med Chem (2014) 57: 4273-4288 [PMID:24738581]
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL Antagonist activity at estrogen receptor F 5 pIC50 >10000 nM IC50 J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL Antagonist activity at glucocorticoid receptor F 5 pIC50 >10000 nM IC50 J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Antagonist activity at glucocorticoid receptor (unknown origin) by Gal4-based cellular assay B 5 pIC50 >10000 nM IC50 J Med Chem (2014) 57: 4273-4288 [PMID:24738581]
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
ChEMBL Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay F 7.68 pIC50 21 nM IC50 J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Antagonist activity at mineralocorticoid receptor (unknown origin) by Gal4-based cellular assay B 8.04 pIC50 9.2 nM IC50 J Med Chem (2014) 57: 4273-4288 [PMID:24738581]
GtoPdb - - 8.04 pIC50 9.2 nM IC50 J Med Chem (2014) 57: 4273-88 [PMID:24738581]
ChEMBL Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay F 8.05 pIC50 9 nM IC50 J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Binding affinity to mineralocorticoid receptor (unknown origin) B 8.05 pIC50 9 nM IC50 J Med Chem (2014) 57: 4273-4288 [PMID:24738581]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
GtoPdb - - 6.38 pIC50 416 nM IC50 J Med Chem (2014) 57: 4273-88 [PMID:24738581]
ChEMBL Antagonist activity at progesterone receptor F 6.38 pIC50 416 nM IC50 J Med Chem (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Antagonist activity at progesterone receptor (unknown origin) by Gal4-based cellular assay B 6.38 pIC50 416 nM IC50 J Med Chem (2014) 57: 4273-4288 [PMID:24738581]

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]