eplerenone [Ligand Id: 2876] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1095097 (Eplerenone, SC-66110, Inspra, SC-6611O)
  • 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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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
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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 Antagonist activity at androgen receptor (unknown origin) by NH Pro assay B 4.7 pIC50 >20000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL Antagonist activity at androgen receptor F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Displacement of [3H]testosterone from AR B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL Displacement of [3H]testosterone from androgen receptor (unknown origin) expressed in 293 cells after 16 hrs by scintillation counting B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL Agonist activity at androgen receptor (unknown origin) by NH Pro assay B 4.7 pEC50 >20000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL Antagonist activity at estrogen receptor alpha (unknown origin) by NH Pro assay B 4.7 pIC50 >20000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL Antagonist activity at estrogen receptor F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Agonist activity at estrogen receptor alpha (unknown origin) by NH Pro assay B 4.7 pEC50 >20000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL Antagonist activity at estrogen receptor beta (unknown origin) by NH Pro assay B 4.7 pIC50 >20000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL Agonist activity at estrogen receptor beta (unknown origin) by NH Pro assay B 4.7 pEC50 >20000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL Antagonist activity at glucocorticoid receptor (unknown origin) by NH Pro assay B 4.74 pIC50 18000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL Displacement of [3H]dexomethasone from GR B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL Antagonist activity at glucocorticoid receptor F 5.05 pIC50 >8940 nM IC50 J. Med. Chem. (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Agonist activity at glucocorticoid receptor (unknown origin) by NH Pro assay B 4.7 pEC50 >20000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
GtoPdb - - 6.91 pKi 124 nM Ki J. Med. Chem. (2007) 50: 6443-5 [PMID:18038968]
ChEMBL Displacement of [3H]aldosterone from human mineralocorticoid receptor expressed in 293 cells after 16 hrs by scintillation counting B 5.59 pIC50 2600 nM IC50 Bioorg. Med. Chem. (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting B 5.59 pIC50 2600 nM IC50 J. Med. Chem. (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay B 5.89 pIC50 1300 nM IC50 Bioorg. Med. Chem. (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay F 5.89 pIC50 1300 nM IC50 J. Med. Chem. (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL Antagonist activity at mineralocorticoid receptor (unknown origin) by PathHunter assay B 6.61 pIC50 244 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1681-1684 [PMID:24630411]
ChEMBL Antagonist activity at human mineralocorticoid receptor assessed as inhibition of binding to coactivator peptide by NH Pro assay B 6.62 pIC50 240 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL Antagonist activity at Gal4-fused mineralocorticoid receptor expressed in human HuH7 cells assessed as inhibition of aldosterone-induced receptor activation by luciferase reporter gene assay F 6.87 pIC50 135 nM IC50 J. Med. Chem. (2010) 53: 4300-4304 [PMID:20408553]
ChEMBL Antagonist activity at mineralocorticoid receptor (unknown origin) by Gal4-based cellular assay B 6.91 pIC50 122 nM IC50 J. Med. Chem. (2014) 57: 4273-4288 [PMID:24738581]
ChEMBL Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay F 6.91 pIC50 122 nM IC50 J. Med. Chem. (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Antagonist activity at mineralocorticoid receptor LBD expressed in human HUH7 cells coexpressing GAL4 by luciferase reporter gene assay F 6.91 pIC50 122 nM IC50 J. Med. Chem. (2010) 53: 5970-5978 [PMID:20672820]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Antagonist activity at progesterone receptor beta (unknown origin) by NH Pro assay B 4.7 pIC50 >20000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]
ChEMBL Antagonist activity at progesterone receptor F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 5979-6002 [PMID:20672822]
ChEMBL Displacement of [3H]progesterone from PR B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2011) 54: 8616-8631 [PMID:22074142]
ChEMBL Displacement of [[3H]-Progesterone from progesterone receptor (unknown origin) expressed in 293 cells after 16 hrs by scintillation counting B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL Displacement of [3H]-Dexamethasone from glucocorticoid receptor (unknown origin) expressed in 293 cells after 16 hrs by scintillation counting B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. (2014) 22: 5428-5445 [PMID:25187277]
ChEMBL Agonist activity at progesterone receptor beta (unknown origin) by NH Pro assay B 4.7 pEC50 >20000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 4388-4392 [PMID:23777778]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]