esaxerenone [Ligand Id: 9894] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2181932
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
ChEMBL Antagonist activity at Gal4-fused human MR LBD (671 to 984 residues) expressed in African Green Monkey CV-1 cells assessed as inhibition of aldosterone-induced transactivation activity after 20 hrs by luciferase reporter gene assay B 6 pIC50 >1000 nM IC50 J Med Chem (2017) 60: 2629-2650 [PMID:28051871]
ChEMBL Antagonist activity at Gal4-fused human MR LBD (671 to 984 residues) expressed in African Green Monkey CV-1 cells assessed as inhibition of aldosterone-induced transactivation activity after 20 hrs by luciferase reporter gene assay B 8.03 pIC50 9.4 nM IC50 J Med Chem (2017) 60: 2629-2650 [PMID:28051871]
ChEMBL Antagonist activity at mineralocorticoid receptor F 8.62 pIC50 2.4 nM IC50 J Med Chem (2012) 55: 7957-7966 [PMID:22866979]
GtoPdb - - 8.62 pIC50 2.4 nM IC50 J Med Chem (2012) 55: 7957-66 [PMID:22866979];
Br J Clin Pharmacol (2018) 84: 1821-1829 [PMID:29688582]

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]