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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
