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Assay Detail

CHEMBL4008014

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]-Aldosterone from MR in rat renal soluble fraction measured after 18 hrs in presence of glucocorticoid receptor antagonist RU-486 by liquid scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mineralocorticoid receptor (CHEMBL3507)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects.
Martín-Martínez M, Pérez-Gordillo FL, Álvarez de la Rosa D, Rodríguez Y, Gerona-Navarro G, González-Muñiz R, Zhou MM.
J Med Chem (2017) 60 : 2629 -2650
PubMed 28051871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.28 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4087750 1 7.66
CHEMBL4085281 1 7.51
CHEMBL4095450 1 7.22
CHEMBL4066419 1 7.21
CHEMBL4075017 1 7.08
CHEMBL4079872 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4087750 IC50 = 22.0 nM 7.66
CHEMBL4085281 IC50 = 31.0 nM 7.51
CHEMBL4095450 IC50 = 60.0 nM 7.22
CHEMBL4066419 IC50 = 61.0 nM 7.21
CHEMBL4075017 IC50 = 84.0 nM 7.08
CHEMBL4079872 IC50 = 100.0 nM 7.00