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Assay Detail

CHEMBL4008041

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

Binding
Antagonist activity at human MR overexpressed in HEK293 cells assessed as inhibition of aldosterone-induced response measured after overnight incubation by luciferase reporter gene assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

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 1 7.68 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4099276 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4099276 IC50 = 21.0 nM 7.68