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Assay Detail

CHEMBL4008049

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

Binding
Displacement of [3H]-cortisol from MR overexpressed in human 293 cells measured after 2 hrs by Microbeta scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
Ki 2 7.99 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3775798 1 8.05
CHEMBL3775714 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3775798 Ki = 9.0 nM 8.05
CHEMBL3775714 Ki = 12.0 nM 7.92