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Assay Detail

CHEMBL935183

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

Binding
Antagonist activity at human MR ligand binding domain expressed in african green monkey COS7 cells in presence of aldosterone by Gal4 hybrid assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).
Fensome A, Adams WR, Adams AL, Berrodin TJ, Cohen J, Huselton C, Illenberger A, Kern JC, Hudak VA, Marella MA, Melenski EG, McComas CC, Mugford CA, Slayden OD, Yudt M, Zhang Z, Zhang P, Zhu Y, Winneker RC, Wrobel JE.
J Med Chem (2008) 51 : 1861 -1873
PubMed 18318463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.62 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267431 ASOPRISNIL 3.0 1 5.80
CHEMBL407848 1 5.43
CHEMBL1276308 MIFEPRISTONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267431 ASOPRISNIL IC50 = 1600.0 nM 5.80
CHEMBL407848 IC50 = 3700.0 nM 5.43
CHEMBL1276308 MIFEPRISTONE IC50 - -