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Assay Detail

CHEMBL681737

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Functional
Inhibition of antagonist activity towards glucocorticoid receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
Zhi L, Ringgenberg JD, Edwards JP, Tegley CM, West SJ, Pio B, Motamedi M, Jones TK, Marschke KB, Mais DE, Schrader WT.
Bioorg Med Chem Lett (2003) 13 : 2075 -2078
PubMed 12781198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.66 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.10
CHEMBL1908373 ONAPRISTONE 2.0 1 7.57
CHEMBL62227 1 6.71
CHEMBL64294 1 6.16
CHEMBL293409 1 5.73
CHEMBL63870 1 5.71
CHEMBL62761 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.8 nM 9.10
CHEMBL1908373 ONAPRISTONE IC50 = 27.0 nM 7.57
CHEMBL62227 IC50 = 194.0 nM 6.71
CHEMBL64294 IC50 = 689.0 nM 6.16
CHEMBL293409 IC50 = 1872.0 nM 5.73
CHEMBL63870 IC50 = 1929.0 nM 5.71
CHEMBL62761 IC50 = 2170.0 nM 5.66