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Assay Detail

CHEMBL729167

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

Binding
Inhibitory activity against human Mineralocorticoid receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.
Zhi L, Tegley CM, Pio B, Edwards JP, Motamedi M, Jones TK, Marschke KB, Mais DE, Risek B, Schrader WT.
J Med Chem (2003) 46 : 4104 -4112
PubMed 12954062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.36 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103 PROGESTERONE 4.0 1 7.85
CHEMBL415524 1 6.48
CHEMBL130141 1 6.44
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 5.92
CHEMBL337856 1 5.73
CHEMBL134277 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103 PROGESTERONE IC50 = 14.0 nM 7.85
CHEMBL415524 IC50 = 334.0 nM 6.48
CHEMBL130141 IC50 = 363.0 nM 6.44
CHEMBL717 MEDROXYPROGESTERONE ACETATE IC50 = 1197.0 nM 5.92
CHEMBL337856 IC50 = 1850.0 nM 5.73
CHEMBL134277 IC50 = 1900.0 nM 5.72