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Assay Detail

CHEMBL729160

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

Functional
Antagonistic activity was determined in Human mineralocorticoid receptor(hMR) of CV-1 cells in cotransfection assay.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mineralocorticoid receptor (CHEMBL1994)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.
Zhi L, Tegley CM, Kallel EA, Marschke KB, Mais DE, Gottardis MM, Jones TK.
J Med Chem (1998) 41 : 291 -302
PubMed 9464360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.09 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103 PROGESTERONE 4.0 1 7.85
CHEMBL101914 1 6.45
CHEMBL320690 1 6.13
CHEMBL103232 1 6.01
CHEMBL103092 1 6.00
CHEMBL317921 1 5.97
CHEMBL430855 1 5.97
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 5.92
CHEMBL102754 1 5.87
CHEMBL286595 1 5.82
CHEMBL102403 1 5.80
CHEMBL102720 1 5.69
CHEMBL318513 1 5.65
CHEMBL101907 1 -
CHEMBL102541 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103 PROGESTERONE IC50 = 14.0 nM 7.85
CHEMBL101914 IC50 = 354.0 nM 6.45
CHEMBL320690 IC50 = 748.0 nM 6.13
CHEMBL103232 IC50 = 977.0 nM 6.01
CHEMBL103092 IC50 = 1000.0 nM 6.00
CHEMBL317921 IC50 = 1062.0 nM 5.97
CHEMBL430855 IC50 = 1068.0 nM 5.97
CHEMBL717 MEDROXYPROGESTERONE ACETATE IC50 = 1197.0 nM 5.92
CHEMBL102754 IC50 = 1358.0 nM 5.87
CHEMBL286595 IC50 = 1525.0 nM 5.82
CHEMBL102403 IC50 = 1592.0 nM 5.80
CHEMBL102720 IC50 = 2035.0 nM 5.69
CHEMBL318513 IC50 = 2219.0 nM 5.65
CHEMBL101907 IC50 > 10000.0 nM -
CHEMBL102541 IC50 > 10000.0 nM -