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Assay Detail

CHEMBL768144

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

Functional
Antagonistic activity was determined in Human progesterone receptor(hPR) of CV-1 cells in cotransfection assay.
24
Total Activities
24
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

Progesterone receptor (CHEMBL208)
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 24 6.39 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL102179 1 7.27
CHEMBL101852 1 7.15
CHEMBL103468 1 6.98
CHEMBL320411 1 6.88
CHEMBL321584 1 6.82
CHEMBL103237 1 6.82
CHEMBL102403 1 6.60
CHEMBL101914 1 6.54
CHEMBL323324 1 6.47
CHEMBL286595 1 6.22
CHEMBL317921 1 6.14
CHEMBL320690 1 6.03
CHEMBL101907 1 5.96
CHEMBL430855 1 5.95
CHEMBL102602 1 5.92
CHEMBL103232 1 5.50
CHEMBL320423 1 5.34
CHEMBL102541 1 -
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 -
CHEMBL102720 1 -
CHEMBL102754 1 -
CHEMBL103 PROGESTERONE 4.0 1 -
CHEMBL103092 1 -
CHEMBL318513 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL102179 IC50 = 54.0 nM 7.27
CHEMBL101852 IC50 = 71.0 nM 7.15
CHEMBL103468 IC50 = 105.0 nM 6.98
CHEMBL320411 IC50 = 132.0 nM 6.88
CHEMBL321584 IC50 = 150.0 nM 6.82
CHEMBL103237 IC50 = 150.0 nM 6.82
CHEMBL102403 IC50 = 250.0 nM 6.60
CHEMBL101914 IC50 = 290.0 nM 6.54
CHEMBL323324 IC50 = 342.0 nM 6.47
CHEMBL286595 IC50 = 600.0 nM 6.22
CHEMBL317921 IC50 = 720.0 nM 6.14
CHEMBL320690 IC50 = 930.0 nM 6.03
CHEMBL101907 IC50 = 1100.0 nM 5.96
CHEMBL430855 IC50 = 1136.0 nM 5.95
CHEMBL102602 IC50 = 1207.0 nM 5.92
CHEMBL103232 IC50 = 3138.0 nM 5.50
CHEMBL320423 IC50 = 4600.0 nM 5.34
CHEMBL102541 IC50 > 10000.0 nM -
CHEMBL717 MEDROXYPROGESTERONE ACETATE IC50 < 10000.0 nM -
CHEMBL102720 IC50 > 10000.0 nM -
CHEMBL102754 IC50 > 10000.0 nM -
CHEMBL103 PROGESTERONE IC50 < 10000.0 nM -
CHEMBL103092 IC50 > 10000.0 nM -
CHEMBL318513 IC50 > 10000.0 nM -