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Assay Detail

CHEMBL679351

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

Functional
Antagonistic activity was determined in Human estrogen receptor(hER) of CV-1 cells in cotransfection assay.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CV-1
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
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 14 5.88 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101914 1 6.52
CHEMBL101907 1 5.98
CHEMBL430855 1 5.96
CHEMBL102720 1 5.91
CHEMBL103092 1 5.84
CHEMBL102754 1 5.84
CHEMBL320690 1 5.83
CHEMBL318513 1 5.81
CHEMBL286595 1 5.74
CHEMBL102403 1 5.62
CHEMBL317921 1 5.58
CHEMBL103232 1 -
CHEMBL103 PROGESTERONE 4.0 1 -
CHEMBL102541 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101914 IC50 = 299.0 nM 6.52
CHEMBL101907 IC50 = 1037.0 nM 5.98
CHEMBL430855 IC50 = 1095.0 nM 5.96
CHEMBL102720 IC50 = 1220.0 nM 5.91
CHEMBL103092 IC50 = 1449.0 nM 5.84
CHEMBL102754 IC50 = 1449.0 nM 5.84
CHEMBL320690 IC50 = 1480.0 nM 5.83
CHEMBL318513 IC50 = 1537.0 nM 5.81
CHEMBL286595 IC50 = 1803.0 nM 5.74
CHEMBL102403 IC50 = 2395.0 nM 5.62
CHEMBL317921 IC50 = 2632.0 nM 5.58
CHEMBL103232 IC50 > 10000.0 nM -
CHEMBL103 PROGESTERONE IC50 < 10000.0 nM -
CHEMBL102541 IC50 > 10000.0 nM -