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Assay Detail

CHEMBL768817

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Functional
Inhibitory concentration for antagonistic activity towards human progesterone receptor (hPR) using the cotransfection assay in CV-1 cells
7
Total Activities
7
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

Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.
Zhi L, Tegley CM, Pio B, Edwards JP, Jones TK, Marschke KB, Mais DE, Risek B, Schrader WT.
Bioorg Med Chem Lett (2003) 13 : 2071 -2074
PubMed 12781197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.86 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.52
CHEMBL62731 1 7.19
CHEMBL65227 1 6.91
CHEMBL65689 1 6.61
CHEMBL418670 1 6.10
CHEMBL63015 1 6.01
CHEMBL303768 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.3 nM 9.52
CHEMBL62731 IC50 = 65.0 nM 7.19
CHEMBL65227 IC50 = 124.0 nM 6.91
CHEMBL65689 IC50 = 243.0 nM 6.61
CHEMBL418670 IC50 = 800.0 nM 6.10
CHEMBL63015 IC50 = 980.0 nM 6.01
CHEMBL303768 IC50 = 1930.0 nM 5.71