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Assay Detail

CHEMBL764954

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Functional
Effective concentration for agonist activity towards human progesterone receptor (hPR) using the cotransfection assay in CV-1 cells
13
Total Activities
13
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
EC50 13 7.86 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292284 1 9.82
CHEMBL65690 1 8.77
CHEMBL65929 1 8.68
CHEMBL62700 1 8.66
CHEMBL103 PROGESTERONE 4.0 1 8.54
CHEMBL302362 1 8.24
CHEMBL62981 1 7.96
CHEMBL63015 1 7.57
CHEMBL65014 1 7.55
CHEMBL65410 1 7.54
CHEMBL418670 1 7.32
CHEMBL64913 1 6.00
CHEMBL62731 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292284 EC50 = 0.15 nM 9.82
CHEMBL65690 EC50 = 1.7 nM 8.77
CHEMBL65929 EC50 = 2.1 nM 8.68
CHEMBL62700 EC50 = 2.2 nM 8.66
CHEMBL103 PROGESTERONE EC50 = 2.9 nM 8.54
CHEMBL302362 EC50 = 5.7 nM 8.24
CHEMBL62981 EC50 = 11.0 nM 7.96
CHEMBL63015 EC50 = 27.0 nM 7.57
CHEMBL65014 EC50 = 28.0 nM 7.55
CHEMBL65410 EC50 = 29.0 nM 7.54
CHEMBL418670 EC50 = 48.0 nM 7.32
CHEMBL64913 EC50 = 1000.0 nM 6.00
CHEMBL62731 EC50 = 2700.0 nM 5.57