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Assay Detail

CHEMBL768822

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

Binding
Inhibition of human progesterone receptor activation in T47D human breast cancer cell.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type T47D
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
Zhi L, Ringgenberg JD, Edwards JP, Tegley CM, West SJ, Pio B, Motamedi M, Jones TK, Marschke KB, Mais DE, Schrader WT.
Bioorg Med Chem Lett (2003) 13 : 2075 -2078
PubMed 12781198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.76 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1908373 ONAPRISTONE 2.0 1 8.48
CHEMBL1276308 MIFEPRISTONE 4.0 1 8.48
CHEMBL294116 1 7.00
CHEMBL293409 1 6.98
CHEMBL67362 1 6.86
CHEMBL62227 1 6.83
CHEMBL64294 1 6.82
CHEMBL65522 1 6.73
CHEMBL63788 1 6.66
CHEMBL65079 1 6.47
CHEMBL62798 1 6.43
CHEMBL63610 1 6.43
CHEMBL62761 1 6.34
CHEMBL65380 1 6.32
CHEMBL63870 1 6.31
CHEMBL65054 1 6.30
CHEMBL62714 1 6.11
CHEMBL65307 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1908373 ONAPRISTONE IC50 = 3.3 nM 8.48
CHEMBL1276308 MIFEPRISTONE IC50 = 3.3 nM 8.48
CHEMBL294116 IC50 = 100.0 nM 7.00
CHEMBL293409 IC50 = 104.0 nM 6.98
CHEMBL67362 IC50 = 138.0 nM 6.86
CHEMBL62227 IC50 = 149.0 nM 6.83
CHEMBL64294 IC50 = 152.0 nM 6.82
CHEMBL65522 IC50 = 187.0 nM 6.73
CHEMBL63788 IC50 = 217.0 nM 6.66
CHEMBL65079 IC50 = 335.0 nM 6.47
CHEMBL62798 IC50 = 374.0 nM 6.43
CHEMBL63610 IC50 = 368.0 nM 6.43
CHEMBL62761 IC50 = 461.0 nM 6.34
CHEMBL65380 IC50 = 483.0 nM 6.32
CHEMBL63870 IC50 = 485.0 nM 6.31
CHEMBL65054 IC50 = 499.0 nM 6.30
CHEMBL62714 IC50 = 782.0 nM 6.11
CHEMBL65307 IC50 = 811.0 nM 6.09