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Assay Detail

CHEMBL768814

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Functional
In vitro antagonist activity against human progesterone receptor isoform B(hPR-B) in mammalian(CV-1) cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore.
Pooley CL, Edwards JP, Goldman ME, Wang MW, Marschke KB, Crombie DL, Jones TK.
J Med Chem (1998) 41 : 3461 -3466
PubMed 9719599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.44 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.52
CHEMBL1908373 ONAPRISTONE 2.0 1 8.66
CHEMBL117465 1 7.52
CHEMBL115904 1 7.42
CHEMBL93027 1 7.38
CHEMBL117308 1 7.16
CHEMBL117586 1 7.10
CHEMBL117585 1 6.12
CHEMBL93463 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.3 nM 9.52
CHEMBL1908373 ONAPRISTONE IC50 = 2.2 nM 8.66
CHEMBL117465 IC50 = 30.0 nM 7.52
CHEMBL115904 IC50 = 38.0 nM 7.42
CHEMBL93027 IC50 = 42.0 nM 7.38
CHEMBL117308 IC50 = 70.0 nM 7.16
CHEMBL117586 IC50 = 79.0 nM 7.10
CHEMBL117585 IC50 = 750.0 nM 6.12
CHEMBL93463 IC50 = 783.0 nM 6.11