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Assay Detail

CHEMBL844073

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

Functional
Antagonist activity against progesterone receptor (PR) in an alkaline phosphatase assay in the T47D human breast carcinoma cell line
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
Zhang P, Terefenko EA, Fensome A, Wrobel J, Winneker R, Lundeen S, Marschke KB, Zhang Z.
J Med Chem (2002) 45 : 4379 -4382
PubMed 12238914 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.83 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.89
CHEMBL138059 1 8.10
CHEMBL138005 1 8.09
CHEMBL136721 1 7.82
CHEMBL303209 1 7.77
CHEMBL136166 1 7.71
CHEMBL343306 1 7.64
CHEMBL139406 1 7.58
CHEMBL136806 1 7.52
CHEMBL342199 1 7.52
CHEMBL343083 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.13 nM 9.89
CHEMBL138059 IC50 = 8.0 nM 8.10
CHEMBL138005 IC50 = 8.2 nM 8.09
CHEMBL136721 IC50 = 15.1 nM 7.82
CHEMBL303209 IC50 = 17.0 nM 7.77
CHEMBL136166 IC50 = 19.5 nM 7.71
CHEMBL343306 IC50 = 23.0 nM 7.64
CHEMBL139406 IC50 = 26.2 nM 7.58
CHEMBL136806 IC50 = 30.0 nM 7.52
CHEMBL342199 IC50 = 30.0 nM 7.52
CHEMBL343083 IC50 = 300.0 nM 6.52