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Assay Detail

CHEMBL763445

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Functional
Antagonistic activity against Progesterone receptor (PR) in transcriptional activation assay in human T47D breast carcinoma cell line
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type T47D
Confidence 9 — Direct single protein target
Curated By Expert

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.
Zhang P, Terefenko EA, Fensome A, Zhang Z, Zhu Y, Cohen J, Winneker R, Wrobel J, Yardley J.
Bioorg Med Chem Lett (2002) 12 : 787 -790
PubMed 11859003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.43 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.70
CHEMBL117465 1 7.43
CHEMBL163833 1 7.33
CHEMBL164140 1 7.29
CHEMBL167620 1 7.03
CHEMBL350283 1 6.99
CHEMBL349398 1 6.90
CHEMBL165055 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.2 nM 9.70
CHEMBL117465 IC50 = 37.0 nM 7.43
CHEMBL163833 IC50 = 47.0 nM 7.33
CHEMBL164140 IC50 = 51.2 nM 7.29
CHEMBL167620 IC50 = 92.6 nM 7.03
CHEMBL350283 IC50 = 103.0 nM 6.99
CHEMBL349398 IC50 = 126.6 nM 6.90
CHEMBL165055 IC50 = 158.8 nM 6.80