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Assay Detail

CHEMBL983678

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Functional
Antagonist activity at progesterone receptor assessed as progesterone-induced alkaline phosphatase activity in human T47D cells
13
Total Activities
13
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 Autocuration

Target

Progesterone receptor (CHEMBL208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.
Kern JC, Terefenko EA, Fensome A, Unwalla R, Wrobel J, Cohen J, Zhu Y, Berrodin TJ, Yudt MR, Winneker RC, Zhang Z, Zhang P.
Bioorg Med Chem Lett (2008) 18 : 5015 -5017
PubMed 18722119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.59 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.70
CHEMBL483246 1 8.18
CHEMBL521610 1 8.00
CHEMBL520169 1 7.95
CHEMBL521760 1 7.84
CHEMBL521141 1 7.84
CHEMBL491030 1 7.77
CHEMBL523825 1 7.44
CHEMBL489991 1 7.25
CHEMBL482625 1 6.92
CHEMBL482624 1 6.76
CHEMBL483454 1 6.71
CHEMBL482831 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.2 nM 9.70
CHEMBL483246 IC50 = 6.6 nM 8.18
CHEMBL521610 IC50 = 10.0 nM 8.00
CHEMBL520169 IC50 = 11.3 nM 7.95
CHEMBL521760 IC50 = 14.6 nM 7.84
CHEMBL521141 IC50 = 14.3 nM 7.84
CHEMBL491030 IC50 = 17.1 nM 7.77
CHEMBL523825 IC50 = 36.5 nM 7.44
CHEMBL489991 IC50 = 56.6 nM 7.25
CHEMBL482625 IC50 = 119.8 nM 6.92
CHEMBL482624 IC50 = 175.1 nM 6.76
CHEMBL483454 IC50 = 197.4 nM 6.71
CHEMBL482831 IC50 = 500.0 nM 6.30