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Assay Detail

CHEMBL983679

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

Binding
Displacement of [3H]progesterone from progesterone receptor in human T47D cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 8 7.85 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492021 1 8.62
CHEMBL522432 1 8.47
CHEMBL523659 1 8.42
CHEMBL491206 1 7.97
CHEMBL483246 1 7.55
CHEMBL521141 1 7.44
CHEMBL520169 1 7.22
CHEMBL521760 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492021 IC50 = 2.4 nM 8.62
CHEMBL522432 IC50 = 3.4 nM 8.47
CHEMBL523659 IC50 = 3.8 nM 8.42
CHEMBL491206 IC50 = 10.7 nM 7.97
CHEMBL483246 IC50 = 28.4 nM 7.55
CHEMBL521141 IC50 = 36.0 nM 7.44
CHEMBL520169 IC50 = 60.0 nM 7.22
CHEMBL521760 IC50 = 75.0 nM 7.12