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Assay Detail

CHEMBL983677

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

Binding
Activity at progesterone receptor assessed as alkaline phosphatase activity in human T47D cells
15
Total Activities
15
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
EC50 15 8.36 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489788 1 9.40
CHEMBL490825 1 9.30
CHEMBL523659 1 9.15
CHEMBL492021 1 9.10
CHEMBL522432 1 9.10
CHEMBL103 PROGESTERONE 4.0 1 9.05
CHEMBL67860 1 8.96
CHEMBL492228 1 8.96
CHEMBL491206 1 8.48
CHEMBL522264 1 8.48
CHEMBL489781 1 7.52
CHEMBL520127 1 7.43
CHEMBL506863 1 6.96
CHEMBL491205 1 6.86
CHEMBL446389 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489788 EC50 = 0.4 nM 9.40
CHEMBL490825 EC50 = 0.5 nM 9.30
CHEMBL523659 EC50 = 0.7 nM 9.15
CHEMBL492021 EC50 = 0.8 nM 9.10
CHEMBL522432 EC50 = 0.8 nM 9.10
CHEMBL103 PROGESTERONE EC50 = 0.9 nM 9.05
CHEMBL67860 EC50 = 1.1 nM 8.96
CHEMBL492228 EC50 = 1.1 nM 8.96
CHEMBL491206 EC50 = 3.3 nM 8.48
CHEMBL522264 EC50 = 3.3 nM 8.48
CHEMBL489781 EC50 = 30.5 nM 7.52
CHEMBL520127 EC50 = 37.5 nM 7.43
CHEMBL506863 EC50 = 110.0 nM 6.96
CHEMBL491205 EC50 = 137.7 nM 6.86
CHEMBL446389 EC50 = 245.8 nM 6.61