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Assay Detail

CHEMBL983682

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

Binding
Antagonist activity at glucocorticoid receptor by Gal4-DNA binding domain-hormone receptor LBD one-hybrid assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Glucocorticoid receptor (CHEMBL2034)
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 5 7.68 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276308 MIFEPRISTONE 4.0 1 9.22
CHEMBL489788 1 6.92
CHEMBL522432 1 6.90
CHEMBL520169 1 -
CHEMBL483246 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276308 MIFEPRISTONE IC50 = 0.6 nM 9.22
CHEMBL489788 IC50 = 120.0 nM 6.92
CHEMBL522432 IC50 = 127.0 nM 6.90
CHEMBL520169 IC50 > 3000.0 nM -
CHEMBL483246 IC50 > 3000.0 nM -