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Assay Detail

CHEMBL4151848

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

Binding
Antagonist activity at GR in human OVCAR5 assessed as reduction in dexamethasone-induced GILZ gene expression incubated for 24 hrs by RT-qPCR method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Rew Y, Du X, Eksterowicz J, Zhou H, Jahchan N, Zhu L, Yan X, Kawai H, McGee LR, Medina JC, Huang T, Chen C, Zavorotinskaya T, Sutimantanapi D, Waszczuk J, Jackson E, Huang E, Ye Q, Fantin VR, Sun D.
J Med Chem (2018) 61 : 7767 -7784
PubMed 30091920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.76 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161754 1 7.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161754 IC50 = 17.2 nM 7.76