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Assay Detail

CHEMBL4151845

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

Binding
Antagonist activity at GR in monkey PBMC assessed as reduction in dexamethasone-induced FKBP5 gene expression incubated for 6 hrs by RT-qPCR method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca mulatta
Cell Type PBMC
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 2 7.81 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161754 1 7.96
CHEMBL1276308 MIFEPRISTONE 4.0 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161754 IC50 = 11.1 nM 7.96
CHEMBL1276308 MIFEPRISTONE IC50 = 21.9 nM 7.66