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Assay Detail

CHEMBL4151827

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

ADMET
Inhibition of CYP3A4 (unknown origin) using midazolam as substrate
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 3A4 (CHEMBL340)
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 3 5.45 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4161754 1 5.80
CHEMBL4163069 1 5.54
CHEMBL1276308 MIFEPRISTONE 4.0 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4161754 IC50 = 1600.0 nM 5.80
CHEMBL4163069 IC50 = 2900.0 nM 5.54
CHEMBL1276308 MIFEPRISTONE IC50 = 9500.0 nM 5.02