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Assay Detail

CHEMBL4158409

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

ADMET
Inhibition of of CYP3A4 in human liver microsomes using midazolam as substrate after 10 mins in presence of NADPH by LC-MS/MS analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).
Wehn PM, Rizzi JP, Dixon DD, Grina JA, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Cao Z, Cheng T, Czerwinski RM, Goggin BS, Huang H, Halfmann MM, Maddie MA, Morton EL, Olive SR, Tan H, Xie S, Wong T, Josey JA, Wallace EM.
J Med Chem (2018) 61 : 9691 -9721
PubMed 30289716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.88 4.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4175320 1 4.88
CHEMBL4173075 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4175320 IC50 = 13300.0 nM 4.88
CHEMBL4173075 IC50 > 50000.0 nM -