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Assay Detail

CHEMBL3789265

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

ADMET
Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate by LC-MS/MS analysis in presence of NADPH
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

Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase.
Diaz P, Huang W, Keyari CM, Buttrick B, Price L, Guilloteau N, Tripathy S, Sperandio VG, Fronczek FR, Astruc-Diaz F, Isoherranen N.
J Med Chem (2016) 59 : 2579 -2595
PubMed 26918322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.82 5.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3787323 1 5.12
CHEMBL3786581 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3787323 IC50 = 7500.0 nM 5.12
CHEMBL3786581 IC50 = 30000.0 nM 4.52