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Assay Detail

CHEMBL1634997

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ADMET
Competitive inhibition of CYP3A in human liver microsomes assessed as midazolam 4-hydroxylation after 5 mins by Dixon plot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Tissue Liver
Subcellular Microsome
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cytochrome P450 3A (CHEMBL2364675)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Comprehensive in vitro analysis of voriconazole inhibition of eight cytochrome P450 (CYP) enzymes: major effect on CYPs 2B6, 2C9, 2C19, and 3A.
Jeong S, Nguyen PD, Desta Z.
Antimicrob Agents Chemother (2009) 53 : 541 -551
PubMed 19029318 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.18 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL638 VORICONAZOLE 4.0 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL638 VORICONAZOLE Ki = 660.0 nM 6.18