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Assay Detail

CHEMBL4843561

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

ADMET
Inhibition of CYP3A4 in human liver microsome using Nifedipine as a substrate incubated for 10 mins in the presence of NADPH by LC-MS/MS analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
Zhao L, Yin W, Sun Y, Sun N, Tian L, Zheng Y, Zhang C, Zhao S, Su X, Zhao D, Cheng M.
Eur J Med Chem (2021) 224 : 113715 -113715
PubMed 34364163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.52 7.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157101 KETOCONAZOLE 4.0 1 7.93
CHEMBL64391 ITRACONAZOLE 4.0 1 7.49
CHEMBL91 MICONAZOLE 4.0 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157101 KETOCONAZOLE IC50 = 11.7 nM 7.93
CHEMBL64391 ITRACONAZOLE IC50 = 32.6 nM 7.49
CHEMBL91 MICONAZOLE IC50 = 74.2 nM 7.13