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Assay Detail

CHEMBL5326284

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 prewarmed for 10 mins followed by NADPH addition and measured after 10 mins 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 Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimization of BAX trigger site activator BTSA1 with improved antitumor potency and in vitro ADMET properties.
Zhang Z, Zhao S, Pei J, Hou L, Luan S, Deng H, Liu D, Huang M, Zhao L.
Eur J Med Chem (2023) 248 : 115076 -115076
PubMed 36680883 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.53 4.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790235 1 4.53
CHEMBL5422432 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790235 IC50 = 29500.0 nM 4.53
CHEMBL5422432 IC50 > 50000.0 nM -