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Assay Detail

CHEMBL5045404

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

ADMET
Time dependent inhibition of recombinant human CYP3A5 incubated for 30 mins in presence of NADPH generating system 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
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 3A5 (CHEMBL3019)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Unique Oxidative Metabolism of Bufalin Generates Two Reactive Metabolites That Strongly Inactivate Human Cytochrome P450 3A.
Tu D, Ning J, Zou L, Wang P, Zhang Y, Tian X, Zhang F, Zheng J, Ge G.
J Med Chem (2022) 65 : 4018 -4029
PubMed 35094507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.41 5.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399680 BUFALIN 1 5.56
CHEMBL2068968 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399680 BUFALIN IC50 = 2760.0 nM 5.56
CHEMBL2068968 IC50 = 5490.0 nM 5.26