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Assay Detail

CHEMBL4406416

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

ADMET
Inhibition of CYP2B6 in human pooled liver microsomes using bupropion as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 10 mins by UPLC-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 Microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2B6 (CHEMBL4729)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.
Kowalski JP, McDonald MG, Pelletier RD, Hanenberg H, Wiek C, Rettie AE.
J Med Chem (2020) 63 : 4824 -4836
PubMed 32302132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.21 4.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4557940 1 4.21
CHEMBL4442292 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4557940 IC50 = 62000.0 nM 4.21
CHEMBL4442292 IC50 = 258000.0 nM -