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Assay Detail

CHEMBL957339

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

ADMET
Inhibition of CYP2D6 in human liver microsomes assessed as dextromethorphan O-demethylase activity
6
Total Activities
6
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 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
Wijtmans M, Celanire S, Snip E, Gillard MR, Gelens E, Collart PP, Venhuis BJ, Christophe B, Hulscher S, van der Goot H, Lebon F, Timmerman H, Bakker RA, Lallemand BI, Leurs R, Talaga PE, de Esch IJ.
J Med Chem (2008) 51 : 2944 -2953
PubMed 18433114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.13 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494982 1 6.54
CHEMBL449840 1 6.31
CHEMBL455475 1 6.26
CHEMBL451399 1 6.19
CHEMBL493014 1 5.75
CHEMBL489493 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494982 IC50 = 292.0 nM 6.54
CHEMBL449840 IC50 = 488.0 nM 6.31
CHEMBL455475 IC50 = 543.0 nM 6.26
CHEMBL451399 IC50 = 644.0 nM 6.19
CHEMBL493014 IC50 = 1785.0 nM 5.75
CHEMBL489493 IC50 = 1926.0 nM 5.71