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Assay Detail

CHEMBL3768882

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

ADMET
Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate incubated for 7 mins by LC-MS analysis
4
Total Activities
4
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 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.
Chupak LS, Zheng X, Hu S, Huang Y, Ding M, Lewis MA, Westphal RS, Blat Y, McClure A, Gentles RG.
Bioorg Med Chem (2016) 24 : 1455 -1468
PubMed 26917221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.77 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3765022 1 5.40
CHEMBL3764017 1 4.89
CHEMBL3764044 1 4.40
CHEMBL3764377 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3765022 IC50 = 4000.0 nM 5.40
CHEMBL3764017 IC50 = 13000.0 nM 4.89
CHEMBL3764044 IC50 = 40000.0 nM 4.40
CHEMBL3764377 IC50 = 40000.0 nM 4.40