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Assay Detail

CHEMBL2186747

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

ADMET
Inhibition of CYP2D6 in human liver microsomes using dextrometorphan as substrate
1
Total Activities
1
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

Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators.
Bischoff F, Berthelot D, De Cleyn M, Macdonald G, Minne G, Oehlrich D, Pieters S, Surkyn M, Trabanco AA, Tresadern G, Van Brandt S, Velter I, Zaja M, Borghys H, Masungi C, Mercken M, Gijsen HJ.
J Med Chem (2012) 55 : 9089 -9106
PubMed 22650177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.44 5.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151164 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151164 IC50 = 3600.0 nM 5.44