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Assay Detail

CHEMBL861796

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

ADMET
Inhibition of CYP2D6 in human liver microsomes
2
Total Activities
2
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 Expert

Target

Cytochrome P450 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
Vaccaro WD, Sher R, Berlin M, Shih NY, Aslanian R, Schwerdt JH, McCormick KD, Piwinski JJ, West RE, Anthes JC, Williams SM, Wu RL, She HS, Rivelli MA, Mutter JC, Corboz MR, Hey JA, Favreau L.
Bioorg Med Chem Lett (2006) 16 : 395 -399
PubMed 16246552 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.20 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371730 1 7.40
CHEMBL200382 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371730 IC50 = 40.0 nM 7.40
CHEMBL200382 IC50 = 100.0 nM 7.00