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Assay Detail

CHEMBL866476

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ADMET
Inhibition of CYP2D6 by supersome assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.
Berlin M, Ting PC, Vaccaro WD, Aslanian R, McCormick KD, Lee JF, Albanese MM, Mutahi MW, Piwinski JJ, Shih NY, Duguma L, Solomon DM, Zhou W, Sher R, Favreau L, Bryant M, Korfmacher WA, Nardo C, West RE, Anthes JC, Williams SM, Wu RL, Susan She H, Rivelli MA, Corboz MR, Hey JA.
Bioorg Med Chem Lett (2006) 16 : 989 -994
PubMed 16297617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.67 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205129 1 6.00
CHEMBL203805 1 5.70
CHEMBL204705 1 5.30
CHEMBL203604 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205129 IC50 = 1000.0 nM 6.00
CHEMBL203805 IC50 = 2000.0 nM 5.70
CHEMBL204705 IC50 = 5000.0 nM 5.30
CHEMBL203604 IC50 > 30000.0 nM -