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Assay Detail

CHEMBL4433306

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

ADMET
Inhibition of human recombinant CYP2D6 using luciferin as substrate preincubated for 10 mins followed by substrate addition and measured after 50 mins in presence of NADPH by CYP450-Glo assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H<sub>3</sub> receptor ligands.
Łażewska D, Kaleta M, Schwed JS, Karcz T, Mogilski S, Latacz G, Olejarz A, Siwek A, Kubacka M, Lubelska A, Honkisz E, Handzlik J, Filipek B, Stark H, Kieć-Kononowicz K.
Bioorg Med Chem (2017) 25 : 5341 -5354
PubMed 28797771 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.16 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1294 QUINIDINE 4.0 1 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1294 QUINIDINE IC50 = 6.9 nM 8.16