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Assay Detail

CHEMBL5375743

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 5 mins in presence of NADPH by UPLC-MS/MS analysis
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 Autocuration

Target

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

Publication

Atypical <i>N</i>-Alkyl to <i>N</i>-Noralkoxy Switch in a Dual cSRC/BCR-ABL1 Kinase Inhibitor Improves Drug Efflux and hERG Affinity.
Hill J, Jones RM, Crich D.
ACS Med Chem Lett (2023) 14 : 1869 -1875
PubMed 38116407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.12 5.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5435819 1 5.12
CHEMBL288441 BOSUTINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5435819 IC50 = 7600.0 nM 5.12
CHEMBL288441 BOSUTINIB IC50 - -