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Assay Detail

CHEMBL5107199

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

ADMET
Inhibition of CYP2D6 in human liver microsomes at 10 uM using dextromethorphan as substrate preincubated for 10 mins followed by NADPH addition by LC/MS analysis
3
Total Activities
3
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

Discovery of Orally Bioavailable SOS1 Inhibitors for Suppressing KRAS-Driven Carcinoma.
He H, Zhang Y, Xu J, Li Y, Fang H, Liu Y, Zhang S.
J Med Chem (2022) 65 : 13158 -13171
PubMed 36173339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.21 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5209105 1 5.60
CHEMBL5196432 1 5.21
CHEMBL5203150 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5209105 IC50 = 2500.0 nM 5.60
CHEMBL5196432 IC50 = 6100.0 nM 5.21
CHEMBL5203150 IC50 = 14800.0 nM 4.83