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Assay Detail

CHEMBL4222469

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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 microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Yu T, Zhang Y, Kerekes AD, Tagat JR, Doll RJ, Xiao Y, Esposite S, Hruza A, Belanger DB, Voss M, Rainka MP, Basso A, Liu M, Liang L, Sui N, Prelusky D, Rindgen D, Zhang L.
Bioorg Med Chem Lett (2018) 28 : 1397 -1403
PubMed 29545102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.94 4.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4225923 1 4.94
CHEMBL4227082 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4225923 IC50 = 11500.0 nM 4.94
CHEMBL4227082 IC50 > 20000.0 nM -