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Assay Detail

CHEMBL1832819

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ADMET
Inhibition of CYP2C19 in human liver microsomes by fluorescence assay
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 2C19 (CHEMBL3622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
Wang H, Yu N, Chen D, Lee KC, Lye PL, Chang JW, Deng W, Ng MC, Lu T, Khoo ML, Poulsen A, Sangthongpitag K, Wu X, Hu C, Goh KC, Wang X, Fang L, Goh KL, Khng HH, Goh SK, Yeo P, Liu X, Bonday Z, Wood JM, Dymock BW, Kantharaj E, Sun ET.
J Med Chem (2011) 54 : 4694 -4720
PubMed 21634430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.11 5.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3215861 1 5.24
CHEMBL1830397 1 5.09
CHEMBL1830424 1 4.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3215861 IC50 = 5780.0 nM 5.24
CHEMBL1830397 IC50 = 8100.0 nM 5.09
CHEMBL1830424 IC50 = 10300.0 nM 4.99