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Assay Detail

CHEMBL5167767

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

ADMET
Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate incubated for 5 to 45 mins in presence of NADPH 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 2C19 (CHEMBL3622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Novel Series of Imipridone Compounds as <i>Homo sapiens</i> Caseinolytic Protease P Agonists with Potent Antitumor Activities In Vitro and In Vivo.
Huang J, Zhang J, Luo B, Qiao W, Qiu Z, Song R, Dai Z, Sui J, Xu X, Ruan S, Li C, Luo Y, Yang T.
J Med Chem (2022) 65 : 7629 -7655
PubMed 35609303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.68 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1503 OMEPRAZOLE 4.0 1 5.68
CHEMBL5191392 1 -
CHEMBL4297310 DORDAVIPRONE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1503 OMEPRAZOLE IC50 = 2080.0 nM 5.68
CHEMBL5191392 IC50 > 10000.0 nM -
CHEMBL4297310 DORDAVIPRONE IC50 > 10000.0 nM -