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Assay Detail

CHEMBL5384795

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 assessed as reduction in substrate hydroxylation incubated for 10 mins in presence of NADPH by LC-MS/MS analysis
1
Total Activities
1
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 Potent, Selective, and Orally Bioavailable Small-Molecule Inhibitors of CDK8 for the Treatment of Cancer.
Li Y, Liu Y, Wu J, Liu X, Wang L, Wang J, Yu J, Qi H, Qin L, Ding X, Ren F, Zhavoronkov A.
J Med Chem (2023) 66 : 5439 -5452
PubMed 37029334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.51 4.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5396725 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5396725 IC50 = 30800.0 nM 4.51