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Assay Detail

CHEMBL5636881

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

ADMET
Inhibition of CYP2C19 in human liver microsomes using mephenytoin as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by LC-MS analysis
2
Total Activities
2
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

Exploring the structural-activity relationship of hexahydropyrazino[1,2-d]pyrido[3,2-b][1,4]oxazine derivatives as potent and orally-bioavailable PARP7 inhibitors.
Zhang S, Zhang Y, Wang Z, Qing L, Fu S, Xu J, Li Y, Fang H, He H.
Eur J Med Chem (2023) 261 : 115836 -115836
PubMed 37826932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.12 5.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5639789 1 5.12
CHEMBL5095043 ATAMPARIB 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5639789 IC50 = 7550.0 nM 5.12
CHEMBL5095043 ATAMPARIB IC50 > 30000.0 nM -