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Assay Detail

CHEMBL5035201

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

ADMET
Inhibition of CYP2C19 in human pooled liver microsomes using S-mephenytoin as substrate in presence of NADPH by LC-MS/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 Microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2C19 (CHEMBL3622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer.
Liu Z, Yu P, Dong L, Wang W, Duan S, Wang B, Gong X, Ye L, Wang H, Tian J.
J Med Chem (2021) 64 : 10286 -10296
PubMed 34253025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.48 4.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4298138 REPOTRECTINIB 4.0 1 4.91
CHEMBL5080010 1 4.05
CHEMBL4297627 SELITRECTINIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4298138 REPOTRECTINIB IC50 = 12300.0 nM 4.91
CHEMBL5080010 IC50 = 89000.0 nM 4.05
CHEMBL4297627 SELITRECTINIB IC50 > 50000.0 nM -