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Assay Detail

CHEMBL959569

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

ADMET
Inhibition of CYP3A4
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.
Schroeder GM, An Y, Cai ZW, Chen XT, Clark C, Cornelius LA, Dai J, Gullo-Brown J, Gupta A, Henley B, Hunt JT, Jeyaseelan R, Kamath A, Kim K, Lippy J, Lombardo LJ, Manne V, Oppenheimer S, Sack JS, Schmidt RJ, Shen G, Stefanski K, Tokarski JS, Trainor GL, Wautlet BS, Wei D, Williams DK, Zhang Y, Zhang Y, Fargnoli J, Borzilleri RM.
J Med Chem (2009) 52 : 1251 -1254
PubMed 19260711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.40 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462624 1 5.40
CHEMBL462622 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462624 IC50 = 4000.0 nM 5.40
CHEMBL462622 IC50 < 1000.0 nM -