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Assay Detail

CHEMBL959570

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Binding
Inhibition of MET
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Hepatocyte growth factor receptor (CHEMBL3717)
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 12 8.56 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462622 1 9.00
CHEMBL462624 1 9.00
CHEMBL509101 1 8.74
CHEMBL461583 1 8.59
CHEMBL518656 1 8.57
CHEMBL461582 1 8.49
CHEMBL517293 1 8.47
CHEMBL462623 1 8.47
CHEMBL460502 1 8.42
CHEMBL460702 BMS-777607 2.0 1 8.41
CHEMBL516790 1 8.35
CHEMBL515858 1 8.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462622 IC50 = 1.0 nM 9.00
CHEMBL462624 IC50 = 1.0 nM 9.00
CHEMBL509101 IC50 = 1.8 nM 8.74
CHEMBL461583 IC50 = 2.6 nM 8.59
CHEMBL518656 IC50 = 2.7 nM 8.57
CHEMBL461582 IC50 = 3.2 nM 8.49
CHEMBL517293 IC50 = 3.4 nM 8.47
CHEMBL462623 IC50 = 3.4 nM 8.47
CHEMBL460502 IC50 = 3.8 nM 8.42
CHEMBL460702 BMS-777607 IC50 = 3.9 nM 8.41
CHEMBL516790 IC50 = 4.5 nM 8.35
CHEMBL515858 IC50 = 5.9 nM 8.23