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Assay Detail

CHEMBL960945

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

Binding
Inhibition of c-Met
4
Total Activities
4
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

N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.
Raeppel S, Claridge S, Saavedra O, Gaudette F, Zhan L, Mannion M, Zhou N, Raeppel F, Granger MC, Isakovic L, Déziel R, Nguyen H, Beaulieu N, Beaulieu C, Dupont I, Robert MF, Lefebvre S, Dubay M, Rahil J, Wang J, Ste-Croix H, Robert Macleod A, Besterman J, Vaisburg A.
Bioorg Med Chem Lett (2009) 19 : 1323 -1328
PubMed 19211249 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.40 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489326 EXELIXIS 1 7.68
CHEMBL450786 PHA-665752 1 7.42
CHEMBL404881 1 7.10
CHEMBL535 SUNITINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489326 EXELIXIS IC50 = 21.0 nM 7.68
CHEMBL450786 PHA-665752 IC50 = 38.0 nM 7.42
CHEMBL404881 IC50 = 80.0 nM 7.10
CHEMBL535 SUNITINIB IC50 > 5000.0 nM -