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Assay Detail

CHEMBL924778

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

Binding
Inhibition of human VEGFR2-dependent ERK phosphorylation in HUVEC
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HUVEC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases.
Claridge S, Raeppel F, Granger MC, Bernstein N, Saavedra O, Zhan L, Llewellyn D, Wahhab A, Deziel R, Rahil J, Beaulieu N, Nguyen H, Dupont I, Barsalou A, Beaulieu C, Chute I, Gravel S, Robert MF, Lefebvre S, Dubay M, Pascal R, Gillespie J, Jin Z, Wang J, Besterman JM, MacLeod AR, Vaisburg A.
Bioorg Med Chem Lett (2008) 18 : 2793 -2798
PubMed 18434145 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.52 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535 SUNITINIB 4.0 1 7.52
CHEMBL254760 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535 SUNITINIB IC50 = 30.0 nM 7.52
CHEMBL254760 IC50 = 30.0 nM 7.52