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Assay Detail

CHEMBL929422

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

Binding
Inhibition of mouse Flk1
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vascular endothelial growth factor receptor 2 (CHEMBL3337)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Ruel R, Thibeault C, L'Heureux A, Martel A, Cai ZW, Wei D, Qian L, Barrish JC, Mathur A, D'Arienzo C, Hunt JT, Kamath A, Marathe P, Zhang Y, Derbin G, Wautlet B, Mortillo S, Jeyaseelan R, Henley B, Tejwani R, Bhide RS, Trainor GL, Fargnoli J, Lombardo LJ.
Bioorg Med Chem Lett (2008) 18 : 2985 -2989
PubMed 18395443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.28 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261592 1 7.28
CHEMBL258694 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261592 IC50 = 53.0 nM 7.28
CHEMBL258694 IC50 - -