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Assay Detail

CHEMBL929425

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

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

Assay Information

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

Target

Platelet-derived growth factor receptor beta (CHEMBL1913)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.41 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258694 1 6.41
CHEMBL261592 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258694 IC50 = 389.0 nM 6.41
CHEMBL261592 IC50 > 2000.0 nM -