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Assay Detail

CHEMBL859792

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

Binding
Inhibitory activity against Flk1
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Bhide RS, Cai ZW, Zhang YZ, Qian L, Wei D, Barbosa S, Lombardo LJ, Borzilleri RM, Zheng X, Wu LI, Barrish JC, Kim SH, Leavitt K, Mathur A, Leith L, Chao S, Wautlet B, Mortillo S, Jeyaseelan R, Kukral D, Hunt JT, Kamath A, Fura A, Vyas V, Marathe P, D'Arienzo C, Derbin G, Fargnoli J.
J Med Chem (2006) 49 : 2143 -2146
PubMed 16570908 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.05 7.05
Ki 1 7.55 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377300 BRIVANIB 3.0 2 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377300 BRIVANIB Ki = 28.0 nM 7.55
CHEMBL377300 BRIVANIB IC50 = 89.0 nM 7.05