Target Validation Information
TTD ID T63966
Target Name Vascular endothelial growth factor receptor 1 (FLT-1)
Type of Target
Drug Potency against Target Sorafenib Drug Info Ki = 20~90 nM [3]
Axitinib Drug Info IC50 = 1.2 nM [8]
Cediranib Drug Info IC50 = 2 nM [6]
CEP-11981 Drug Info IC50 = 12 nM [2]
KRN633 Drug Info IC50 = 1.16 nM [4]
Motesanib Drug Info IC50 = 2 nM [5]
SU-14813 Drug Info IC50 = 2 nM [5]
SU-11652 Drug Info IC50 = 50 nM [1]
Action against Disease Model Sorafenib Drug Info Activity on H9c2 cellline is 10,160 nM [7]
REF 1 Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
REF 2 CEP-7055: a novel, orally active pan inhibitor of vascular endothelial growth factor receptor tyrosine kinases with potent antiangiogenic activity and antitumor efficacy in preclinical models. Cancer Res. 2003 Sep 15;63(18):5978-91.
REF 3 BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109.
REF 4 Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
REF 5 A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32.
REF 6 Therapeutic potential of novel selective-spectrum kinase inhibitors in oncology. Expert Opin Investig Drugs. 2008 Jul;17(7):1013-28.
REF 7 Effect of the multitargeted tyrosine kinase inhibitors imatinib, dasatinib, sunitinib, and sorafenib on mitochondrial function in isolated rat heart mitochondria and H9c2 cells. Toxicol Sci. 2008 Nov;106(1):153-61.
REF 8 Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res. 2008 Nov 15;14(22):7272-83.

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