| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T63966 | ||||
| Target Name | Vascular endothelial growth factor receptor 1 | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Cediranib | Drug Info | IC50 = 2 nM | [552828] | |
| SU-14813 | Drug Info | IC50 = 2 nM | [552773] | ||
| CEP-11981 | Drug Info | IC50 = 12 nM | [552381] | ||
| Motesanib | Drug Info | IC50 = 2 nM | [552773] | ||
| SU-11652 | Drug Info | IC50 = 50 nM | [526575] | ||
| KRN633 | Drug Info | IC50 = 1.16 nM | [552727] | ||
| Sorafenib | Drug Info | Ki = 20~90 nM | [552459] | ||
| Axitinib | Drug Info | IC50 = 1.2 nM | [552885] | ||
| Action against Disease Model | Sorafenib | Activity on H9c2 cellline is 10,160 nM | [552843] | Drug Info | |
| References | |||||
| Ref 552828 | Therapeutic potential of novel selective-spectrum kinase inhibitors in oncology. Expert Opin Investig Drugs. 2008 Jul;17(7):1013-28. doi: 10.1517/13543784.17.7.1013 . | ||||
| Ref 552773 | A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358. | ||||
| Ref 552381 | 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 552773 | A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358. | ||||
| Ref 526575 | J Med Chem. 2003 Mar 27;46(7):1116-9.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 tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. | ||||
| Ref 552727 | Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93. | ||||
| Ref 552459 | 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 552843 | 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. doi: 10.1093/toxsci/kfn157. Epub 2008 Jul 29. | ||||
| Ref 552885 | 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. doi: 10.1158/1078-0432.CCR-08-0652. | ||||
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