Target Validation Information
TTD ID	T91331
Target Name	Fibroblast growth factor receptor 3 (FGFR3)
Type of Target	Successful
Drug Potency against Target	AEE-788	Drug Info	IC50 = 6 nM	[5]
	TKI258	Drug Info	Ki = 8 nM	[6]
	5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol	Drug Info	IC50 = 400 nM	[2]
	PD-0183812	Drug Info	IC50 = 8620 nM	[1]
	Ro-4396686	Drug Info	IC50 = 92 nM	[3]
Action against Disease Model	AEE-788	Drug Info	AEE788 inhibited EGFR and VEGF receptor tyrosine kinases in the nm range (IC(50)s: EGFR 2 nm, ErbB2 6 nm, KDR 77 nm, and Flt-1 59 nm). In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited (IC(50)s: 11 and 220 nm, respectively). AEE788 demonstrated antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines (including EGFRvIII-dependent lines) and inhibited the proliferation of epidermal growth factor- and VEGF-stimulated h uMan uMbilical vein endothelial cells.	[4]
References
REF 1	Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem. 2000 Nov 30;43(24):4606-16.
REF 2	Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases. J Med Chem. 2005 Oct 6;48(20):6194-201.
REF 3	Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
REF 4	AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 2004 Jul 15;64(14):4931-41.
REF 5	Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
REF 6	An overview of small-molecule inhibitors of VEGFR signaling. Nat Rev Clin Oncol. 2009 Oct;6(10):569-79.

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