Target Validation Information
TTD ID	T47101
Target Name	Fibroblast growth factor receptor 1 (FGFR1)
Type of Target	Successful
Drug Potency against Target	Rosiglitazone + metformin	Drug Info	Ki = 1200 nM	[9]
	2-(1H-indazol-3-yl)-1H-benzo[d]imidazole	Drug Info	IC50 = 1400 nM	[5]
	3-Benzimidazol-2-ylhydroquinolin-2-one	Drug Info	IC50 = 390 nM	[8]
	BMS-695735	Drug Info	IC50 < 5000 nM	[6]
	Brivanib	Drug Info	IC50 = 148 nM	[4]
	HKI-9924129	Drug Info	IC50 = 934 nM	[1]
	NP-506	Drug Info	IC50 = 100 nM	[7]
	PD-0166326	Drug Info	IC50 = 61.5 nM	[1]
	PD-0173952	Drug Info	IC50 = 98.8 nM	[1]
	PD-0173955	Drug Info	IC50 = 1250 nM	[1]
	PD-0173956	Drug Info	IC50 = 933 nM	[1]
	PD-0173958	Drug Info	IC50 = 451 nM	[1]
	PD-0179483	Drug Info	IC50 = 244 nM	[1]
	PD-0183812	Drug Info	IC50 = 8620 nM	[2]
	Ro-4396686	Drug Info	IC50 = 92 nM	[3]
Action against Disease Model	Rosiglitazone + metformin	Drug Info	To determine whether inhibition of purified receptors translated into a biological effect in cells, the ability of SU6668 to modulate VEGF- and acidic FGF-induced mitogenesis ofendothelial cells was examined. SU6668 inhibited VEGF-driven mitogenesis of HUVECs in a dose-dependent manner with a mean IC50 of 0.34 ???0.05 uM.In comparison, FGF-driven mitogenesis of HUVECs was inhibited with a mean IC50 of 9.6 ???0.4 uM.	[9]
References
REF 1	Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. Biochem Pharmacol. 2000 Oct 1;60(7):885-98.
REF 2	Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem. 2000 Nov 30;43(24):4606-16.
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	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-... J Med Chem. 2006 Apr 6;49(7):2143-6.
REF 5	Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9.
REF 6	Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)py... J Med Chem. 2008 Oct 9;51(19):5897-900.
REF 7	5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorg Med Chem Lett. 2009 Feb 1;19(3):745-50.
REF 8	Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor... J Med Chem. 2009 Jan 22;52(2):278-92.
REF 9	SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60.

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