Target Validation Information
TTD ID	T07303
Target Name	Vascular endothelial growth factor receptor 3 (FLT-4)
Type of Target	Successful
Drug Potency against Target	Axitinib	Drug Info	IC50 = 0.1~0.3 nM	[10]
	Cediranib	Drug Info	IC50 < 1 nM	[8]
	CEP-11981	Drug Info	IC50 = 17 nM	[7]
	KRN633	Drug Info	IC50 = 50 nM	[3]
	Motesanib	Drug Info	IC50 = 6 nM	[9]
	SU-14813	Drug Info	IC50 = 15 nM	[9]
	(2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine	Drug Info	IC50 = 3260 nM	[4]
	(5-Phenyl-oxazol-2-yl)-m-tolyl-amine	Drug Info	IC50 = 1700 nM	[4]
	2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile	Drug Info	IC50 = 14400 nM	[4]
	3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine	Drug Info	IC50 = 622 nM	[1]
	3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile	Drug Info	IC50 = 7600 nM	[4]
	4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide	Drug Info	IC50 = 4660 nM	[4]
	4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 14000 nM	[2]
	4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 15000 nM	[2]
	4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 14000 nM	[2]
	4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 6300 nM	[2]
	4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 11000 nM	[2]
	CB-676475	Drug Info	IC50 = 1000 nM	[5]
	CEP-6331	Drug Info	IC50 = 2459 nM	[6]
	N-(2,4-Dichloro-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 530 nM	[2]
	N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide	Drug Info	IC50 = 15000 nM	[2]
	Phenyl-(5-phenyl-oxazol-2-yl)-amine	Drug Info	IC50 = 3000 nM	[4]
	VATALANIB	Drug Info	IC50 = 100 nM	[4]
	[3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol	Drug Info	IC50 = 1650 nM	[4]
References
REF 1	Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors. Bioorg Med Chem Lett. 2002 Oct 7;12(19):2767-70.
REF 2	Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents. J Med Chem. 2004 Oct 21;47(22):5367-80.
REF 3	KRN633: A selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase that suppresses tumor angiogenesis and growth. Mol Cancer Ther. 2004 Dec;3(12):1639-49.
REF 4	Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9.
REF 5	Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases. Bioorg Med Chem Lett. 2006 Jan 1;16(1):129-33.
REF 6	Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-linea... J Med Chem. 2008 Sep 25;51(18):5680-9.
REF 7	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 8	Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
REF 9	A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32.
REF 10	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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