Target Validation Information
TTD ID	T80782
Target Name	VEGFR1 messenger RNA (VEGFR1 mRNA)
Type of Target	Successful
Drug Potency against Target	(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-(1H-indazol-3-yl)-1H-benzo[d]imidazole	Drug Info	IC50 = 720 nM	[7]
	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	[2]
	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	[3]
	4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 15000 nM	[3]
	4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 14000 nM	[3]
	4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 6300 nM	[3]
	4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 11000 nM	[3]
	AAL-993	Drug Info	IC50 = 170 nM	[5]
	Brivanib	Drug Info	Ki = 60 nM	[6]
	CB-676475	Drug Info	IC50 = 14100 nM	[10]
	C[homoPhe-Hca-Glu-Gly-Leu-Glu-Glu]-NH2	Drug Info	IC50 = 19300 nM	[9]
	N-(2,4-Dichloro-benzoyl)-benzenesulfonamide	Drug Info	IC50 = 530 nM	[3]
	N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide	Drug Info	IC50 = 15000 nM	[3]
	N3-GHQMFYYPra-NH2	Drug Info	IC50 = 19400 nM	[8]
	Phenyl-(5-phenyl-oxazol-2-yl)-amine	Drug Info	IC50 = 3000 nM	[4]
	Romiplostim	Drug Info	IC50 = 8 nM	[1]
	VATALANIB	Drug Info	IC50 = 140 nM	[5]
	[3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol	Drug Info	IC50 = 1650 nM	[4]
References
REF 1	New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
REF 2	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 3	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 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	Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1913-9.
REF 6	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 7	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 8	On-resin cyclization of peptide ligands of the Vascular Endothelial Growth Factor Receptor 1 by copper(I)-catalyzed 1,3-dipolar azide-alkyne cycloa... Bioorg Med Chem Lett. 2007 Oct 15;17(20):5590-4.
REF 9	Rational design, structure, and biological evaluation of cyclic peptides mimicking the vascular endothelial growth factor. J Med Chem. 2007 Oct 18;50(21):5135-46.
REF 10	Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endo... Bioorg Med Chem. 2010 May 15;18(10):3575-87.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.