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Vascular Endothelial Growth Factor Receptor-2

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Definition: A 200-230-kDa tyrosine kinase receptor for vascular endothelial growth factors found primarily in endothelial and hematopoietic cells and their precursors. VEGFR-2 is important for vascular and hematopoietic development, and mediates almost all endothelial cell responses to VEGF.      Other names Vascular Endothelial Growth Factor Receptor 2; VEGF Receptor Flk 1; Tyrosine Kinase, KDR; KDR, VEGF Receptor; Flk-1, VEGF Receptor; Flk 1 Receptor Tyrosine Kinase; Flk 1 Protein; Fetal Liver Kinase 1; VEGF Receptor KDR; VEGF Receptor Flk-1; Kinase Insert Domain Receptor; KDR Tyrosine Kinase; Flk-1 Receptor Tyrosine Kinase; Flk-1 Protein; Fetal Liver Kinase-1; VEGFR-2
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
XL647  0   *Quinazolines *Azabicyclo Compounds Receptor, Epidermal Growth Factor/antagonists & inhibitors Receptor, erbB-2/antagonists & inhibitors Receptor, EphB4/antagonists & inhibitors Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. Clin Cancer Res. 2007 Jun 15;13(12):3713-23.
6-chloro-2-methoxy-N-(2-methoxybenzyl)acridin-9-amine  0   *Aminoacridines src-Family Kinases/antagonists & inhibitors Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. Bioorg Med Chem 2011 Jun 1;19(11):3312-9
GU 81 compound  0   *Peptides Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. BMC Cancer 2010;10:397
1-(2-fluoro-4-((5-methyl-5H-pyrrolo(3,2-d)pyrimidin-4-yl)oxy)phenyl)-3-(3-(trifluoromethyl)phenyl)urea  0   *Phenylurea Compounds *Bicyclo Compounds, Heterocyclic Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. Bioorg Med Chem 2010 Oct 15;18(20):7260-73
1-(2-chloro-4-((5-methyl-5H-pyrrolo(3,2-d)pyrimidin-4-yl)oxy)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea  0   *Phenylurea Compounds *Bicyclo Compounds, Heterocyclic Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors Receptor, Fibroblast Growth Factor, Type 1/antagonists & inhibitors. Bioorg Med Chem 2010 Oct 15;18(20):7150-63
boletopsin C  0   *Terphenyl Compounds Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Nat Prod. 2010 May 28;73(5):1002-4
3-(4-dimethylaminobenzylidene)-1,3-dihydroindol-2-one  0   *Indoles Vascular Endothelial Growth Factor Receptor-1/antagonists & inhibitors Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Cell Physiol 2010 Jul;224(1):262-72
N-(2-fluoro-4-((2-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)carbonylaminopyridin-4-yl)oxy)phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide  0   *Aminopyridines *Piperazines Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. Cancer Sci 2010 Jan;101(1):210-5
1-(4-(6-amino-5-(methoxyiminomethyl)pyrimidin-4-yloxy)-2-chlorophenyl)-3-ethylurea  0   *Oximes *Phenylurea Compounds Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. Angiogenesis 2009;12(3):287-96
4-((2-((4-chloro-3-(((1-methyl-2-pyrrolidinyl)methyl)oxy)phenyl)amino)-1,3-benzoxazol-5-yl)oxy)-N-methyl-2-pyridinecarboxamide  0   *Benzoxazoles *Pyridines Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2007 Sep 6;50(18):4351-73
N-cyclopropyl-2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5-ylmethyl)amino)benzamide  0   *Aminopyridines *Thiazoles Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2006 Jun 29;49(13):3766-9
brivanib alaninate  0   *Triazines Alanine/*analogs & derivatives Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2006 Apr 6;49(7):2143-6
2-methoxy-5-((6-methoxy-7-(2-methoxyethoxy)quinazolin-4-yl)amino)benzo-1,4-quinone  0   *Quinazolines *Benzoquinones Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2005 Dec 1;48(24):7560-81
N-(5-(6-(3-chlorophenylamino)pyrazin-2-yl)pyridin-3-yl)-N',N'-dimethylethane-1,2-diamine  0   *Aminopyridines *Pyrazines Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2005 Jul 28;48(15):4892-909
4-(5-(6-(3-chlorophenylamino)pyrazin-2-yl)pyridin-3-ylamino)butan-1-ol  0   *Aminopyridines *Pyrazines Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2005 Jul 28;48(15):4892-909
5-(6-(5-(difluoro(methylsulfonyl)methyl)-1,3,4-oxadiazol-2-yl)-5-isopropylpyrrolo(2,1-f)(1,2,4)triazin-4-ylamino)-2,4-difluoro-N-methoxybenzamide  0   *Oxadiazoles *Triazines Receptors, Fibroblast Growth Factor/antagonists & inhibitors Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2005 Jun 16;48(12):3991-4008
2,4-difluoro-5-(5-isopropyl-6-(5-(methylsulfonylmethyl)-1,3,4-oxadiazol-2-yl)pyrrolo(2,1-f)(1,2,4)triazin-4-ylamino)-N-methoxybenzamide  0   *Oxadiazoles *Triazines Receptors, Fibroblast Growth Factor/antagonists & inhibitors Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2005 Jun 16;48(12):3991-4008
5-(6-(5-(difluoromethyl)-1,3,4-oxadiazol-2-yl)-5-isopropylpyrrolo(2,1-f)(1,2,4)triazin-4-ylamino)-2,4-difluoro-N-methoxybenzamide  0   *Oxadiazoles *Triazines Receptors, Fibroblast Growth Factor/antagonists & inhibitors Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2005 Jun 16;48(12):3991-4008
3-((5-(6-((3-chlorophenyl)amino)pyrazinyl)-3-pyridinyl)amino)-1-propanol  0   *Pyrazines *Pyridines Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2005 Mar 24;48(6):1886-900
4-(benzothiazol-6-ylamino)-6-(benzyl-isopropyl-amino)-(1,3,5)triazin-2-ol  0   *Triazines *Benzothiazoles Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2005 Mar 24;48(6):1717-20
N-(2,4-difluorophenyl)-N'-(4-((6,7-dimethoxy-4-quinolyl)oxy)-2-fluorophenyl)urea  0   *Phenylurea Compounds *Quinolines Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Med Chem 2005 Mar 10;48(5):1359-66
SU 1498  0   *Cinnamates Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors. J Biol Chem 2004 Feb 13;279(7):5716-24
quail endothelial kinase 1  EC 2.7.1.-   *Receptors, Neurotransmitter *Vascular Endothelial Growth Factor Receptor-2. Mech Dev 1993 Jul;42(1-2):33-48

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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012
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