Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00348
Target NameProto-oncogene tyrosine-protein kinase receptor ret    
Type of TargetSuccessful target    
Drug Potency against TargetSorafenibIC50 = 20 nM[1]
SorafenibIC50 = 22 nM[2]
SorafenibIC50 = 28 nM[3]
SorafenibIC50 = 6 nM[4]
SorafenibIC50 = 6 nM[5]
SorafenibKi = 15 nM[6]
SorafenibKi = 5.9 nM[7]
VandetanibIC50 = 100 nM[2]
SU-5614IC50 = 1000 nM[8]
SU-4984IC50 = 1100 nM[8]
SU-11248IC50 = 1300 nM[8]
SU-9516IC50 = 1600 nM[8]
SEMAXINIBIC50 = 170 nM[8]
(E)-3-(4-hydroxybenzylidene)indolin-2-oneIC50 = 2300 nM[8]
(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-oneIC50 = 460 nM[8]
(Z)-5-Amino-3-(4-methoxybenzylidene)indolin-2-oneIC50 = 5300 nM[8]
SU-6656IC50 = 770 nM[8]
TG-100435Ki = 407 nM[9]
Ref 1Nat Biotechnol. 2005 Mar;23(3):329-36. Epub 2005 Feb 13.A small molecule-kinase interaction map for clinical kinase inhibitors. To Reference
Ref 2Nat Biotechnol. 2008 Jan;26(1):127-32.A quantitative analysis of kinase inhibitor selectivity. To Reference
Ref 3Expert Opin Investig Drugs. 2008 Jul;17(7):1013-28.Therapeutic potential of novel selective-spectrum kinase inhibitors in oncology. To Reference
Ref 4Curr Top Med Chem. 2006;6(11):1071-89.Recent advances in the research and development of RAF kinase inhibitors. To Reference
Ref 5Curr Top Med Chem. 2007;7(14):1364-78.Recent advances of MEK inhibitors and their clinical progress. To Reference
Ref 6Curr Opin Pharmacol. 2008 Aug;8(4):419-26. Epub 2008 Aug 3.Therapeutic strategies for inhibiting oncogenic BRAF signaling. To Reference
Ref 7J Biol Chem. 2007 Oct 5;282(40):29230-40. Epub 2007 Jul 30.Sorafenib functions to potently suppress RET tyrosine kinase activity by direct enzymatic inhibition and promoting RET lysosomal degradation independent of proteasomal targeting. To Reference
Ref 8Bioorg Med Chem. 2010 Feb 15;18(4):1482-96. Epub 2010 Jan 11.Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. To Reference
Ref 9Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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