Target Validation Information
Target ID T60631
Target Name Proto-oncogene tyrosine-protein kinase receptor ret
Target Type
Successful
Drug Potency against Target Sorafenib Drug Info Ki = 5.9 nM [552725]
TG-100435 Drug Info Ki = 407 nM [528527]
Sunitinib Drug Info IC50 = 1300 nM [530673]
(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one Drug Info IC50 = 460 nM [530673]
(Z)-5-Amino-3-(4-methoxybenzylidene)indolin-2-one Drug Info IC50 = 5300 nM [530673]
(E)-3-(4-hydroxybenzylidene)indolin-2-one Drug Info IC50 = 2300 nM [530673]
Vandetanib Drug Info IC50 = 100 nM [552773]
SEMAXINIB Drug Info IC50 = 170 nM [530673]
References
Ref 552725Sorafenib functions to potently suppress RET tyrosine kinase activity by direct enzymatic inhibition and promoting RET lysosomal degradation independent of proteasomal targeting. J Biol Chem. 2007 Oct 5;282(40):29230-40. Epub 2007 Jul 30.
Ref 528527Bioorg 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.
Ref 530673Bioorg 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.
Ref 530673Bioorg 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.
Ref 530673Bioorg 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.
Ref 530673Bioorg 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.
Ref 552773A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358.
Ref 530673Bioorg 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.

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