| 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 552725 | Sorafenib 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 528527 | Bioorg 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 530673 | Bioorg 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 530673 | Bioorg 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 530673 | Bioorg 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 530673 | Bioorg 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 552773 | A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. doi: 10.1038/nbt1358. | ||||
| Ref 530673 | Bioorg 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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