Target
Validation Information |
TTD ID | TTDS00348 |
Target Name | Proto-oncogene tyrosine-protein kinase receptor ret |
Type of Target | Successful target |
Drug Potency against Target | Sorafenib |  | IC50 = 20 nM | [1] |
Sorafenib |  | IC50 = 22 nM | [2] |
Sorafenib |  | IC50 = 28 nM | [3] |
Sorafenib |  | IC50 = 6 nM | [4] |
Sorafenib |  | IC50 = 6 nM | [5] |
Sorafenib |  | Ki = 15 nM | [6] |
Sorafenib |  | Ki = 5.9 nM | [7] |
Vandetanib |  | IC50 = 100 nM | [2] |
SU-5614 |  | IC50 = 1000 nM | [8] |
SU-4984 |  | IC50 = 1100 nM | [8] |
SU-11248 |  | IC50 = 1300 nM | [8] |
SU-9516 |  | IC50 = 1600 nM | [8] |
SEMAXINIB |  | IC50 = 170 nM | [8] |
(E)-3-(4-hydroxybenzylidene)indolin-2-one |  | IC50 = 2300 nM | [8] |
(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one |  | IC50 = 460 nM | [8] |
(Z)-5-Amino-3-(4-methoxybenzylidene)indolin-2-one |  | IC50 = 5300 nM | [8] |
SU-6656 |  | IC50 = 770 nM | [8] |
TG-100435 |  | Ki = 407 nM | [9] |
Ref 1 | Nat Biotechnol. 2005 Mar;23(3):329-36. Epub 2005 Feb 13.A small molecule-kinase interaction map for clinical kinase inhibitors. To Reference |
Ref 2 | Nat Biotechnol. 2008 Jan;26(1):127-32.A quantitative analysis of kinase inhibitor selectivity. To Reference |
Ref 3 | Expert Opin Investig Drugs. 2008 Jul;17(7):1013-28.Therapeutic potential of novel selective-spectrum kinase inhibitors in oncology. To Reference |
Ref 4 | Curr Top Med Chem. 2006;6(11):1071-89.Recent advances in the research and development of RAF kinase inhibitors. To Reference |
Ref 5 | Curr Top Med Chem. 2007;7(14):1364-78.Recent advances of MEK inhibitors and their clinical progress. To Reference |
Ref 6 | Curr Opin Pharmacol. 2008 Aug;8(4):419-26. Epub 2008 Aug 3.Therapeutic strategies for inhibiting oncogenic BRAF signaling. To Reference |
Ref 7 | J 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 8 | 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. To Reference |
Ref 9 | 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. To Reference |