Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T60631 | ||||
Target Name | Proto-oncogene c-Ret (RET) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Drug Info | Ki = 5.9 nM | [3] | ||
Vandetanib | Drug Info | IC50 = 100 nM | [4] | ||
Drug Info | IC50 = 5300 nM | [2] | |||
Drug Info | IC50 = 2300 nM | [2] | |||
(Z)-3-((1H-pyrrol-2-yl)methylene)indolin-2-one | Drug Info | IC50 = 460 nM | [2] | ||
Romiplostim | Drug Info | IC50 = 170 nM | [2] | ||
Sunitinib | Drug Info | IC50 = 1300 nM | [2] | ||
TG-100435 | Drug Info | Ki = 407 nM | [1] | ||
References | |||||
REF 1 | 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 kinas... Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. | ||||
REF 2 | Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. Bioorg Med Chem. 2010 Feb 15;18(4):1482-96. | ||||
REF 3 | Sorafenib functions to potently suppress RET tyrosine kinase activity by direct enzymatic inhibition and promoting RET lysosomal degradation indepe... J Biol Chem. 2007 Oct 5;282(40):29230-40. | ||||
REF 4 | A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol. 2008 Jan;26(1):127-32. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.