Target Validation Information
TTD ID T57700
Target Name Tyrosine-protein kinase Kit (KIT)
Type of Target
Drug Potency against Target Imatinib Drug Info Ki = 100 nM
Sunitinib Drug Info Ki = 1~10 nM [9]
Motesanib Drug Info Ki = 8 nM [7]
Nilotinib Drug Info Ki = 27 nM [6]
OSI-930 Drug Info IC50 = 8 nM [8]
4-(4-aminophenyl)-1H-indazol-3yl-amine Drug Info IC50 = 7360 nM [4]
5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol Drug Info IC50 = 10 nM [2]
9-Bromo-5,11-dimethyl-6H-pyrido[4,3-b]carbazole Drug Info IC50 = 200 nM [2]
9-Methoxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazole Drug Info IC50 = 300 nM [2]
Bis-(5-hydroxy-1H-indol-2-yl)-methanone Drug Info IC50 = 500 nM [3]
PD-0166326 Drug Info IC50 = 636 nM [5]
PD-0173956 Drug Info IC50 = 290 nM [5]
Romiplostim Drug Info IC50 = 400 nM [1]
REF 1 New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven a... J Med Chem. 2000 Jun 15;43(12):2310-23.
REF 2 Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases. J Med Chem. 2005 Oct 6;48(20):6194-201.
REF 3 Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2006 Jun 1;49(11):3101-15.
REF 4 Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted ... J Med Chem. 2007 Apr 5;50(7):1584-97.
REF 5 Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6872-6.
REF 6 Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell. 2005 Feb;7(2):129-41.
REF 7 AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res. 2006 Sep 1;66(17):8715-21.
REF 8 Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
REF 9 BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000.

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