Target Validation Information
Target ID T57700
Target Name Mast/stem cell growth factor receptor
Target Type
Successful
Drug Potency against Target OSI-930 Drug Info IC50 = 8 nM [552727]
Sunitinib Drug Info Ki = 1~10 nM [552892]
4-(4-aminophenyl)-1H-indazol-3yl-amine Drug Info IC50 = 7360 nM [528716]
Imatinib Drug Info Ki = 100 nM
SEMAXINIB Drug Info IC50 = 400 nM [525812]
5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol Drug Info IC50 = 10 nM [527769]
Motesanib Drug Info Ki = 8 nM [552634]
PD-0173956 Drug Info IC50 = 290 nM [530497]
PD-0166326 Drug Info IC50 = 636 nM [530497]
9-Bromo-5,11-dimethyl-6H-pyrido[4,3-b]carbazole Drug Info IC50 = 200 nM [527769]
Bis-(5-hydroxy-1H-indol-2-yl)-methanone Drug Info IC50 = 500 nM [528209]
Nilotinib Drug Info Ki = 27 nM [552494]
9-Methoxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazole Drug Info IC50 = 300 nM [527769]
References
Ref 552727Molecular design and clinical development of VEGFR kinase inhibitors. Curr Top Med Chem. 2007;7(14):1379-93.
Ref 552892BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000. doi: 10.1038/nrd2658.
Ref 528716J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.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 receptor tyrosine kinase inhibitor.
Ref 525812J Med Chem. 2000 Jun 15;43(12):2310-23.New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.
Ref 527769J Med Chem. 2005 Oct 6;48(20):6194-201.Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
Ref 552634AMG 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 530497Bioorg Med Chem Lett. 2009 Dec 15;19(24):6872-6. Epub 2009 Oct 23.Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.
Ref 530497Bioorg Med Chem Lett. 2009 Dec 15;19(24):6872-6. Epub 2009 Oct 23.Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.
Ref 527769J Med Chem. 2005 Oct 6;48(20):6194-201.Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.
Ref 528209J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Ref 552494Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell. 2005 Feb;7(2):129-41.
Ref 527769J Med Chem. 2005 Oct 6;48(20):6194-201.Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases.

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