Target Validation Information
Target ID T96788
Target Name mRNA of HER2
Target Type
Clinical Trial
Drug Potency against Target BMS-536924 Drug Info IC50 = 17100 nM [1]
4-(4-isopropylphenyl)-5-cyano-2H-1,2,3-triazole Drug Info IC50 = 13500 nM [2]
4-(4-chlorophenyl)-5-cyano-2H-1,2,3-triazole Drug Info IC50 = 11000 nM [2]
4-(3-phenoxylphenyl)-5-cyano-2H-1,2,3-triazole Drug Info IC50 = 6600 nM [2]
AG-213 Drug Info IC50 = 5700 nM [3]
(1-Benzyl-1H-indol-5-yl)-quinazolin-4-yl-amine Drug Info IC50 = 1300 nM [4]
4-(Bis(2-chloroethyl)amino)-N-p-tolylbenzamide Drug Info IC50 = 1880 nM [5]
CL-387785 Drug Info IC50 = 17 nM [6]
17-allylamino-17-desmethoxy-geldanamycin Drug Info IC50 = 31 nM [7]
HKI-272 Drug Info IC50 = 59 nM [8]
N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide Drug Info IC50 = 2.2 nM [9]
4-(4-bromophenyl)-5-cyano-2H-1,2,3-triazole Drug Info IC50 = 7900 nM [2]
PD-168393 Drug Info IC50 = 5.7 nM [9]
References
REF 1J Med Chem. 2005 Sep 8;48(18):5639-43.Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
REF 2Bioorg Med Chem. 2007 Feb 1;15(3):1533-8. Epub 2006 Dec 15.Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1,2,3-triazoles as inhibitor of HER2 tyrosine kinase.
REF 3Eur J Med Chem. 2008 Jul;43(7):1478-88. Epub 2007 Sep 29.Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.
REF 4Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5.Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
REF 5Bioorg Med Chem. 2010 Jan 15;18(2):880-6. Epub 2009 Nov 22.Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumoragents.
REF 6J Med Chem. 2006 Feb 23;49(4):1475-85.Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
REF 7Bioorg Med Chem. 2009 Mar 15;17(6):2225-35. Epub 2008 Nov 6.Discovery and development of heat shock protein 90 inhibitors.
REF 8Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19936-41. Epub 2007 Dec 6.Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
REF 9J Med Chem. 1999 May 20;42(10):1803-15.Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding siteof the epidermal growth factor receptor.

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