Target Validation Information
TTD ID	T96788
Target Name	ERBB2 messenger RNA (HER2 mRNA)
Type of Target	Clinical trial
Drug Potency against Target		Drug Info	IC50 = 31 nM	[8]
	(1-Benzyl-1H-indol-5-yl)-quinazolin-4-yl-amine	Drug Info	IC50 = 1300 nM	[2]
	4-(3-phenoxylphenyl)-5-cyano-2H-1,2,3-triazole	Drug Info	IC50 = 6600 nM	[5]
	4-(4-bromophenyl)-5-cyano-2H-1,2,3-triazole	Drug Info	IC50 = 7900 nM	[5]
	4-(4-chlorophenyl)-5-cyano-2H-1,2,3-triazole	Drug Info	IC50 = 11000 nM	[5]
	4-(4-isopropylphenyl)-5-cyano-2H-1,2,3-triazole	Drug Info	IC50 = 13500 nM	[5]
	4-(Bis(2-chloroethyl)amino)-N-p-tolylbenzamide	Drug Info	IC50 = 1880 nM	[9]
	AG-213	Drug Info	IC50 = 5700 nM	[6]
	BMS-536924	Drug Info	IC50 = 17100 nM	[3]
	CL-387785	Drug Info	IC50 = 17 nM	[4]
	HKI-272	Drug Info	IC50 = 59 nM	[7]
	N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide	Drug Info	IC50 = 2.2 nM	[1]
	PD-168393	Drug Info	IC50 = 5.7 nM	[1]
References
REF 1	Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP... J Med Chem. 1999 May 20;42(10):1803-15.
REF 2	Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2. Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5.
REF 3	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 antitum... J Med Chem. 2005 Sep 8;48(18):5639-43.
REF 4	Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB... J Med Chem. 2006 Feb 23;49(4):1475-85.
REF 5	Synthesis and biological evaluation of 4-aryl-5-cyano-2H-1,2,3-triazoles as inhibitor of HER2 tyrosine kinase. Bioorg Med Chem. 2007 Feb 1;15(3):1533-8.
REF 6	Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors. Eur J Med Chem. 2008 Jul;43(7):1478-88.
REF 7	Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19936-41.
REF 8	Discovery and development of heat shock protein 90 inhibitors. Bioorg Med Chem. 2009 Mar 15;17(6):2225-35.
REF 9	Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents. Bioorg Med Chem. 2010 Jan 15;18(2):880-6.

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