Target Validation Information
TTD ID	T40474
Target Name	Proto-oncogene c-Met (MET)
Type of Target	Successful
Drug Potency against Target	SGX523	Drug Info	IC50 = 35 nM	[2]
	TAK-701	Drug Info	IC50 = 70 nM	[5]
	Tivantinib	Drug Info	IC50 = 50 nM	[2]
	XL880	Drug Info	IC50 = 0.4 nM	[2]
	1-(2-nitrophenethyl)-1H-pyrrolo[3,2-b]pyridine	Drug Info	IC50 = 250 nM	[4]
	1-(phenylsulfonyl)-1H-pyrrolo[3,2-b]pyridine	Drug Info	IC50 = 3500 nM	[4]
	1-benzyl-1H-pyrrolo[3,2-b]pyridine	Drug Info	IC50 = 19 nM	[4]
	3-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine	Drug Info	IC50 = 1175 nM	[4]
	BMS-536924	Drug Info	IC50 = 4870 nM	[1]
	BMS-777607	Drug Info	IC50 = 20 nM	[3]
Action against Disease Model	MP470	Drug Info	MP470 had an IC50 of 2000 nM in the GIST-R cell line.	[6]
References
REF 1	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 2	Drug development of MET inhibitors: targeting oncogene addiction and expedience. Nat Rev Drug Discov. 2008 Jun;7(6):504-16.
REF 3	Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607... J Med Chem. 2009 Mar 12;52(5):1251-4.
REF 4	Discovery of 4-azaindoles as novel inhibitors of c-Met kinase. Bioorg Med Chem Lett. 2009 May 15;19(10):2780-4.
REF 5	Progress towards therapeutic small molecule MEK inhibitors for use in cancer therapy. Curr Top Med Chem. 2005;5(2):215-29.
REF 6	A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors. Oncogene. 2007 Jun 7;26(27):3909-19.

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