Target Validation Information
TTD ID	T89034
Target Name	Plasminogen (PLG)
Type of Target	Successful
Drug Potency against Target		Drug Info	IC50 = 10000 nM	[5]
	1-guanidino-7-isoquinolinesulphonamide	Drug Info	Ki = 13000 nM	[4]
	1-guanidino-N-phenyl-7-isoquinolinesulphonamide	Drug Info	Ki = 3200 nM	[4]
	2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine	Drug Info	Ki = 12000 nM	[1]
	MELAGATRAN	Drug Info	IC50 = 3060 nM	[3]
	N-(4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine	Drug Info	Ki = 7300 nM	[2]
References
REF 1	Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasmi... J Med Chem. 2001 Aug 16;44(17):2753-71.
REF 2	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.
REF 3	Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
REF 4	Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. J Med Chem. 2007 May 17;50(10):2341-51.
REF 5	Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.

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