Therapeutic Targets Database
BIDD Pharmainformatics Databases


Target Validation Information
Target NameTissue-type plasminogen activator    
Type of TargetResearch target    
Drug Potency against TargetN-(5-Benzyloxy-isoquinolin-1-yl)-guanidineKi = 13000 nM[1]
N-(7-Benzyloxy-isoquinolin-1-yl)-guanidineKi = 13000 nM[1]
1-guanidino-N-phenyl-7-isoquinolinesulphonamideKi = 15000 nM[2]
N-(4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidineKi = 19000 nM[1]
BMS-344577Ki = 665 nM[3]
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidineKi = 9400 nM[4]
Ref 1Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. To Reference
Ref 2J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. To Reference
Ref 3Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. To Reference
Ref 4J Med Chem. 2001 Aug 16;44(17):2753-71.Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasminogen activator and factor Xa. To Reference


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