Target Validation Information
TTD ID T89034
Target Name Plasminogen (PLG)
Type of Target
Successful
Drug Potency against Target 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]
Grassystatin a Drug Info IC50 = 10000 nM [5]
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.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.