| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T89034 | ||||
| Target Name | Plasminogen | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | 1-guanidino-7-isoquinolinesulphonamide | Drug Info | Ki = 13000 nM | [528796] | |
| 1-guanidino-N-phenyl-7-isoquinolinesulphonamide | Drug Info | Ki = 3200 nM | [528796] | ||
| 2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine | Drug Info | Ki = 12000 nM | [526118] | ||
| N-(4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine | Drug Info | Ki = 7300 nM | [527081] | ||
| GRASSYSTATIN A | Drug Info | IC50 = 10000 nM | [530345] | ||
| MELAGATRAN | Drug Info | IC50 = 3060 nM | [528066] | ||
| References | |||||
| Ref 528796 | J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. | ||||
| Ref 528796 | J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. | ||||
| Ref 526118 | J 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. | ||||
| Ref 527081 | Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. | ||||
| Ref 530345 | J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. | ||||
| Ref 528066 | Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7. Epub 2006 Mar 6.Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. | ||||
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