Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDR01233
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



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

 
   
           
 
Computer-aided Drug Design
About BIDD | Databases | Software | Teaching | Research |  Links

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543