Target Validation Information
Target ID T45299
Target Name Tissue-type plasminogen activator
Target Type
Research
Drug Potency against Target N-(7-Benzyloxy-isoquinolin-1-yl)-guanidine Drug Info Ki = 13000 nM [527081]
N-(5-Benzyloxy-isoquinolin-1-yl)-guanidine Drug Info Ki = 13000 nM [527081]
BMS-344577 Drug Info Ki = 665 nM [530503]
1-guanidino-N-phenyl-7-isoquinolinesulphonamide Drug Info Ki = 15000 nM [528796]
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine Drug Info Ki = 9400 nM [526118]
N-(4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine Drug Info Ki = 19000 nM [527081]
References
Ref 527081Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
Ref 527081Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
Ref 530503Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. Epub 2009 Oct 23.Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.
Ref 528796J 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 526118J 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 527081Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.

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