Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T45299 | ||||
Target Name | Tissue-type plasminogen activator (PLAT) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | 1-guanidino-N-phenyl-7-isoquinolinesulphonamide | Drug Info | Ki = 15000 nM | [3] | |
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine | Drug Info | Ki = 9400 nM | [1] | ||
BMS-344577 | Drug Info | Ki = 665 nM | [4] | ||
N-(4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine | Drug Info | Ki = 19000 nM | [2] | ||
N-(5-Benzyloxy-isoquinolin-1-yl)-guanidine | Drug Info | Ki = 13000 nM | [2] | ||
N-(7-Benzyloxy-isoquinolin-1-yl)-guanidine | Drug Info | Ki = 13000 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 | Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. J Med Chem. 2007 May 17;50(10):2341-51. | ||||
REF 4 | Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. | ||||
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