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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