Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T98022 | ||||
Target Name | Carboxypeptidase B2 (CPB2) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | (+/-)-5-amino-2-(mercaptomethyl)pentanoic acid | Drug Info | Ki = 300 nM | [3] | |
2-(3-aminophenyl)-3-mercaptopropanoic acid | Drug Info | IC50 = 785 nM | [2] | ||
2-(3-guanidinophenyl)-3-mercaptopropanoic acid | Drug Info | IC50 = 1720 nM | [2] | ||
2-(4-benzoylpiperidine-1-carbonyl)benzoic acid | Drug Info | Ki = 19600 nM | [4] | ||
3-mercapto-2-(piperidin-3-yl)propanoic acid | Drug Info | IC50 = 19000 nM | [2] | ||
3-mercapto-2-(piperidin-4-yl)propanoic acid | Drug Info | IC50 = 195 nM | [2] | ||
6-Amino-2-(1H-imidazol-4-yl)-hexanoic acid | Drug Info | IC50 = 3700 nM | [1] | ||
DL-benzylsuccinic acid | Drug Info | Ki = 11900 nM | [4] | ||
DL-guanidinoethylmercaptosuccinic acid | Drug Info | Ki = 1100 nM | [4] | ||
SQ-24798 | Drug Info | IC50 = 10 nM | [2] | ||
UK-396082 | Drug Info | Ki = 206 nM | [5] | ||
Action against Disease Model | AZD-9684 | Drug Info | Latexin, a carboxypeptidase U inhibitor, is expressed in rat peritoneal mast cells and is associated with granular structures distinct from secretory granules and lysosomes. | [6] | |
References | |||||
REF 1 | Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group. Bioorg Med Chem Lett. 2004 May 3;14(9):2141-5. | ||||
REF 2 | 3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa). Bioorg Med Chem Lett. 2007 Mar 1;17(5):1349-54. | ||||
REF 3 | Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis. J Med Chem. 2007 Nov 29;50(24):6095-103. | ||||
REF 4 | A new type of five-membered heterocyclic inhibitors of basic metallocarboxypeptidases. Eur J Med Chem. 2009 Aug;44(8):3266-71. | ||||
REF 5 | Oxygenated analogues of UK-396082 as inhibitors of activated thrombin activatable fibrinolysis inhibitor. Bioorg Med Chem Lett. 2010 Jan 1;20(1):92-6. | ||||
REF 6 | Latexin, a carboxypeptidase A inhibitor, is expressed in rat peritoneal mast cells and is associated with granular structures distinct from secretory granules and lysosomes. Biochem J. 2000 Mar 15;346 Pt 3:817-26. | ||||
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