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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