Target Validation Information
TTD ID	T61746
Target Name	Cathepsin B (CTSB)
Type of Target	Preclinical
Drug Potency against Target		Drug Info	IC50 = 1360 nM	[9]
	(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate	Drug Info	IC50 = 810 nM	[3]
	1-(phenyl(p-tolyl)methylene)thiosemicarbazide	Drug Info	IC50 = 13000 nM	[8]
	Ac-hPhe-Leu-Ala-LeuVSMe	Drug Info	IC50 = 1600 nM	[5]
	Ac-hPhe-Leu-Phe-LeuVSMe	Drug Info	IC50 = 850 nM	[5]
	Bis(3-bromophenyl)(4-hydroxy)thiosemicarbazone	Drug Info	IC50 = 9493 nM	[11]
	Cbz-Ile-Leu-Ala-LeuVSMe	Drug Info	IC50 = 5800 nM	[5]
	Cbz-Ile-t-ButylhomoGlu-Ala-LeuVSMe	Drug Info	IC50 = 18000 nM	[5]
	GNF-PF-5434	Drug Info	Ki = 64 nM	[7]
	Gold trichloride sodium chloride	Drug Info	Ki = 4200 nM	[2]
	L-006235-1	Drug Info	IC50 = 17 nM	[4]
	L-873724	Drug Info	IC50 = 925 nM	[6]
	PTosyl-Glu(OtBu)-Ala-LeuVSMe	Drug Info	IC50 = 13000 nM	[5]
	Z-Ala-Leu-lle-Agly-Ile-Val-NHBzl	Drug Info	Ki = 0.25 nM	[1]
	Z-Ala-Leu-lle-Agly-Ile-Val-OMe	Drug Info	Ki = 0.3 nM	[1]
	Z-Ala-Leu-Nal-Agly-Ile-Val-OMe	Drug Info	Ki = 1.58 nM	[1]
	Z-Ala-Leu-Phe-Agly-Ile-Val-OMe	Drug Info	Ki = 0.13 nM	[1]
	Z-Ala-Leu-Tyr(Me)-Agly-Ile-Val-OMe	Drug Info	Ki = 1.41 nM	[1]
	Z-Arg-Leu-Val-Agly-Ala-Gly-NH2	Drug Info	Ki = 7.29 nM	[1]
	Z-Arg-Leu-Val-Agly-Ile-Val-Trp-NH2	Drug Info	Ki = 13 nM	[1]
	Z-Arg-Leu-Val-Agly-Trp-Val-Ala-NH2	Drug Info	Ki = 43 nM	[1]
	Z-Arg-Leu-Val-Agly-Val-Ala-NH2	Drug Info	Ki = 0.12 nM	[1]
	Z-leu-Val-Agly-Val-OBzl	Drug Info	Ki = 40 nM	[1]
	[(3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone	Drug Info	IC50 = 5690 nM	[10]
References
REF 1	Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases. J Med Chem. 2002 Sep 12;45(19):4202-11.
REF 2	Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I). Bioorg Med Chem Lett. 2004 Oct 18;14(20):5113-6.
REF 3	Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83.
REF 4	Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional se... J Med Chem. 2005 Dec 1;48(24):7535-43.
REF 5	Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and c... J Med Chem. 2006 May 18;49(10):2953-68.
REF 6	The identification of potent, selective, and bioavailable cathepsin S inhibitors. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33.
REF 7	Substrate optimization for monitoring cathepsin C activity in live cells. Bioorg Med Chem. 2009 Feb 1;17(3):1064-70.
REF 8	Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB. Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5.
REF 9	Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity. J Med Chem. 2009 May 14;52(9):3093-7.
REF 10	Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1415-9.
REF 11	Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6610-5.

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