Target Validation Information
TTD ID	T41141
Target Name	Cathepsin L (CTSL)
Type of Target	Clinical trial
Drug Potency against Target		Drug Info	IC50 = 1270 nM	[7]
	(3-Bromobenzoylpyridine)thiosemicarbazone	Drug Info	IC50 = 1000 nM	[10]
	(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate	Drug Info	IC50 = 2000 nM	[1]
	(S)-tert-butyl 1-oxohexan-2-ylcarbamate	Drug Info	IC50 = 8900 nM	[1]
	1-(1,3-diphenylpropylidene)thiosemicarbazide	Drug Info	IC50 = 910 nM	[6]
	1-(phenyl(p-tolyl)methylene)thiosemicarbazide	Drug Info	IC50 = 1020 nM	[6]
	6-(benzylamino)-9-butyl-9H-purine-2-carbonitrile	Drug Info	IC50 = 4380 nM	[5]
	9-benzyl-6-(benzylamino)-9H-purine-2-carbonitrile	Drug Info	IC50 = 12220 nM	[5]
	Bis(3-bromophenyl)(4-hydroxy)thiosemicarbazone	Drug Info	IC50 = 126.1 nM	[10]
	Bis(3-bromophenyl)(5-hydroxy)thiosemicarbazone	Drug Info	IC50 = 232.4 nM	[10]
	Bis(3-Fluorophenyl)-ketone]thiosemicarbazone	Drug Info	IC50 = 4870 nM	[9]
	BOCEPREVIR	Drug Info	IC50 = 760 nM	[8]
	L-006235-1	Drug Info	IC50 = 340 nM	[2]
	L-873724	Drug Info	IC50 = 90 nM	[4]
	N-(4-phenylbenzoyl)-phenylalanyl-glycine-nitrile	Drug Info	Ki = 550 nM	[3]
	N-(benzyloxycarbonyl)-leucyl-glycine-nitrile	Drug Info	Ki = 750 nM	[3]
	N-(tert-butoxycarbonyl)-isoleucyl-glycine-nitrile	Drug Info	Ki = 4900 nM	[3]
	N-(tert-butoxycarbonyl)-leucyl-glycine-nitrile	Drug Info	Ki = 1200 nM	[3]
	N-(tert-butoxycarbonyl)-methionyl-glycine-nitrile	Drug Info	Ki = 19000 nM	[3]
	N-(tert-butoxycarbonyl)-norleucyl-glycine-nitrile	Drug Info	Ki = 19000 nM	[3]
	N-(tert-butoxycarbonyl)-tyrosyl-glycine-nitrile	Drug Info	Ki = 400 nM	[3]
	N-(tert-butoxycarbonyl)-valyl-glycine-nitrile	Drug Info	Ki = 2800 nM	[3]
	N-acetyl-phenylalanyl-glycine-nitrile	Drug Info	Ki = 5800 nM	[3]
	N-benzoyl-phenylalanyl-glycine-nitrile	Drug Info	Ki = 230 nM	[3]
	[(3-Bromophenyl)-m-tolyl-ketone]thiosemicarbazone	Drug Info	IC50 = 224 nM	[9]
	[(3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone	Drug Info	IC50 = 2160 nM	[9]
	[2-Phenylacetophenone]thiosemicarbazone	Drug Info	IC50 = 5410 nM	[10]
References
REF 1	Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83.
REF 2	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 3	Interaction of papain-like cysteine proteases with dipeptide-derived nitriles. J Med Chem. 2005 Dec 1;48(24):7688-707.
REF 4	The identification of potent, selective, and bioavailable cathepsin S inhibitors. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33.
REF 5	Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB. J Med Chem. 2008 Feb 14;51(3):545-52.
REF 6	Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB. Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5.
REF 7	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 8	MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. Antimicrob Agents Chemother. 2010 Jan;54(1):305-11.
REF 9	Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1415-9.
REF 10	Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6610-5.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.