Target Validation Information
Target ID T41141
Target Name Cathepsin L
Target Type
Clinical Trial
Drug Potency against Target Bis(3-Fluorophenyl)-ketone]thiosemicarbazone Drug Info IC50 = 4870 nM [1]
MDL-2170 Drug Info IC50 = 1270 nM [2]
1-(phenyl(p-tolyl)methylene)thiosemicarbazide Drug Info IC50 = 1020 nM [3]
L-006235-1 Drug Info IC50 = 340 nM [4]
(S)-tert-butyl 1-oxohexan-2-ylcarbamate Drug Info IC50 = 8900 nM [5]
9-benzyl-6-(benzylamino)-9H-purine-2-carbonitrile Drug Info IC50 = 12220 nM [6]
BOCEPREVIR Drug Info IC50 = 760 nM [7]
N-acetyl-phenylalanyl-glycine-nitrile Drug Info Ki = 5800 nM [8]
Bis(3-bromophenyl)(5-hydroxy)thiosemicarbazone Drug Info IC50 = 232.4 nM [9]
[(3-Bromophenyl)-m-tolyl-ketone]thiosemicarbazone Drug Info IC50 = 224 nM [1]
6-(benzylamino)-9-butyl-9H-purine-2-carbonitrile Drug Info IC50 = 4380 nM [6]
N-(tert-butoxycarbonyl)-leucyl-glycine-nitrile Drug Info Ki = 1200 nM [8]
N-(tert-butoxycarbonyl)-isoleucyl-glycine-nitrile Drug Info Ki = 4900 nM [8]
N-(tert-butoxycarbonyl)-norleucyl-glycine-nitrile Drug Info Ki = 19000 nM [8]
N-(tert-butoxycarbonyl)-valyl-glycine-nitrile Drug Info Ki = 2800 nM [8]
N-(tert-butoxycarbonyl)-tyrosyl-glycine-nitrile Drug Info Ki = 400 nM [8]
1-(1,3-diphenylpropylidene)thiosemicarbazide Drug Info IC50 = 910 nM [3]
N-(4-phenylbenzoyl)-phenylalanyl-glycine-nitrile Drug Info Ki = 550 nM [8]
N-(tert-butoxycarbonyl)-methionyl-glycine-nitrile Drug Info Ki = 19000 nM [8]
Bis(3-bromophenyl)(4-hydroxy)thiosemicarbazone Drug Info IC50 = 126.1 nM [9]
N-benzoyl-phenylalanyl-glycine-nitrile Drug Info Ki = 230 nM [8]
[(3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone Drug Info IC50 = 2160 nM [1]
N-(benzyloxycarbonyl)-leucyl-glycine-nitrile Drug Info Ki = 750 nM [8]
[2-Phenylacetophenone]thiosemicarbazone Drug Info IC50 = 5410 nM [9]
(3-Bromobenzoylpyridine)thiosemicarbazone Drug Info IC50 = 1000 nM [9]
(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate Drug Info IC50 = 2000 nM [5]
L-873724 Drug Info IC50 = 90 nM [10]
References
REF 1Bioorg Med Chem Lett. 2010 Feb 15;20(4):1415-9. Epub 2010 Jan 6.Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.
REF 2J Med Chem. 2009 May 14;52(9):3093-7.Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
REF 3Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. Epub 2008 Apr 8.Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
REF 4J Med Chem. 2005 Dec 1;48(24):7535-43.Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.
REF 5Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15.Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?.
REF 6J Med Chem. 2008 Feb 14;51(3):545-52. Epub 2008 Jan 4.Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.
REF 7Antimicrob Agents Chemother. 2010 Jan;54(1):305-11. Epub 2009 Oct 19.MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
REF 8J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
REF 9Bioorg Med Chem Lett. 2010 Nov 15;20(22):6610-5. Epub 2010 Sep 15.Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.
REF 10Bioorg Med Chem Lett. 2007 Sep 1;17(17):4929-33. Epub 2007 Jun 10.The identification of potent, selective, and bioavailable cathepsin S inhibitors.

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