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 [530644]
MDL-2170 Drug Info IC50 = 1270 nM [530104]
1-(phenyl(p-tolyl)methylene)thiosemicarbazide Drug Info IC50 = 1020 nM [529432]
L-006235-1 Drug Info IC50 = 340 nM [527882]
(S)-tert-butyl 1-oxohexan-2-ylcarbamate Drug Info IC50 = 8900 nM [527872]
9-benzyl-6-(benzylamino)-9H-purine-2-carbonitrile Drug Info IC50 = 12220 nM [529240]
BOCEPREVIR Drug Info IC50 = 760 nM [530459]
N-acetyl-phenylalanyl-glycine-nitrile Drug Info Ki = 5800 nM [527885]
Bis(3-bromophenyl)(5-hydroxy)thiosemicarbazone Drug Info IC50 = 232.4 nM [531200]
[(3-Bromophenyl)-m-tolyl-ketone]thiosemicarbazone Drug Info IC50 = 224 nM [530644]
6-(benzylamino)-9-butyl-9H-purine-2-carbonitrile Drug Info IC50 = 4380 nM [529240]
N-(tert-butoxycarbonyl)-leucyl-glycine-nitrile Drug Info Ki = 1200 nM [527885]
N-(tert-butoxycarbonyl)-isoleucyl-glycine-nitrile Drug Info Ki = 4900 nM [527885]
N-(tert-butoxycarbonyl)-norleucyl-glycine-nitrile Drug Info Ki = 19000 nM [527885]
N-(tert-butoxycarbonyl)-valyl-glycine-nitrile Drug Info Ki = 2800 nM [527885]
N-(tert-butoxycarbonyl)-tyrosyl-glycine-nitrile Drug Info Ki = 400 nM [527885]
1-(1,3-diphenylpropylidene)thiosemicarbazide Drug Info IC50 = 910 nM [529432]
N-(4-phenylbenzoyl)-phenylalanyl-glycine-nitrile Drug Info Ki = 550 nM [527885]
N-(tert-butoxycarbonyl)-methionyl-glycine-nitrile Drug Info Ki = 19000 nM [527885]
Bis(3-bromophenyl)(4-hydroxy)thiosemicarbazone Drug Info IC50 = 126.1 nM [531200]
N-benzoyl-phenylalanyl-glycine-nitrile Drug Info Ki = 230 nM [527885]
[(3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone Drug Info IC50 = 2160 nM [530644]
N-(benzyloxycarbonyl)-leucyl-glycine-nitrile Drug Info Ki = 750 nM [527885]
[2-Phenylacetophenone]thiosemicarbazone Drug Info IC50 = 5410 nM [531200]
(3-Bromobenzoylpyridine)thiosemicarbazone Drug Info IC50 = 1000 nM [531200]
(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate Drug Info IC50 = 2000 nM [527872]
L-873724 Drug Info IC50 = 90 nM [528921]
References
Ref 530644Bioorg 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 530104J 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 529432Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. Epub 2008 Apr 8.Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
Ref 527882J 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 527872Bioorg 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 529240J 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 530459Antimicrob 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 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 531200Bioorg 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 530644Bioorg 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 529240J 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 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 529432Bioorg Med Chem Lett. 2008 May 1;18(9):2883-5. Epub 2008 Apr 8.Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
Ref 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 531200Bioorg 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 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 530644Bioorg 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 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Ref 531200Bioorg 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 531200Bioorg 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 527872Bioorg 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 528921Bioorg 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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