Target General Infomation
Target ID
Former ID
Target Name
Cathepsin L
Gene Name
MEP; Major excreted protein; CTSL
Target Type
Clinical Trial
Disease Asthma [ICD10: J45]
Coagulation [ICD10: I80-I82]
Important for the overall degradation of proteins inlysosomes.
BioChemical Class
Target Validation
UniProt ID
EC Number
Drugs and Mode of Action
Drug(s) KGP94 Drug Info Clinical trial Coagulation [541661]
MDL-2170 Drug Info Terminated Discovery agent [545554]
Inhibitor (3-Bromobenzoylpyridine)thiosemicarbazone Drug Info [531200]
(S)-1-benzylcyclopentyl 1-oxohexan-2-ylcarbamate Drug Info [527872]
(S)-tert-butyl 1-oxohexan-2-ylcarbamate Drug Info [527872]
1-(1,3-diphenylpropylidene)thiosemicarbazide Drug Info [529432]
1-(phenyl(p-tolyl)methylene)thiosemicarbazide Drug Info [529432]
6-(benzylamino)-9-butyl-9H-purine-2-carbonitrile Drug Info [529240]
9-benzyl-6-(benzylamino)-9H-purine-2-carbonitrile Drug Info [529240]
Bis(3-bromophenyl)(4-hydroxy)thiosemicarbazone Drug Info [531200]
Bis(3-bromophenyl)(5-hydroxy)thiosemicarbazone Drug Info [531200]
Bis(3-Fluorophenyl)-ketone]thiosemicarbazone Drug Info [530644]
CAA0225 Drug Info [529990]
Cysteinesulfonic Acid Drug Info [551393]
KGP94 Drug Info [531200]
L-006235-1 Drug Info [527882]
L-873724 Drug Info [528921]
MDL-2170 Drug Info [530104]
N-(4-phenylbenzoyl)-phenylalanyl-glycine-nitrile Drug Info [527885]
N-(benzyloxycarbonyl)-leucyl-glycine-nitrile Drug Info [527885]
N-(tert-butoxycarbonyl)-isoleucyl-glycine-nitrile Drug Info [527885]
N-(tert-butoxycarbonyl)-leucyl-glycine-nitrile Drug Info [527885]
N-(tert-butoxycarbonyl)-methionyl-glycine-nitrile Drug Info [527885]
N-(tert-butoxycarbonyl)-norleucyl-glycine-nitrile Drug Info [527885]
N-(tert-butoxycarbonyl)-tyrosyl-glycine-nitrile Drug Info [527885]
N-(tert-butoxycarbonyl)-valyl-glycine-nitrile Drug Info [527885]
N-acetyl-phenylalanyl-glycine-nitrile Drug Info [527885]
N-benzoyl-phenylalanyl-glycine-nitrile Drug Info [527885]
[(3-Bromophenyl)-m-tolyl-ketone]thiosemicarbazone Drug Info [530644]
[(3-Bromophenyl)-p-tolyl-ketone]thiosemicarbazone Drug Info [530644]
[2-Phenylacetophenone]thiosemicarbazone Drug Info [531200]
KEGG Pathway Lysosome
Antigen processing and presentation
Proteoglycans in cancer
Rheumatoid arthritis
NetPath Pathway IL4 Signaling Pathway
TGF_beta_Receptor Signaling Pathway
Reactome Endosomal/Vacuolar pathway
Collagen degradation
Degradation of the extracellular matrix
Trafficking and processing of endosomal TLR
Assembly of collagen fibrils and other multimeric structures
MHC class II antigen presentation
WikiPathways Primary Focal Segmental Glomerulosclerosis FSGS
Ref 541661( Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6533).
Ref 545554Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003692)
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 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 527885J Med Chem. 2005 Dec 1;48(24):7688-707.Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
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.
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 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 529990Characterization of CAA0225, a novel inhibitor specific for cathepsin L, as a probe for autophagic proteolysis. Biol Pharm Bull. 2009 Mar;32(3):475-9.
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 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 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 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 1587926URL: The ChEMBL database in 2017

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