General Information of the Protein
Protein ID
PT00830
Protein Name
Procathepsin L
Secondarily
Protein Name
Cathepsin L1
Major excreted protein
Gene Name
CTSL
Secondarily
Gene Name
CTSL1
Sequence
MNPTLILAAFCLGIASATLTFDHSLEAQWTKWKAMHNRLYGMNEEGWRRAVWEKNMKMIELHNQEYREGKHSFTMAMNAFGDMTSEEFRQVMNGFQNRKPRKGKVFQEPLFYEAPRSVDWREKGYVTPVKNQGQCGSCWAFSATGALEGQMFRKTGRLISLSEQNLVDCSGPQGNEGCNGGLMDYAFQYVQDNGGLDSEESYPYEATEESCKYNPKYSVANDTGFVDIPKQEKALMKAVATVGPISVAIDAGHESFLFYKEGIYFEPDCSSEDMDHGVLVVGYGFESTESDNNKYWLVKNSWGEEWGMGGYVKMAKDRRNHCGIASAASYPTV
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Cysteine protease
>
Cysteine protease CA clan
>
Cysteine protease C1A family
Function
Thiol protease important for the overall degradation of proteins in lysosomes (Probable). Plays a critical for normal cellular functions such as general protein turnover, antigen processing and bone remodeling. Involved in the solubilization of cross-linked TG/thyroglobulin and in the subsequent release of thyroid hormone thyroxine (T4) by limited proteolysis of TG/thyroglobulin in the thyroid follicle lumen (By similarity). In neuroendocrine chromaffin cells secretory vesicles, catalyzes the prohormone proenkephalin processing to the active enkephalin peptide neurotransmitter (By similarity). In thymus, regulates CD4(+) T cell positive selection by generating the major histocompatibility complex class II (MHCII) bound peptide ligands presented by cortical thymic epithelial cells. Also mediates invariant chain processing in cortical thymic epithelial cells (By similarity). Major elastin-degrading enzyme at neutral pH. Accumulates as a mature and active enzyme in the extracellular space of antigen presenting cells (APCs) to regulate degradation of the extracellular matrix in the course of inflammation (By similarity). Secreted form generates endostatin from COL18A1 (PubMed:10716919). Critical for cardiac morphology and function. Plays an important role in hair follicle morphogenesis and cycling, as well as epidermal differentiation (By similarity). Required for maximal stimulation of steroidogenesis by TIMP1 (By similarity).
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Uniprot ID
Primary ID:
P07711

Secondarily ID:
Q6IAV1
Q96QJ0
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Ensembl ID
ENSG00000135047
HGNC ID
HGNC:2537
Subcellular Location
Lysosome
Apical cell membrane
Cytoplasmic vesicle
Secretory vesicle
Chromaffin granule
Secreted
Extracellular space
Secreted
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000063 , Hep-G2
Compound ID Compound Name Compound Formula
CP0060236
Balicatib
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C23H33N5O2
 1
1
IC50 = 48 nM
   TI
   LI
   LO
   TS
CP0146153
(2S)-N-(cyanomethyl)-3-cyclohexyl-2-(phenylformamido)propanamide
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C18H23N3O2
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0041940
(2R)-N-(cyanomethyl)-4-methyl-2-{3-[4-(piperazin-1-yl)phenyl]phenyl}pentanamide
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C24H30N4O
 1
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
CP0134851
N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
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C24H30N6O2S
 1
1
IC50 = 340 nM
   TI
   LI
   LO
   TS
CP0077258
N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-[2-(morpholin-4-yl)-1,3-thiazol-4-yl]benzamide
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C23H27N5O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0077259
N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(morpholin-4-yl)benzamide
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C20H26N4O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0057881
(2S)-N-(cyanomethyl)-4-methyl-2-{[(1S)-2,2,2-trifluoro-1-{4-[4-(piperazin-1-yl)phenyl]phenyl}ethyl]amino}pentanamide
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C26H32F3N5O
 1
1 IC50 = 47 nM
CP0146153
(2S)-N-(cyanomethyl)-3-cyclohexyl-2-(phenylformamido)propanamide
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C18H23N3O2
 1
1 IC50 = 55 nM
CP0059345
(2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfon
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C23H26F3N3O3S
 1
1 IC50 = 264 nM
CP0060236
Balicatib
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C23H33N5O2
 4
1 IC50 = 503 nM
2 Ki = 503 nM
3 Ki = 3260 nM
4 Ki = 18000 nM
CP0041940
(2R)-N-(cyanomethyl)-4-methyl-2-{3-[4-(piperazin-1-yl)phenyl]phenyl}pentanamide
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C24H30N4O
 3
1 IC50 = 2600 nM
2 IC50 = 3725 nM
3 Ki = 4641 nM
CP0148723
(2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide
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C25H27F4N3O3S
 2
1 IC50 = 2995 nM
2 Ki = 1258.93 nM
CP0134851
N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
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C24H30N6O2S
 3
1 IC50 = 3903 nM
2 IC50 = 6300 nM
3 Ki = 6000 nM
CP0077258
N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-[2-(morpholin-4-yl)-1,3-thiazol-4-yl]benzamide
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C23H27N5O3S
 2
1 IC50 = 24000 nM
2 Ki = 74000 nM
CP0077259
N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(morpholin-4-yl)benzamide
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C20H26N4O3
 2
1 IC50 = 32000 nM
2 Ki = 50000 nM
CP0059908
(2S)-2-(1-benzofuran-2-ylformamido)-4-methyl-N-[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]pentanamide
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C27H32N4O6S
 1
1 Ki = 0.068 nM
Clinical Information about the Protein
Target 1 ( Cathepsin L (CTSL) )
Target Type Clinical trial Target
Disease 5 Target-related Diseases  5
1 Coronavirus infection [ICD-11: 1D92]
2 Abdominal aortic aneurysm [ICD-11: BD50.4]
3 Osteoarthritis [ICD-11: FA00-FA05]
4 Alzheimer disease [ICD-11: 8A20]
5 Asthma [ICD-11: CA23]
Investigative Drug(s) 1 Investigative Drug  1
1 L-873724 Investigative
Asthma
Patented Agent(s) 2 Patented Agents  2
1 PMID27998201-Compound-1 Patented
Coronavirus infection
2 PMID27998201-Compound-7 Patented
Abdominal aortic aneurysm
Preclinical Drug(s) 2 Preclinical Drugs  2
1 L-006235-1 Preclinical
Osteoarthritis
2 Z-Phe-Ala-diazomethylketone Preclinical
Alzheimer disease
Target 2 ( HUMAN cathepsin L (CTSL) )
Target Type Unknown Type Target
Disease 1 Target-related Disease  1
1 Severe acute respiratory syndrome (SARS) [ICD-11: 1D65]
Preclinical Drug(s) 1 Preclinical Drug  1
1 E-64D Preclinical
Severe acute respiratory syndrome (SARS)