General Information of the Protein
Protein ID
PT00974
Protein Name
Cathepsin B
Secondarily
Protein Name
APP secretase
Cathepsin B1
Gene Name
CTSB
Secondarily
Gene Name
CPSB
Sequence
MWQLWASLCCLLVLANARSRPSFHPLSDELVNYVNKRNTTWQAGHNFYNVDMSYLKRLCGTFLGGPKPPQRVMFTEDLKLPASFDAREQWPQCPTIKEIRDQGSCGSCWAFGAVEAISDRICIHTNAHVSVEVSAEDLLTCCGSMCGDGCNGGYPAEAWNFWTRKGLVSGGLYESHVGCRPYSIPPCEHHVNGSRPPCTGEGDTPKCSKICEPGYSPTYKQDKHYGYNSYSVSNSEKDIMAEIYKNGPVEGAFSVYSDFLLYKSGVYQHVTGEMMGGHAIRILGWGVENGTPYWLVANSWNTDWGDNGFFKILRGQDHCGIESEVVAGIPRTDQYWEKI
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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 which is believed to participate in intracellular degradation and turnover of proteins (PubMed:12220505). Cleaves matrix extracellular phosphoglycoprotein MEPE (PubMed:12220505). Involved in the solubilization of cross-linked TG/thyroglobulin in the thyroid follicle lumen (By similarity). Has also been implicated in tumor invasion and metastasis (PubMed:3972105).
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Uniprot ID
Primary ID:
P07858

Secondarily ID:
B3KQR5
B3KRR5
Q503A6
Q96D87
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Ensembl ID
ENSG00000164733
HGNC ID
HGNC:2527
Subcellular Location
Lysosome
Melanosome
Secreted
Extracellular space
Apical cell membrane
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: CL000011 , CHO
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0034074
 Compound Info 
N-[(2S)-1-[(3-fluoro-2-oxopropyl)amino]-1-oxo-3-phenylpropan-2-yl]naphthalene-1-carboxamide
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C23H21FN2O3
  1
1
IC50 = 200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0030570
 Compound Info 
benzyl N-[(2S)-1-[[(2S)-4-fluoro-3-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate
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C21H23FN2O4
  1
1
IC50 = 300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0024522
 Compound Info 
N-[(2S)-1-[(3-fluoro-2-oxopropyl)amino]-1-oxo-3-phenylpropan-2-yl]benzamide
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C19H19FN2O3
  1
1
IC50 = 700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000063 , Hep-G2
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0249137
 Compound Info 
(2S)-1-[(2S,3S)-3-methyl-2-{[(2S,3S)-3-(propylcarbamoyl)oxiran-2-yl]formamido}pentanoyl]pyrrolidine-2-carboxylic acid
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C18H29N3O6
  2
1 IC50 = 2.24 nM
2 IC50 = 3.7 nM
CP0255533
 Compound Info 
(S)-N-((S)-1-cyano-2-(4-cyano-2-fluorophenyl)ethyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
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C31H29F5N4O3S
  1
1 IC50 = 9 nM
CP0105431
 Compound Info 
(S)-N-((S)-1-cyano-2-(4-cyano-2-fluorophenyl)ethyl)-2-((S)-1-(4'-((R)-2,2-difluoro-1-hydroxyethyl)biphenyl-4-yl)-2,2,2-trifluoroethylamino)-3-methylbutanamide
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C31H28F6N4O2
  1
1 IC50 = 87 nM
CP0076419
 Compound Info 
(S)-4-methyl-2-[(S)-2,2,2-trifluoro-1-(4'-methanesulfonyl-biphenyl-4-yl)-ethylamino]-pentanoic acid ((S)-benzyl-cyano-methyl)-amide
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C30H32F3N3O3S
  1
1 IC50 = 953 nM
CP0148723
 Compound Info 
(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 = 1034 nM
2 IC50 < 2000 nM
CP0134851
 Compound Info 
N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
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C24H30N6O2S
  3
1 IC50 = 1050 nM
2 IC50 = 1100 nM
3 Ki = 1000 nM
CP0057881
 Compound Info 
(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 = 1111 nM
CP0041940
 Compound Info 
(2R)-N-(cyanomethyl)-4-methyl-2-{3-[4-(piperazin-1-yl)phenyl]phenyl}pentanamide
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C24H30N4O
  3
1 IC50 = 3950 nM
2 IC50 = 86000 nM
3 Ki = 3843 nM
CP0077258
 Compound Info 
N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-[2-(morpholin-4-yl)-1,3-thiazol-4-yl]benzamide
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C23H27N5O3S
  2
1 IC50 = 4200 nM
2 Ki = 3100 nM
CP0060236
 Compound Info 
Balicatib
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C23H33N5O2
  4
1 IC50 = 4750 nM
2 IC50 = 4800 nM
3 Ki = 2900 nM
4 Ki = 3800 nM
CP0059345
 Compound Info 
(2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfon
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C23H26F3N3O3S
  1
1 IC50 = 5239 nM
CP0219229
 Compound Info 
(E)-1-(2,4-dihydroxyphenyl)-3-(4-hydroxynaphthalen-1-yl)prop-2-en-1-one
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C19H14O4
  2
1 IC50 = 6340 nM
2 Ki = 10610 nM
CP0176887
 Compound Info 
(2E,4E)-5-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)penta-2,4-dien-1-one
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C18H16O4
  2
1 IC50 = 11050 nM
2 Ki = 4740 nM
CP0077259
 Compound Info 
N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(morpholin-4-yl)benzamide
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C20H26N4O3
  2
1 IC50 = 15400 nM
2 Ki = 8600 nM
CP0146153
 Compound Info 
(2S)-N-(cyanomethyl)-3-cyclohexyl-2-(phenylformamido)propanamide
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C18H23N3O2
  1
1 IC50 = 19000 nM
CP0059908
 Compound Info 
(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 = 13 nM
Clinical Information about the Protein
Target 1 ( Cathepsin B (CTSB) )
Target Type Preclinical Target
Disease 5 Target-related Diseases  5
1 Neurodegenerative disorder [ICD-11: 8A20-8A23]
2 Cardiac arrest [ICD-11: MC82]
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
 Drug Info 
Investigative
Asthma
Patented Agent(s) 1 Patented Agent  1
1 PMID27998201-Compound-22
 Drug Info 
Patented
Neurodegenerative disorder
Preclinical Drug(s) 3 Preclinical Drugs  3
1 CA-074Me
 Drug Info 
Preclinical
Cardiac arrest
2 L-006235-1
 Drug Info 
Preclinical
Osteoarthritis
3 Z-Phe-Ala-diazomethylketone
 Drug Info 
Preclinical
Alzheimer disease