General Information of the Protein
Protein ID
PT00824
Protein Name
Cathepsin K
Secondarily
Protein Name
Cathepsin O
Cathepsin O2
Cathepsin X
Gene Name
CTSK
Secondarily
Gene Name
CTSO
CTSO2
Sequence
MWGLKVLLLPVVSFALYPEEILDTHWELWKKTHRKQYNNKVDEISRRLIWEKNLKYISIHNLEASLGVHTYELAMNHLGDMTSEEVVQKMTGLKVPLSHSRSNDTLYIPEWEGRAPDSVDYRKKGYVTPVKNQGQCGSCWAFSSVGALEGQLKKKTGKLLNLSPQNLVDCVSENDGCGGGYMTNAFQYVQKNRGIDSEDAYPYVGQEESCMYNPTGKAAKCRGYREIPEGNEKALKRAVARVGPVSVAIDASLTSFQFYSKGVYYDESCNSDNLNHAVLAVGYGIQKGNKHWIIKNSWGENWGNKGYILMARNKNNACGIANLASFPKM
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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 involved in osteoclastic bone resorption and may participate partially in the disorder of bone remodeling. Displays potent endoprotease activity against fibrinogen at acid pH. May play an important role in extracellular matrix degradation. Involved in the release of thyroid hormone thyroxine (T4) by limited proteolysis of TG/thyroglobulin in the thyroid follicle lumen (PubMed:11082042).
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Uniprot ID
Primary ID:
P43235

Secondarily ID:
Q6FHS6
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HGNC ID
HGNC:2536
Subcellular Location
Lysosome
Secreted
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: CL000003 , Ramos
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0091658
 Compound Info 
(S)-N-((S)-1-cyano-2-(4-cyano-2-fluorophenyl)ethyl)-3-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)butanamide
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C30H28F4N4O3S
  1
1
IC50 = 0.9 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
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 = 2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0076420
 Compound Info 
1-(4'-((S)-1-((S)-1-((S)-1-cyano-2-(4-cyano-2-fluorophenyl)ethylamino)-3-methyl-1-oxobutan-2-ylamino)-2,2,2-trifluoroethyl)biphenyl-4-yl)cyclopropanecarboxamide
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C33H31F4N5O2
  1
1
IC50 = 3 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Cathepsin K (CTSK) )
Target Type Clinical trial Target
Disease 5 Target-related Diseases  5
1 Osteoporosis [ICD-11: FB83.0]
2 Rheumatoid arthritis [ICD-11: FA20]
3 Bone metastases [ICD-11: 2D50]
4 Osteoarthritis [ICD-11: FA00-FA05]
5 Asthma [ICD-11: CA23]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Odanacatib
 Drug Info 
Phase 3
Osteoporosis
2 VEL-0230
 Drug Info 
Phase 1
Rheumatoid arthritis
Discontinued Drug(s) 2 Discontinued Drugs  2
1 Balicatib
 Drug Info 
Discontinued in Phase 2
Osteoporosis
2 Relacatib
 Drug Info 
Discontinued in Phase 2
Bone metastases
Investigative Drug(s) 1 Investigative Drug  1
1 L-873724
 Drug Info 
Investigative
Asthma
Preclinical Drug(s) 1 Preclinical Drug  1
1 L-006235-1
 Drug Info 
Preclinical
Osteoarthritis
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02490 Cathepsin K Rattus norvegicus, Rat
 Protein Info