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Literature summary for 3.4.22.38 extracted from

  • Svelander, L.; Erlandsson-Harris, H.; Astner, L.; Grabowska, U.; Klareskog, L.; Lindstrom, E.; Hewitt, E.
    Inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice (2009), Eur. J. Pharmacol., 613, 155-162.
    View publication on PubMed
Search for more literature for 3.4.22.38

Inhibitors

Inhibitors Comment Organism Structure
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide i.e. L-006235 or CRA-013788/L Homo sapiens
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide i.e. L-006235 or CRA-013788/L Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
collagen I + H2O Homo sapiens
-
 ?
-
 ?
collagen I + H2O Mus musculus inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice, overview ?
-
 ?
collagen I + H2O Mus musculus DBA/1J inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice, overview ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
 DBA/1J mice
-
Mus musculus DBA/1J
-
 DBA/1J mice
-

Source Tissue

Source Tissue Comment Organism Textmining
bone
-
 Mus musculus
-
bone
-
 Homo sapiens
-
osteoclast
-
 Mus musculus
-
osteoclast
-
 Homo sapiens
-
synovial fibroblast
-
 Mus musculus
-
synovial fibroblast
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
collagen I + H2O
-
 Mus musculus ?
-
 ?
collagen I + H2O
-
 Homo sapiens ?
-
 ?
collagen I + H2O inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice, overview Mus musculus ?
-
 ?
collagen I + H2O
-
 Mus musculus DBA/1J ?
-
 ?
collagen I + H2O inhibition of cathepsin K reduces bone erosion, cartilage degradation and inflammation evoked by collagen-induced arthritis in mice, overview Mus musculus DBA/1J ?
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000073
-
 N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide recombinant cathepsin K Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000024
-
 recombinant cathepsin K Mus musculus N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
0.000028
-
 at the cellular level in human osteoclasts Homo sapiens N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide