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Literature summary for 3.4.22.38 extracted from

  • Kim, S.H.; Jhon, D.J.; Song, J.H.; No, J.S.; Kang, N.S.
    Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts (2008), Bioorg. Med. Chem. Lett., 18, 3988-3991.
    View publication on PubMed
Search for more literature for 3.4.22.38

Inhibitors

Inhibitors Comment Organism Structure
1-(3-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
 Homo sapiens
1-(4-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
 Homo sapiens
1-(4-cyanophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
 Homo sapiens
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-(3-methylphenyl)urea
-
 Homo sapiens
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-phenylurea
-
 Homo sapiens
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-[3-(trifluoromethyl)phenyl]urea
-
 Homo sapiens
additional information inhibitory activities of N-cyano-tetrahydro-pyridazine derivatives, docking studies, overview Homo sapiens
tert-butyl ([1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]carbamoyl)carbamate
-
 Homo sapiens
[1-(2-cyano-tetrahydro-pyridazine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester inhibits the bone resorptive activity of mature osteoclasts, structure and interaction pattern with cathepsin K, overview Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Homo sapiens 5764
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens cathepsin K is the key regulator in the osteoclast-mediated bone resorption ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
bone
-
 Homo sapiens
-
osteoclast mature Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
carbobenzoxy-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens carbobenzoxy-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
 ?
additional information cathepsin K is the key regulator in the osteoclast-mediated bone resorption Homo sapiens ?
-
 ?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5.5
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
 pH 5.5, 30°C Homo sapiens [1-(2-cyano-tetrahydro-pyridazine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester
0.000004
-
 pH 5.5, 30°C Homo sapiens 1-(4-cyanophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
0.000006
-
 pH 5.5, 30°C Homo sapiens 1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-(3-methylphenyl)urea
0.000011
-
 pH 5.5, 30°C Homo sapiens 1-(3-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
0.000023
-
 pH 5.5, 30°C Homo sapiens 1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-[3-(trifluoromethyl)phenyl]urea
0.000024
-
 pH 5.5, 30°C Homo sapiens 1-(4-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
0.000025
-
 pH 5.5, 30°C Homo sapiens 1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-phenylurea
0.000055
-
 pH 5.5, 30°C Homo sapiens tert-butyl ([1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]carbamoyl)carbamate