BRENDA - Enzyme Database show
show all sequences of 3.4.22.38

Dioxo-triazines as a novel series of cathepsin K inhibitors

Rankovic, Z.; Cai, J.; Fradera, X.; Dempster, M.; Mistry, A.; Mitchell, A.; Long, C.; Hamilton, E.; King, A.; Boucharens, S.; Jamieson, C.; Gillespie, J.; Cumming, I.; Uitdehaag, J.; van Zeeland, M.; Bioorg. Med. Chem. Lett. 20, 1488-1490 (2010)

Data extracted from this reference:

Inhibitors
Inhibitors
Commentary
Organism
Structure
2-(3-methoxyphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-(3-methylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-(3-tert-butylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-(biphenyl-3-yl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cycloheptyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cycloheptyl-3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cycloheptyl-4-[2-(dimethylamino)ethyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cycloheptyl-4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cyclohexyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cyclopentyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-[3-(hydroxymethyl)phenyl]-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-2-phenyl-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-2-[3-(propan-2-yl)phenyl]-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-(2-phenylethyl)-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-phenyl-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-propyl-2-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-[2-(piperidin-1-yl)ethyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(propan-2-yl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-ethyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-methyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-[2-(dimethylamino)ethyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-[3-(dimethylamino)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
6-cyano-2-(3-trifluoromethyl-phenyl)-3,5-dioxo-1,2,4-triazine
poor catK potency
Homo sapiens
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Homo sapiens
-
-
-
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
707694
Homo sapiens
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
IC50 Value
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.000017
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000038
-
pH and temperature not specified in the publication
Homo sapiens
2-cycloheptyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000038
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(propan-2-yl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000072
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-2-[3-(propan-2-yl)phenyl]-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0001
-
pH and temperature not specified in the publication
Homo sapiens
2-cycloheptyl-3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0001
-
pH and temperature not specified in the publication
Homo sapiens
4-[3-(dimethylamino)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00011
-
pH and temperature not specified in the publication
Homo sapiens
2-cycloheptyl-4-[2-(dimethylamino)ethyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000112
-
pH and temperature not specified in the publication
Homo sapiens
4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000182
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-[2-(piperidin-1-yl)ethyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000197
-
pH and temperature not specified in the publication
Homo sapiens
2-cyclohexyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000288
-
pH and temperature not specified in the publication
Homo sapiens
2-(3-tert-butylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0005
-
pH and temperature not specified in the publication
Homo sapiens
2-cycloheptyl-4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00081
-
pH and temperature not specified in the publication
Homo sapiens
4-[2-(dimethylamino)ethyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00087
-
pH and temperature not specified in the publication
Homo sapiens
2-cyclopentyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.001
-
pH and temperature not specified in the publication
Homo sapiens
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0011
-
pH and temperature not specified in the publication
Homo sapiens
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.002
-
pH and temperature not specified in the publication
Homo sapiens
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.002
-
pH and temperature not specified in the publication
Homo sapiens
6-cyano-2-(3-trifluoromethyl-phenyl)-3,5-dioxo-1,2,4-triazine
0.0025
-
pH and temperature not specified in the publication
Homo sapiens
4-ethyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0035
-
pH and temperature not specified in the publication
Homo sapiens
2-(3-methylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00446
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-(2-phenylethyl)-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00478
-
pH and temperature not specified in the publication
Homo sapiens
4-methyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0074
-
pH and temperature not specified in the publication
Homo sapiens
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
2-[3-(hydroxymethyl)phenyl]-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
2-(3-methoxyphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
2-(biphenyl-3-yl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-2-phenyl-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-propyl-2-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.012
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-phenyl-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
IC50 Value (protein specific)
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.000017
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000038
-
pH and temperature not specified in the publication
Homo sapiens
2-cycloheptyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000038
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(propan-2-yl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000072
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-2-[3-(propan-2-yl)phenyl]-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0001
-
pH and temperature not specified in the publication
Homo sapiens
2-cycloheptyl-3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0001
-
pH and temperature not specified in the publication
Homo sapiens
4-[3-(dimethylamino)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00011
-
pH and temperature not specified in the publication
Homo sapiens
2-cycloheptyl-4-[2-(dimethylamino)ethyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000112
-
pH and temperature not specified in the publication
Homo sapiens
4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000182
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-[2-(piperidin-1-yl)ethyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000197
-
pH and temperature not specified in the publication
Homo sapiens
2-cyclohexyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.000288
-
pH and temperature not specified in the publication
Homo sapiens
2-(3-tert-butylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0005
-
pH and temperature not specified in the publication
Homo sapiens
2-cycloheptyl-4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00081
-
pH and temperature not specified in the publication
Homo sapiens
4-[2-(dimethylamino)ethyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00087
-
pH and temperature not specified in the publication
Homo sapiens
2-cyclopentyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.001
-
pH and temperature not specified in the publication
Homo sapiens
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0011
-
pH and temperature not specified in the publication
Homo sapiens
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.002
-
pH and temperature not specified in the publication
Homo sapiens
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.002
-
pH and temperature not specified in the publication
Homo sapiens
6-cyano-2-(3-trifluoromethyl-phenyl)-3,5-dioxo-1,2,4-triazine
0.0025
-
pH and temperature not specified in the publication
Homo sapiens
4-ethyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0035
-
pH and temperature not specified in the publication
Homo sapiens
2-(3-methylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00446
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-(2-phenylethyl)-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.00478
-
pH and temperature not specified in the publication
Homo sapiens
4-methyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.0074
-
pH and temperature not specified in the publication
Homo sapiens
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
2-[3-(hydroxymethyl)phenyl]-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
2-(3-methoxyphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
2-(biphenyl-3-yl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-2-phenyl-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.01
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-propyl-2-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
0.012
-
pH and temperature not specified in the publication
Homo sapiens
3,5-dioxo-4-phenyl-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
2-(3-methoxyphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-(3-methylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-(3-tert-butylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-(biphenyl-3-yl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cycloheptyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cycloheptyl-3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cycloheptyl-4-[2-(dimethylamino)ethyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cycloheptyl-4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cyclohexyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-cyclopentyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
2-[3-(hydroxymethyl)phenyl]-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-2-phenyl-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-2-[3-(propan-2-yl)phenyl]-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-(2-phenylethyl)-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-phenyl-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-propyl-2-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-[2-(piperidin-1-yl)ethyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(propan-2-yl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-ethyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-methyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-[2-(dimethylamino)ethyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-[3-(dimethylamino)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
Homo sapiens
6-cyano-2-(3-trifluoromethyl-phenyl)-3,5-dioxo-1,2,4-triazine
poor catK potency
Homo sapiens
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
707694
Homo sapiens
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
-
-
?
Other publictions for EC 3.4.22.38
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
731278
Sharma
Structural requirements for th ...
Homo sapiens
Biochem. J.
465
163-173
2015
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1
1
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1
731902
Hu
Cathepsin K activity controls ...
Mus musculus
Hypertension
63
607-615
2014
-
-
-
-
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2
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1
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5
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732561
Novinec
A novel allosteric mechanism i ...
Homo sapiens
Nat. Commun.
5
3287
2014
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1
1
1
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2
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3
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-
732583
Rodnick
Carbon-11 labeled cathepsin K ...
Rattus norvegicus
Nucl. Med. Biol.
41
384-389
2014
-
-
-
-
-
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2
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1
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5
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5
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1
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-
732769
Novinec
Probing the activity modificat ...
Homo sapiens
PLoS ONE
9
e106642
2014
-
-
-
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-
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5
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1
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2
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2
5
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3
-
-
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-
-
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-
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-
-
-
-
732741
Bitu
Cathepsin K is present in inva ...
Homo sapiens
PLoS ONE
8
e70925
2013
-
-
-
-
-
-
1
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1
-
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1
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1
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3
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1
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1
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1
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1
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-
-
-
3
-
-
1
-
-
-
-
-
-
-
-
-
-
2
2
-
-
-
718051
Schmit
Cathepsin K expression and act ...
Canis lupus familiaris
J. Vet. Intern. Med.
26
126-134
2012
-
1
-
-
-
-
-
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1
-
1
1
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3
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8
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1
1
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1
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1
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1
1
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8
-
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1
1
-
-
-
-
-
-
-
-
1
-
-
1
-
-
731571
Borel
Cathepsin K preferentially sol ...
Homo sapiens
Calcif. Tissue Int.
91
32-39
2012
-
-
-
-
-
-
1
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-
-
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3
-
3
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3
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1
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1
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3
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-
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1
1
-
-
-
732842
Roy
-
Expression of recombinant huma ...
Homo sapiens
Process Biochem.
47
1944-1947
2012
3
-
1
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-
-
3
1
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2
2
-
1
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1
-
1
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3
1
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-
1
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1
3
-
1
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1
3
-
1
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2
2
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1
1
-
-
-
3
1
-
-
-
-
1
-
-
-
-
1
1
-
-
-
709307
Yan
Stromal expression of cathepsi ...
Homo sapiens
J. Eur. Acad. Dermatol. Venereol.
25
362-365
2011
-
1
-
-
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3
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3
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-
-
-
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-
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-
717159
Wilder
Manipulating substrate and pH ...
Homo sapiens
Arch. Biochem. Biophys.
516
52-57
2011
-
-
-
-
-
-
-
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2
2
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2
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1
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1
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2
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1
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2
2
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1
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2
1
-
-
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-
-
-
1
-
-
-
-
-
-
-
717363
Isabel
Difluoroethylamines as an amid ...
Oryctolagus cuniculus
Bioorg. Med. Chem. Lett.
21
920-923
2011
-
-
-
-
-
-
10
-
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1
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-
10
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-
10
10
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-
-
-
-
-
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-
-
-
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-
-
717867
Cherney
Structure-activity analysis of ...
Homo sapiens
J. Biol. Chem.
286
8988-8998
2011
2
-
1
1
5
-
1
11
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1
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4
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12
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2
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1
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1
5
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1
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11
-
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2
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-
-
1
-
-
4
-
-
-
-
12
-
-
-
-
-
-
-
-
12
12
707120
Li
Detection of femtomole quantit ...
Homo sapiens
Anal. Biochem.
401
91-98
2010
-
-
-
-
-
-
1
-
-
-
2
1
-
3
-
-
-
-
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1
-
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3
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-
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-
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1
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-
-
-
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1
1
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-
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2
1
-
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-
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1
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
707334
Bai
Cathepsin K gene disruption do ...
Mus musculus
Atherosclerosis
209
96-103
2010
-
-
-
-
-
-
-
-
1
-
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3
-
4
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1
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3
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-
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-
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-
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1
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3
-
-
-
-
-
1
-
-
3
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
707694
Rankovic
Dioxo-triazines as a novel ser ...
Homo sapiens
Bioorg. Med. Chem. Lett.
20
1488-1490
2010
-
-
-
-
-
-
29
-
-
-
-
-
-
2
-
-
-
-
-
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1
-
-
-
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-
-
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-
29
-
-
-
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-
29
29
-
-
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-
-
-
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-
-
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-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
707695
Rankovic
Design and optimization of a s ...
Homo sapiens
Bioorg. Med. Chem. Lett.
20
1524-1527
2010
-
-
-
-
-
-
19
-
-
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-
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2
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-
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1
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19
-
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19
19
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-
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1
-
-
-
-
-
-
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-
-
-
-
-
-
-
-
707712
Isabel
The discovery of MK-0674, an o ...
Homo sapiens
Bioorg. Med. Chem. Lett.
20
887-892
2010
-
-
-
-
-
-
13
-
-
-
-
-
-
2
-
-
-
-
-
-
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-
-
-
-
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-
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-
12
-
-
-
-
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12
13
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
707873
Barascuk
Human macrophage foam cells de ...
Homo sapiens
BMC Cardiovasc. Disord.
10
19
2010
-
-
-
-
-
-
-
-
-
-
-
1
-
3
-
-
-
-
-
4
-
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1
-
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-
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-
-
-
-
-
-
-
-
-
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-
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-
-
1
-
-
-
-
-
4
-
-
1
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
707899
Fuller
The resorptive apparatus of os ...
Homo sapiens
Bone
46
1400-1407
2010
-
-
1
-
-
-
3
-
-
-
-
-
-
3
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
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2
-
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1
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-
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2
3
-
-
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3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
708260
Kometani
Hurdles in the drug discovery ...
Homo sapiens
Curr. Top. Med. Chem.
10
733-744
2010
-
-
-
-
-
-
2
-
1
-
-
3
-
1
-
-
-
-
-
2
-
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4
-
-
-
-
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1
1
1
-
-
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-
-
-
-
-
-
-
-
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2
-
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1
-
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3
-
-
-
-
-
2
-
-
4
-
-
-
-
-
1
1
1
-
-
1
1
-
1
1
708261
Black
Peptidomimetic inhibitors of c ...
Homo sapiens
Curr. Top. Med. Chem.
10
745-751
2010
-
-
-
-
-
-
13
-
-
-
-
1
-
2
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
7
-
-
-
-
-
-
-
-
-
-
13
7
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
708262
Teno
Orally bioavailable cathepsin ...
Homo sapiens
Curr. Top. Med. Chem.
10
752-766
2010
-
-
-
-
-
-
58
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
57
-
-
-
-
-
-
-
57
58
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
708388
Pan
3D QSAR studies on ketoamides ...
Homo sapiens
Eur. J. Med. Chem.
45
667-681
2010
-
-
-
-
-
-
63
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
63
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
708393
Yamaguchi
Low-energy laser irradiation f ...
Rattus norvegicus
Eur. J. Orthod.
32
131-139
2010
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
1
1
1
-
-
708535
Harikrishnan
Immune response and expression ...
Carassius auratus
Fish Shellfish Immunol.
28
511-516
2010
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
-
-
7
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
7
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
709409
Khan
A novel missense mutation in c ...
Homo sapiens
J. Investig. Med.
58
720-724
2010
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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1
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-
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-
-
-
-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
709888
Fontanesi
A single nucleotide polymorphi ...
Sus scrofa
Mol. Biol. Rep.
37
491-495
2010
-
-
-
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1
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-
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3
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6
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4
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1
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3
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-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
717214
Novinec
Conformational flexibility and ...
Homo sapiens
Biochem. J.
429
379-389
2010
5
-
-
-
-
1
2
4
-
-
-
-
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2
-
1
-
-
-
1
-
-
4
-
-
-
-
4
-
-
-
-
-
-
-
5
-
-
-
-
-
1
-
2
-
4
-
-
-
-
-
-
1
-
-
1
-
-
4
-
-
-
-
4
-
-
-
-
-
-
-
-
4
4
696041
Zhao
Cathepsin K: a therapeutic tar ...
Homo sapiens
Biochem. Biophys. Res. Commun.
380
721-723
2009
1
1
1
-
1
-
9
-
1
-
-
1
-
1
-
1
-
-
-
9
-
-
1
1
-
-
-
-
-
-
-
-
-
-
-
1
1
1
-
-
1
-
-
9
-
-
1
-
-
1
-
-
1
-
-
9
-
-
1
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
696664
Morley
5-Aminopyrimidin-2-ylnitriles ...
Homo sapiens
Bioorg. Med. Chem. Lett.
19
1658-1661
2009
-
1
-
-
-
-
17
-
1
-
-
-
-
1
-
-
-
-
-
-
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-
-
-
-
-
-
-
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17
-
1
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-
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-
17
17
-
-
1
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-
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-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
696697
Boyd
Investigation of ketone warhea ...
Homo sapiens, Oryctolagus cuniculus, Rattus norvegicus
Bioorg. Med. Chem. Lett.
19
675-679
2009
-
1
-
-
-
-
52
-
3
-
-
1
-
3
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
50
-
1
-
-
-
-
-
50
52
-
-
3
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
696743
Ayesa
Solid-phase parallel synthesis ...
Homo sapiens
Bioorg. Med. Chem.
17
1307-1324
2009
-
-
1
-
-
-
47
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
47
-
-
-
-
1
-
-
-
-
-
47
47
-
-
-
-
-
-
-
-
1
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
697010
Kozloff
Non-invasive optical detection ...
Homo sapiens, Mus musculus
Bone
44
190-198
2009
2
-
-
-
-
-
2
-
2
-
-
4
-
4
-
2
-
-
-
7
-
-
6
-
2
-
-
-
2
-
-
-
-
-
-
2
-
-
-
-
-
-
-
2
-
-
2
-
-
4
-
-
2
-
-
7
-
-
6
-
2
-
-
-
2
-
-
-
-
-
-
-
-
-
697011
Pennypacker
Bone density, strength, and fo ...
Mus musculus
Bone
44
199-207
2009
-
-
-
-
1
-
3
-
1
-
-
1
-
2
-
-
-
-
-
3
-
-
2
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
3
-
-
1
-
-
1
-
-
-
-
-
3
-
-
2
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
697012
Morko
Overexpression of cathepsin K ...
Mus musculus
Bone
44
717-728
2009
-
-
-
-
1
-
-
-
1
-
-
1
-
3
-
-
-
-
-
3
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
3
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
697066
Boskey
Ablation of cathepsin K activi ...
Mus musculus, Mus musculus C57Bl6/J
Calcif. Tissue Int.
84
229-239
2009
-
-
-
-
1
-
2
-
1
-
-
2
-
10
-
-
-
-
-
9
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
2
-
-
1
-
-
2
-
-
-
-
-
9
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
697150
Guo
Leucocyte cathepsin K affects ...
Mus musculus
Cardiovasc. Res.
81
278-285
2009
-
1
-
-
1
-
-
-
-
-
-
1
-
3
-
-
-
-
-
5
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
5
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
697619
Han
Cathepsin K regulates adipocyt ...
Mus musculus
Endocr. J.
56
55-63
2009
-
1
-
-
-
-
1
-
1
-
-
1
-
1
-
-
-
-
-
2
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
1
-
-
1
-
-
-
-
-
2
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
697775
Svelander
Inhibition of cathepsin K redu ...
Homo sapiens, Mus musculus, Mus musculus DBA/1J
Eur. J. Pharmacol.
613
155-162
2009
-
-
-
-
-
-
2
-
-
-
-
3
-
7
-
-
-
-
-
8
-
-
5
-
-
-
-
-
-
-
-
-
1
-
2
-
-
-
-
-
-
-
2
2
1
-
-
-
-
3
-
-
-
-
-
8
-
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
698935
Wilson
Cathepsin K activity-dependent ...
Homo sapiens, Mus musculus, Mus musculus C57BL/6
J. Biol. Chem.
284
2584-2592
2009
-
-
-
-
1
-
2
-
-
-
-
3
-
142
-
-
-
-
-
4
-
-
6
-
2
-
2
-
2
-
2
-
-
-
-
-
-
-
-
-
1
-
-
2
-
-
-
-
-
3
-
-
-
-
-
4
-
-
6
-
2
-
2
-
2
-
2
-
-
-
-
-
-
-
699396
Li
Molecular analysis of a novel ...
Homo sapiens
J. Int. Med. Res.
37
264-269
2009
-
-
1
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
699723
O'Shea
A practical enantioselective s ...
Homo sapiens
J. Org. Chem.
74
1605-1610
2009
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
699971
Aydin
Cathepsin K/TRAP: Can they be ...
Homo sapiens
Med. Hypotheses
72
464-465
2009
-
1
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
700549
Connor
Protective effects of a cathep ...
Canis lupus familiaris
Osteoarthr. Cartil.
17
1236-1243
2009
-
-
-
-
-
-
1
-
-
-
-
4
-
4
-
-
-
-
-
8
-
-
6
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
4
-
-
-
-
-
8
-
-
6
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
700550
Vinardell
Evidence to suggest that cathe ...
Equus caballus
Osteoarthr. Cartil.
17
375-383
2009
-
-
-
-
-
-
-
-
-
-
-
4
-
4
-
-
-
-
-
3
-
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
-
-
3
-
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
700689
Park
A furanquinone from Paulownia ...
Homo sapiens
Phytother. Res.
23
1485-1488
2009
-
-
1
-
-
-
5
-
1
-
-
-
-
2
-
-
-
-
-
2
-
-
2
-
1
-
-
-
1
-
-
-
-
-
5
-
-
1
-
-
-
-
5
5
-
-
1
-
-
-
-
-
-
-
-
2
-
-
2
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
707013
Veber
Factors that influence oral bi ...
Rattus norvegicus
Adv. Exp. Med. Biol.
611
607-610
2009
-
-
-
-
-
-
5
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
5
-
-
-
-
-
-
-
-
-
-
5
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
707295
Garg
Effect of nonsurgical periodon ...
Homo sapiens
Arch. Oral Biol.
54
1046-1051
2009
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
2
1
1
2
-
-
707318
Takahashi
Down-regulation of cathepsin K ...
Oryctolagus cuniculus
Arthritis Rheum.
60
2372-2380
2009
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
1
2
2
1
-
-
707615
Desmarais
Pharmacological inhibitors to ...
Homo sapiens, Mus musculus, Oryctolagus cuniculus, Rattus norvegicus
Biol. Chem.
390
941-948
2009
-
3
-
-
-
-
36
-
-
-
-
3
-
9
-
-
3
-
-
2
-
-
3
-
-
-
-
-
-
-
-
-
-
-
33
-
3
-
-
-
-
-
33
36
-
-
-
-
-
3
-
-
-
3
-
2
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
707715
Li
Substrate optimization for mon ...
Homo sapiens
Bioorg. Med. Chem.
17
1064-1070
2009
-
-
-
-
-
-
3
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
1
-
-
-
1
-
-
-
3
-
-
-
-
-
-
-
-
-
-
3
3
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
707946
Stroup
Treatment with a potent cathep ...
Macaca fascicularis
Calcif. Tissue Int.
85
344-355
2009
-
1
-
-
-
-
1
-
-
-
-
-
-
5
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
708148
Sun
Free cholesterol accumulation ...
Mus musculus
Circ. Res.
104
455-465
2009
-
-
-
-
-
-
-
-
-
-
-
1
-
2
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
2
-
-
2
-
-
708205
Stoch
Effect of the cathepsin K inhi ...
Homo sapiens
Clin. Pharmacol. Ther.
86
175-182
2009
-
-
-
-
-
-
1
-
-
-
-
-
-
2
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
708216
Je
Molecular cloning, expression ...
Paralichthys olivaceus
Comp. Biochem. Physiol. A
154
474-485
2009
4
-
1
-
-
-
14
-
-
3
1
5
-
4
-
-
1
-
-
14
-
-
16
-
-
-
-
-
1
1
1
-
-
-
-
4
-
1
-
-
-
-
-
14
-
-
-
3
1
5
-
-
-
1
-
14
-
-
16
-
-
-
-
-
1
1
1
-
1
1
1
1
-
-
708423
Quintanilla-Dieck
Expression and regulation of c ...
Homo sapiens
Exp. Dermatol.
18
596-602
2009
-
-
-
-
-
-
-
-
1
-
-
2
-
1
-
-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
2
-
-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
-
2
1
1
2
-
-
708429
Golovatch
Role for cathepsin K in emphys ...
Cavia porcellus, Homo sapiens
Exp. Lung Res.
35
631-645
2009
-
-
-
-
-
-
-
-
-
-
-
-
-
5
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
2
-
-
708450
Broemme
Cathepsin K inhibitors for ost ...
Homo sapiens
Expert Opin. Investig. Drugs
18
585-600
2009
-
-
-
-
-
-
10
-
1
-
-
1
-
3
-
-
-
-
-
11
-
-
1
-
-
-
-
-
-
-
-
-
2
-
2
-
-
-
-
-
-
-
2
10
2
-
1
-
-
1
-
-
-
-
-
11
-
-
1
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
708541
Naumnik
Serum cathepsin K and cystatin ...
Homo sapiens
Folia Histochem. Cytobiol.
47
207-213
2009
-
1
-
-
-
-
1
-
-
-
-
-
-
2
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
708572
Podgorski
Future of anticathepsin K drug ...
Homo sapiens
Future Med. Chem.
1
21-34
2009
-
1
-
-
-
-
6
-
-
-
-
4
-
1
-
-
-
-
-
9
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
6
-
-
-
-
-
4
-
-
-
-
-
9
-
-
4
-
-
-
-
-
-
-
-
-
1
1
1
1
-
-
708580
Balkan
Identification of NFAT binding ...
Rattus norvegicus
Gene
446
90-98
2009
-
-
1
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
1
1
2
-
-
708689
Lewiecki
Odanacatib, a cathepsin K inhi ...
Homo sapiens
IDrugs
12
799-809
2009
-
1
-
-
-
-
1
-
1
-
-
1
-
2
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
1
-
-
1
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
709794
Munoz-Torres
Serum cathepsin K as a marker ...
Homo sapiens
Maturitas
64
188-192
2009
-
1
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
2
-
-
709855
Chappard
The cathepsin K inhibitor AAE5 ...
Homo sapiens
Microsc. Res. Tech.
73
726-732
2009
-
-
-
-
-
-
1
-
-
-
-
1
-
3
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
710073
Lendeckel
Cathepsin K generates enkephal ...
Homo sapiens
Neurochem. Int.
54
410-417
2009
-
-
-
-
-
-
-
-
-
-
-
1
-
2
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
1
1
1
1
-
-
710231
Codriansky
Intracellular degradation of e ...
Homo sapiens
Photochem. Photobiol.
85
1356-1363
2009
-
-
-
-
-
-
-
-
1
-
-
1
-
2
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
1
1
1
1
-
-
677895
Samokhin
Role of cathepsin K in structu ...
Mus musculus
Atherosclerosis
200
58-68
2008
-
1
-
-
1
-
-
-
-
-
-
-
-
4
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
678499
Lecaille
Biochemical properties and reg ...
Homo sapiens
Biochimie
90
208-226
2008
-
1
-
1
1
-
4
-
-
-
1
-
-
1
-
2
-
-
-
-
-
-
1
1
-
-
-
-
1
-
-
-
8
-
-
-
1
-
-
1
1
-
-
4
8
-
-
-
1
-
-
-
2
-
-
-
-
-
1
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
681252
Quintanilla-Dieck
Cathepsin K in Melanoma Invasi ...
Homo sapiens
J. Invest. Dermatol.
128
2281-2288
2008
-
1
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
682861
Asagiri
Cathepsin K-dependent toll-lik ...
Mus musculus, Rattus norvegicus
Science
319
624-627
2008
-
2
-
-
1
-
1
-
-
-
-
-
-
3
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
695456
Dejica
Cleavage of type II collagen b ...
Homo sapiens
Am. J. Pathol.
173
161-169
2008
2
-
1
-
-
-
1
-
-
-
-
2
-
2
-
-
1
-
-
2
-
-
3
-
1
-
-
-
1
1
-
-
-
-
-
2
-
1
-
-
-
-
-
1
-
-
-
-
-
2
-
-
-
1
-
2
-
-
3
-
1
-
-
-
1
1
-
-
-
-
-
-
-
-
695609
Neidhart
Expression of cathepsin K and ...
Homo sapiens
Ann. Rheum. Dis.
68
1334-1339
2008
-
-
-
-
-
-
-
-
-
-
-
1
-
2
-
-
-
-
-
5
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
5
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
695899
Tsuchiya
Comparison of expression patte ...
Rattus norvegicus
Arch. Histol. Cytol.
71
89-100
2008
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
5
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
695943
Yang
Deficiency and inhibition of c ...
Homo sapiens, Mus musculus
Arterioscler. Thromb. Vasc. Biol.
28
2202-2208
2008
-
-
-
-
1
-
4
-
-
-
1
2
-
6
-
-
-
-
-
10
-
-
3
1
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
1
-
-
4
-
-
-
-
1
2
-
-
-
-
-
10
-
-
3
1
1
-
-
-
1
-
-
-
-
-
-
-
-
-
695956
Schurigt
Cathepsin K deficiency partial ...
Mus musculus
Arthritis Rheum.
58
422-434
2008
-
-
1
-
1
-
-
-
-
-
-
-
-
4
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
696617
Teno
New chemotypes for cathepsin K ...
Homo sapiens
Bioorg. Med. Chem. Lett.
18
2599-2603
2008
-
1
-
-
-
-
16
-
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
15
-
1
-
-
-
-
-
15
16
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
696630
Irie
Discovery of selective and non ...
Homo sapiens
Bioorg. Med. Chem. Lett.
18
3959-3962
2008
-
-
1
-
-
-
28
-
-
-
-
1
-
3
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
28
-
-
1
-
-
-
-
28
28
-
-
-
-
-
1
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
696631
Kim
Effect of novel N-cyano-tetrah ...
Homo sapiens
Bioorg. Med. Chem. Lett.
18
3988-3991
2008
-
-
-
-
-
-
9
-
1
-
-
1
-
1
-
-
-
-
-
2
-
-
2
-
1
-
-
-
1
-
-
-
-
-
8
-
-
-
-
-
-
-
8
9
-
-
1
-
-
1
-
-
-
-
-
2
-
-
2
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
696638
Irie
4-Amino-2-cyanopyrimidines: no ...
Homo sapiens
Bioorg. Med. Chem. Lett.
18
4642-4646
2008
-
1
-
-
-
-
23
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
23
-
1
-
-
-
-
-
23
23
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
696654
Gauthier
The discovery of odanacatib (M ...
Canis lupus familiaris, Homo sapiens, Macaca fascicularis, Macaca mulatta, Oryctolagus cuniculus, Rattus norvegicus
Bioorg. Med. Chem. Lett.
18
923-928
2008
-
-
-
-
-
-
41
-
6
-
-
-
-
7
-
-
-
-
-
19
-
-
-
-
-
-
-
-
-
-
-
-
-
-
24
-
-
-
-
-
-
-
24
41
-
-
6
-
-
-
-
-
-
-
-
19
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
697009
Yamane
The anabolic action of intermi ...
Mus musculus
Bone
44
1055-1062
2008
-
-
-
-
-
-
-
-
-
-
-
1
-
2
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
697257
Ravikumar
Virtual screening of cathepsin ...
Homo sapiens
Chem. Biol. Drug Des.
72
79-90
2008
-
1
-
-
-
-
55
-
1
-
-
1
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
55
-
-
1
-
-
1
-
-
-
-
-
2
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
697375
Kleer
Epithelial and stromal catheps ...
Homo sapiens
Clin. Cancer Res.
14
5357-5367
2008
-
1
1
-
-
-
1
-
1
-
-
1
-
2
-
-
-
-
-
10
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
1
-
-
-
-
-
1
-
-
1
-
-
1
-
-
-
-
-
10
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
698653
Tada
Species differences between hu ...
Homo sapiens, Rattus norvegicus
J. Biochem.
144
499-506
2008
2
-
2
-
4
-
-
5
-
-
-
2
-
4
-
-
-
-
-
-
-
-
9
2
2
-
-
5
2
-
-
-
-
-
-
2
-
2
-
-
4
-
-
-
-
5
-
-
-
2
-
-
-
-
-
-
-
-
9
2
2
-
-
5
2
-
-
-
-
-
-
-
-
-
699441
Teno
Effect of cathepsin K inhibito ...
Homo sapiens, Rattus norvegicus
J. Med. Chem.
51
5459-5462
2008
-
1
-
-
-
-
18
-
-
-
-
2
-
4
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
14
-
1
-
-
-
-
-
14
18
-
-
-
-
-
2
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
699442
Irie
Discovery of orally bioavailab ...
Homo sapiens, Rattus norvegicus
J. Med. Chem.
51
5502-5505
2008
-
-
-
-
-
-
11
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
11
-
-
-
-
-
-
-
11
11
-
-
-
-
-
-
-
-
-
-
-
-
-
-
2
-
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Robichaud
Identification of a nonbasic, ...
Oryctolagus cuniculus
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699557
Li
The crystal and molecular stru ...
Homo sapiens
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1
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-
699918
Wendling
Serum levels of MMP-3 and cath ...
Homo sapiens
Joint Bone Spine
75
559-562
2008
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-
-
-
-
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2
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2
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700688
Kim
Inhibition of Ulmus davidiana ...
Mus musculus
Phytother. Res.
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511-517
2008
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1
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2
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1
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8
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8
1
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2
1
1
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1
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701180
Srivastava
Overexpression of cathepsin K ...
Mus musculus, Mus musculus FVB/N
Respir. Res.
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1
1
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1
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5
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-
701297
Mikosch
High cathepsin K levels in men ...
Homo sapiens
Thyroid
18
27-33
2008
1
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2
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1
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2
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1
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677816
Lecaille
Modulation of hypotensive effe ...
Homo sapiens, Rattus norvegicus
Arch. Biochem. Biophys.
459
129-136
2007
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1
2
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1
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2
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7
-
2
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2
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-
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679251
Jaffer
Optical visualization of cathe ...
Homo sapiens
Circulation
115
2292-2298
2007
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1
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1
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681251
Ruenger
Role of cathepsin K in the tur ...
Homo sapiens
J. Invest. Dermatol.
127
293-297
2007
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5
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5
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685569
Barrett
Acyclic, orally bioavailable k ...
Homo sapiens
Bioorg. Med. Chem. Lett.
17
22-27
2007
1
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15
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15
15
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1
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1
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685572
Robichaud
Beta-substituted cyclohexaneca ...
Homo sapiens, Oryctolagus cuniculus
Bioorg. Med. Chem. Lett.
17
3146-3151
2007
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22
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685578
Leger
Primary amides as selective in ...
Homo sapiens
Bioorg. Med. Chem. Lett.
17
4328-4332
2007
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20
4
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4
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4
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20
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20
20
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4
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4
-
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-
-
4
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688262
Altmann
2-Cyano-pyrimidines: a new che ...
Homo sapiens
J. Med. Chem.
50
591-594
2007
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1
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15
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15
15
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1
-
-
-
-
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667121
Rapa
Cathepsin K is selectively exp ...
Homo sapiens
Am. J. Clin. Pathol.
125
847-854
2006
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1
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1
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1
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667977
Altmann
Dipeptide nitrile inhibitors o ...
Homo sapiens
Bioorg. Med. Chem. Lett.
16
2549-2554
2006
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15
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1
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15
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15
15
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1
-
-
-
-
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-
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668097
Mandelin
Human osteoblasts produce cath ...
Homo sapiens
Bone
38
769-777
2006
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2
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2
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-
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-
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669625
Xiao
Cathepsin K in adipocyte diffe ...
Homo sapiens
J. Clin. Endocrinol. Metab.
91
4520-4527
2006
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2
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1
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1
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1
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-
1
-
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-
-
-
-
-
-
-
-
-
-
-
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685560
Shinozuka
4-Aminophenoxyacetic acids as ...
Homo sapiens
Bioorg. Med. Chem. Lett.
16
1502-1505
2006
1
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31
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1
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31
1
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31
31
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1
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1
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685561
Palmer
Keto-1,3,4-oxadiazoles as cath ...
Homo sapiens
Bioorg. Med. Chem. Lett.
16
2909-2914
2006
3
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24
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1
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1
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25
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1
3
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1
24
25
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-
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-
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-
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-
-
-
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-
1
-
-
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-
-
1
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-
-
-
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685563
Setti
Design and synthesis of tetrac ...
Homo sapiens
Bioorg. Med. Chem. Lett.
16
4296-4299
2006
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7
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7
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7
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7
7
7
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-
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-
-
-
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-
-
-
-
-
-
-
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685564
Adkison
Semicarbazone-based inhibitors ...
Homo sapiens
Bioorg. Med. Chem. Lett.
16
978-983
2006
1
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39
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1
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39
39
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1
-
-
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1
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669364
Ljusberg
Proteolytic excision of a repr ...
Homo sapiens
J. Biol. Chem.
280
28370-28381
2005
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1
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2
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1
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1
-
-
2
-
-
-
-
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-
-
-
-
-
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669757
Holzer
Soluble cathepsin K: a novel m ...
Homo sapiens
J. Lab. Clin. Med.
146
13-17
2005
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1
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1
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-
1
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-
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-
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-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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-
669795
Palmer
Design and synthesis of tri-ri ...
Homo sapiens
J. Med. Chem.
48
7520-7534
2005
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1
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53
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-
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1
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-
-
-
-
-
-
-
-
-
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670870
van den Brule
Overexpression of cathepsin K ...
Homo sapiens, Mus musculus
Respir. Res.
6
84
2005
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3
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-
-
-
-
-
-
-
-
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-
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-
-
-
-
-
-
656472
Tavares
Design of potent, selective, a ...
Homo sapiens, Rattus norvegicus
J. Med. Chem.
47
588-599
2004
-
-
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55
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4
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2
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-
-
-
-
-
-
-
-
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55
-
-
-
-
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-
55
55
-
-
-
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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667131
Buehling
Pivotal role of cathepsin K in ...
Homo sapiens, Mus musculus
Am. J. Pathol.
164
2203-2216
2004
-
-
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1
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2
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2
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-
-
-
-
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-
-
-
-
-
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-
-
-
-
-
-
-
-
-
-
1
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2
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-
-
-
-
2
-
-
2
-
-
-
-
-
-
-
-
-
-
-
-
-
-
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667135
Lindeman
Cathepsin K is the principal p ...
Homo sapiens
Am. J. Pathol.
165
593-600
2004
-
-
-
-
-
-
-
-
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1
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-
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-
-
-
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-
-
-
-
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-
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-
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-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
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-
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-
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667486
Godat
Cathepsin K: a cysteine protea ...
Mus musculus
Biochem. J.
383
501-506
2004
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1
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1
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1
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5
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1
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-
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-
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-
668393
Troen
The role of cathepsin K in nor ...
Homo sapiens
Drug News Perspect.
17
19-28
2004
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1
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1
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1
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1
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1
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-
1
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-
-
-
-
-
-
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-
-
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-
669563
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-
-
2
-
-
-
-
-
17
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
17
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-