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Literature summary extracted from

  • Garg, S.; Raghav, N.
    Inhibitory potential of some chalcones on cathepsins B, H and L (2015), RSC Adv., 5, 72937-72949 .
No PubMed abstract available

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.16 3-(2-chlorophenyl)-1-(4-bromophenyl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(2-chlorophenyl)-1-(naphthalen-3-yl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(2-chlorophenyl)-1-(pyridin-2-yl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(2-chlorophenyl)-1-(thien-2-yl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(3-chlorophenyl)-1-(4-aminophenyl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(3-chlorophenyl)-1-(4-fluorophenyl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(3-chlorophenyl)-1-(4-hydroxyphenyl)-prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(3-chlorophenyl)-1-(furan-2-yl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(4-chlorophenyl)-1-(4-(N'-4-nitrophenyl)methylene)aminophenyl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(4-chlorophenyl)-1-(4-methylphenyl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 3-(4-chlorophenyl)-1-(4-nitrophenyl)prop-2-en-1-one
-
 Capra hircus
3.4.22.16 additional information synthesis of a small library of chalcones and study of their role as inhibitors of cathepsins, overview. The most potent inhibitors among all compounds are chloro-substituted compounds for cathepsin H. Docking analysis and modeling, overview Capra hircus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.22.16 lysosome
-
 Capra hircus 5764
-

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.16 Capra hircus A0A060INS8
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.22.16 native enzyme from liver homogenate by acetone powder preparation, acid autolysis, ammonium sulfate fractionation, gel filtration, cation exchange and anion exchange chromatography, and again gel filtration Capra hircus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.22.16 liver
-
 Capra hircus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
3.4.22.16 0.02291
-
 purified native enzyme, pH 5.0, 37°C Capra hircus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.16 Leu-2-naphthylamide + H2O
-
 Capra hircus leucine + 2-naphthylamine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.16 CTSH
-
 Capra hircus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.22.16 37
-
 assay at Capra hircus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.22.16 5
-
 assay at Capra hircus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.22.16 0.0133
-
 3-(4-chlorophenyl)-1-(4-(N'-4-nitrophenyl)methylene)aminophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.0214
-
 3-(2-chlorophenyl)-1-(4-bromophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.0317
-
 3-(3-chlorophenyl)-1-(4-fluorophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.0416
-
 3-(4-chlorophenyl)-1-(4-methylphenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.0472
-
 3-(2-chlorophenyl)-1-(pyridin-2-yl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.0989
-
 3-(2-chlorophenyl)-1-(naphthalen-3-yl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.128
-
 3-(3-chlorophenyl)-1-(4-aminophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.163
-
 3-(3-chlorophenyl)-1-(4-hydroxyphenyl)-prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.217
-
 3-(2-chlorophenyl)-1-(thien-2-yl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.298
-
 3-(3-chlorophenyl)-1-(furan-2-yl)prop-2-en-1-one pH 5.0, 37°C Capra hircus
3.4.22.16 0.405
-
 3-(4-chlorophenyl)-1-(4-nitrophenyl)prop-2-en-1-one pH 5.0, 37°C Capra hircus