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Literature summary extracted from

  • Raghav, N.; Kaur, R.
    A comparative account of sar studies of semicarbazones and thiosemicarbazones on cathepsins H and L (2017), Med. Chem. Res., 26, 1723-1734 .
No PubMed abstract available

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.16 (2E)-1,3-diphenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 93.50% activity remaining Capra hircus
3.4.22.16 (2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 42.00% activity remaining Capra hircus
3.4.22.16 (2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 66.00% activity remaining Capra hircus
3.4.22.16 (2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 0.30% activity remaining Capra hircus
3.4.22.16 (2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 51.40% activity remaining Capra hircus
3.4.22.16 (2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 55.20% activity remaining Capra hircus
3.4.22.16 (2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 73.30% activity remaining Capra hircus
3.4.22.16 (2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 55.60% activity remaining Capra hircus
3.4.22.16 (2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 92.50% activity remaining Capra hircus
3.4.22.16 (2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 61.80% activity remaining Capra hircus
3.4.22.16 (2Z)-2-(2-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
3.4.22.16 (2Z)-2-(2-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
3.4.22.16 (2Z)-2-(2-nitrobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 6.10% activity remaining Capra hircus
3.4.22.16 (2Z)-2-(3-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
3.4.22.16 (2Z)-2-(3-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
3.4.22.16 (2Z)-2-(4-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 20.80% activity remaining Capra hircus
3.4.22.16 (2Z)-2-(4-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 37.00% activity remaining Capra hircus
3.4.22.16 (2Z)-2-(4-nitrobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 25.40% activity remaining Capra hircus
3.4.22.16 (2Z)-2-benzylidenehydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 14.60% activity remaining Capra hircus
3.4.22.16 (2Z)-2-[(2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C, 1 mM, 13.5% activity remaining Capra hircus
3.4.22.16 Leu-CH2Cl
-
 Capra hircus
3.4.22.16 additional information semicarbazones and thiosemicarbazones as inhibitors of cathepsins H, active site docking study and structure-activity relationship analysis, comparison to cathepsin L, 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
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.22.16 liver
-
 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 6
-
 assay at Capra hircus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.22.16 0.009
-
 (2Z)-2-(2-nitrobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 6.10% activity remaining Capra hircus
3.4.22.16 0.016
-
 (2Z)-2-(3-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
3.4.22.16 0.025
-
 (2Z)-2-[(2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C, 1 mM, 13.50% activity remaining Capra hircus
3.4.22.16 0.027
-
 (2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 0.30% activity remaining Capra hircus
3.4.22.16 0.06
-
 (2Z)-2-benzylidenehydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 14.60% activity remaining Capra hircus
3.4.22.16 0.17
-
 (2Z)-2-(4-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 20.80% activity remaining Capra hircus
3.4.22.16 0.2
-
 (2Z)-2-(4-nitrobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 25.40% activity remaining Capra hircus
3.4.22.16 0.208
-
 (2Z)-2-(2-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
3.4.22.16 0.28
-
 (2Z)-2-(2-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
3.4.22.16 0.35
-
 (2Z)-2-(4-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 37.00% activity remaining Capra hircus
3.4.22.16 0.43
-
 (2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 42.00% activity remaining Capra hircus
3.4.22.16 0.63
-
 (2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 51.40% activity remaining Capra hircus
3.4.22.16 0.7
-
 (2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 55.20% activity remaining Capra hircus
3.4.22.16 0.704
-
 (2Z)-2-(3-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
3.4.22.16 0.71
-
 (2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 55.60% activity remaining Capra hircus
3.4.22.16 1
-
 (2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 61.80% activity remaining Capra hircus
3.4.22.16 1.08
-
 (2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 66.00% activity remaining Capra hircus
3.4.22.16 1.66
-
 (2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 73.30% activity remaining Capra hircus
3.4.22.16 7.04
-
 (2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 92.50% activity remaining Capra hircus
3.4.22.16 8.19
-
 (2E)-1,3-diphenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 93.50% activity remaining Capra hircus