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Literature summary for 3.4.22.16 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

Inhibitors Comment Organism Structure
(2E)-1,3-diphenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 93.50% activity remaining Capra hircus
(2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 42.00% activity remaining Capra hircus
(2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 66.00% activity remaining Capra hircus
(2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 0.30% activity remaining Capra hircus
(2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 51.40% activity remaining Capra hircus
(2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 55.20% activity remaining Capra hircus
(2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 73.30% activity remaining Capra hircus
(2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 55.60% activity remaining Capra hircus
(2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 92.50% activity remaining Capra hircus
(2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 61.80% activity remaining Capra hircus
(2Z)-2-(2-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
(2Z)-2-(2-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
(2Z)-2-(2-nitrobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 6.10% activity remaining Capra hircus
(2Z)-2-(3-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
(2Z)-2-(3-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
(2Z)-2-(4-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 20.80% activity remaining Capra hircus
(2Z)-2-(4-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 37.00% activity remaining Capra hircus
(2Z)-2-(4-nitrobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 25.40% activity remaining Capra hircus
(2Z)-2-benzylidenehydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 14.60% activity remaining Capra hircus
(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
Leu-CH2Cl
-
Capra hircus
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

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

Organism

Organism UniProt Comment Textmining
Capra hircus A0A060INS8
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Capra hircus
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
CTSH
-
Capra hircus

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6
-
assay at Capra hircus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.009
-
(2Z)-2-(2-nitrobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 6.10% activity remaining Capra hircus
0.016
-
(2Z)-2-(3-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
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
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
0.06
-
(2Z)-2-benzylidenehydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 14.60% activity remaining Capra hircus
0.17
-
(2Z)-2-(4-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 20.80% activity remaining Capra hircus
0.2
-
(2Z)-2-(4-nitrobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 25.40% activity remaining Capra hircus
0.208
-
(2Z)-2-(2-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
0.28
-
(2Z)-2-(2-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
0.35
-
(2Z)-2-(4-methoxybenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, 37.00% activity remaining Capra hircus
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
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
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
0.704
-
(2Z)-2-(3-chlorobenzylidene)hydrazinecarbothioamide pH 6.0, 37°C, 1 mM, no activity remaining Capra hircus
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
1
-
(2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 61.80% activity remaining Capra hircus
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
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
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
8.19
-
(2E)-1,3-diphenylprop-2-en-1-one pH 6.0, 37°C, 1 mM, 93.50% activity remaining Capra hircus