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Literature summary extracted from
- Chalcones, semicarbazones and pyrazolines as inhibitors of cathepsins B, H and L (2015), Int. J. Biol. Macromol., 80, 710-724 .
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.22.16 | (2E)-1,3-diphenylprop-2-en-1-one | - |
Capra hircus |  |
| 3.4.22.16 | (2E)-2-(1,3-diphenylpropylidene)hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2E)-2-[3-(2-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2E)-2-[3-(2-methoxyphenyl)-1-phenylpropylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2E)-2-[3-(3-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2E)-2-[3-(3-methoxyphenyl)-1-phenylpropylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2E)-2-[3-(3-nitrophenyl)-1-phenylpropylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2E)-2-[3-(4-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2E)-2-[3-(4-methylphenyl)-1-phenylpropylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2E)-2-[3-(4-nitrophenyl)-1-phenylpropylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-one | - |
Capra hircus | |
| 3.4.22.16 | (2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-one | - |
Capra hircus | |
| 3.4.22.16 | (2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-one | - |
Capra hircus | |
| 3.4.22.16 | (2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-one | - |
Capra hircus | |
| 3.4.22.16 | (2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-one | - |
Capra hircus | |
| 3.4.22.16 | (2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one | - |
Capra hircus | |
| 3.4.22.16 | (2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one | - |
Capra hircus | |
| 3.4.22.16 | (2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-one | - |
Capra hircus | |
| 3.4.22.16 | (2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one | - |
Capra hircus | |
| 3.4.22.16 | (2Z)-2-[(2E)-1,3-diphenylprop-2-en-1-ylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2Z)-2-[(2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2Z)-2-[(2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2Z)-2-[(2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2Z)-2-[(2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2Z)-2-[(2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2Z)-2-[(2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2Z)-2-[(2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | (2Z)-2-[(2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | - |
Capra hircus | |
| 3.4.22.16 | 3,5-diphenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | 5-(2-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | 5-(2-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | 5-(3-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | 5-(3-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | 5-(3-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | 5-(4-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | 5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | 5-(4-methylphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | 5-(4-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | - |
Capra hircus | |
| 3.4.22.16 | additional information | chalcones, semicarbazones and pyrazolines as inhibitors of cathepsins H, synthesis and inhibitory potencies, pharmacological evaluation, molecular docking, overview. Structure-activity relationship analysis | 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, and cation exchange and anion exchange chromatography | 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 | 0.024 | - |
purified cathepsin H, pH 6.0, 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 | 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 | 0.021 | - |
(2E)-2-[3-(4-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.023 | - |
(2Z)-2-[(2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.025 | - |
5-(3-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.029 | - |
(2Z)-2-[(2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.032 | - |
(2E)-2-[3-(4-nitrophenyl)-1-phenylpropylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.033 | - |
(2E)-2-[3-(2-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.033 | - |
(2E)-2-[3-(3-nitrophenyl)-1-phenylpropylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.038 | - |
5-(3-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.04 | - |
(2E)-2-[3-(4-methylphenyl)-1-phenylpropylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.04 | - |
5-(2-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.043 | - |
(2Z)-2-[(2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.043 | - |
5-(3-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.045 | - |
(2Z)-2-[(2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.048 | - |
5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.048 | - |
5-(4-methylphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.054 | - |
(2E)-2-[3-(2-methoxyphenyl)-1-phenylpropylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.054 | - |
(2Z)-2-[(2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.06 | - |
(2E)-2-[3-(3-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.06 | - |
(2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.06 | - |
5-(2-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.06 | - |
5-(4-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.066 | - |
(2E)-2-(1,3-diphenylpropylidene)hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.066 | - |
(2E)-2-[3-(3-methoxyphenyl)-1-phenylpropylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.066 | - |
(2Z)-2-[(2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.066 | - |
5-(4-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.074 | - |
(2Z)-2-[(2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.083 | - |
(2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.096 | - |
(2Z)-2-[(2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.1 | - |
(2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.1 | - |
(2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.1 | - |
(2Z)-2-[(2E)-1,3-diphenylprop-2-en-1-ylidene]hydrazinecarboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.11 | - |
(2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.11 | - |
(2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.138 | - |
(2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.151 | - |
(2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.192 | - |
3,5-diphenyl-4,5-dihydro-1H-pyrazole-1-carboxamide | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.263 | - |
(2E)-1,3-diphenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
| 3.4.22.16 | 0.312 | - |
(2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-one | pH 6.0, 37°C | Capra hircus | |
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