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Literature summary for 3.4.22.16 extracted from

  • Raghav, N.; Kaur, R.
    Chalcones, semicarbazones and pyrazolines as inhibitors of cathepsins B, H and L (2015), Int. J. Biol. Macromol., 80, 710-724 .
    View publication on PubMed
Search for more literature for 3.4.22.16

Inhibitors

Inhibitors Comment Organism Structure
(2E)-1,3-diphenylprop-2-en-1-one
-
 Capra hircus
(2E)-2-(1,3-diphenylpropylidene)hydrazinecarboxamide
-
 Capra hircus
(2E)-2-[3-(2-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide
-
 Capra hircus
(2E)-2-[3-(2-methoxyphenyl)-1-phenylpropylidene]hydrazinecarboxamide
-
 Capra hircus
(2E)-2-[3-(3-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide
-
 Capra hircus
(2E)-2-[3-(3-methoxyphenyl)-1-phenylpropylidene]hydrazinecarboxamide
-
 Capra hircus
(2E)-2-[3-(3-nitrophenyl)-1-phenylpropylidene]hydrazinecarboxamide
-
 Capra hircus
(2E)-2-[3-(4-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide
-
 Capra hircus
(2E)-2-[3-(4-methylphenyl)-1-phenylpropylidene]hydrazinecarboxamide
-
 Capra hircus
(2E)-2-[3-(4-nitrophenyl)-1-phenylpropylidene]hydrazinecarboxamide
-
 Capra hircus
(2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-one
-
 Capra hircus
(2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-one
-
 Capra hircus
(2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-one
-
 Capra hircus
(2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-one
-
 Capra hircus
(2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-one
-
 Capra hircus
(2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one
-
 Capra hircus
(2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one
-
 Capra hircus
(2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-one
-
 Capra hircus
(2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one
-
 Capra hircus
(2Z)-2-[(2E)-1,3-diphenylprop-2-en-1-ylidene]hydrazinecarboxamide
-
 Capra hircus
(2Z)-2-[(2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide
-
 Capra hircus
(2Z)-2-[(2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide
-
 Capra hircus
(2Z)-2-[(2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide
-
 Capra hircus
(2Z)-2-[(2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide
-
 Capra hircus
(2Z)-2-[(2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide
-
 Capra hircus
(2Z)-2-[(2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide
-
 Capra hircus
(2Z)-2-[(2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide
-
 Capra hircus
(2Z)-2-[(2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide
-
 Capra hircus
3,5-diphenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
5-(2-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
5-(2-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
5-(3-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
5-(3-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
5-(3-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
5-(4-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
5-(4-methylphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
5-(4-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide
-
 Capra hircus
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

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

Organism

Organism UniProt Comment Textmining
Capra hircus A0A060INS8
-
-

Purification (Commentary)

Purification (Comment) Organism
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

Source Tissue Comment Organism Textmining
liver
-
 Capra hircus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.024
-
 purified cathepsin H, pH 6.0, 37°C 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
0.021
-
 (2E)-2-[3-(4-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.023
-
 (2Z)-2-[(2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.025
-
 5-(3-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.029
-
 (2Z)-2-[(2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.032
-
 (2E)-2-[3-(4-nitrophenyl)-1-phenylpropylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.033
-
 (2E)-2-[3-(2-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.033
-
 (2E)-2-[3-(3-nitrophenyl)-1-phenylpropylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.038
-
 5-(3-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.04
-
 (2E)-2-[3-(4-methylphenyl)-1-phenylpropylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.04
-
 5-(2-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.043
-
 (2Z)-2-[(2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.043
-
 5-(3-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.045
-
 (2Z)-2-[(2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.048
-
 5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.048
-
 5-(4-methylphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.054
-
 (2E)-2-[3-(2-methoxyphenyl)-1-phenylpropylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.054
-
 (2Z)-2-[(2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.06
-
 (2E)-2-[3-(3-chlorophenyl)-1-phenylpropylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.06
-
 (2E)-3-(3-nitrophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C Capra hircus
0.06
-
 5-(2-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.06
-
 5-(4-nitrophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.066
-
 (2E)-2-(1,3-diphenylpropylidene)hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.066
-
 (2E)-2-[3-(3-methoxyphenyl)-1-phenylpropylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.066
-
 (2Z)-2-[(2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.066
-
 5-(4-chlorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.074
-
 (2Z)-2-[(2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.083
-
 (2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C Capra hircus
0.096
-
 (2Z)-2-[(2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.1
-
 (2E)-3-(2-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C Capra hircus
0.1
-
 (2E)-3-(4-nitrophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C Capra hircus
0.1
-
 (2Z)-2-[(2E)-1,3-diphenylprop-2-en-1-ylidene]hydrazinecarboxamide pH 6.0, 37°C Capra hircus
0.11
-
 (2E)-3-(2-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C Capra hircus
0.11
-
 (2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C Capra hircus
0.138
-
 (2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C Capra hircus
0.151
-
 (2E)-3-(4-methylphenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C Capra hircus
0.192
-
 3,5-diphenyl-4,5-dihydro-1H-pyrazole-1-carboxamide pH 6.0, 37°C Capra hircus
0.263
-
 (2E)-1,3-diphenylprop-2-en-1-one pH 6.0, 37°C Capra hircus
0.312
-
 (2E)-3-(3-chlorophenyl)-1-phenylprop-2-en-1-one pH 6.0, 37°C Capra hircus