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Literature summary extracted from

  • Raghav, N.; Singh, M.
    Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H (2014), Eur. J. Med. Chem., 77, 231-242.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.1 2-chlorobenzohydrazide competitive inhibition Capra hircus
3.4.22.1 2-methoxybenzohydrazide competitive inhibition Capra hircus
3.4.22.1 3,5-diphenyl-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.1 3-(2-hydroxy-3-methylphenyl)-5-(2-hydroxy-3-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.1 3-(2-methylphenyl)-5-(2-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.1 3-(3-aminophenyl)-5-(3-aminophenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.1 3-(3-methylphenyl)-5-(3-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.1 3-(4-chlorophenyl)-5-(4-chlorophenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.1 3-(4-methylphenyl)-5-(4-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.1 3-phenyl-5-(3-nitrophenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.1 3-phenyl-5-(4-nitrophenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.1 4-hydroxybenzohydrazide competitive inhibition Capra hircus
3.4.22.1 4-methoxybenzohydrazide competitive inhibition Capra hircus
3.4.22.1 phenylacetyl hydrazine competitive inhibition Capra hircus
3.4.22.16 2-chlorobenzohydrazide non-competitive inhibition; non-competitive inhibition, 89.46% residual activity at 0.01 mM Capra hircus
3.4.22.16 2-methoxybenzohydrazide non-competitive inhibition; non-competitive inhibition, 97.83% residual activity at 0.01 mM Capra hircus
3.4.22.16 3,5-diphenyl-4-amino-1,2,4-triazole non-competitive inhibition; non-competitive inhibition, 69.73% residual activity at 0.01 mM Capra hircus
3.4.22.16 3-(2'-hydroxy-3'-methylphenyl)-5-(2'-hydroxy-3'-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition, 88.11% residual activity at 0.01 mM Capra hircus
3.4.22.16 3-(2'-methylphenyl)-5-(2'-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition, 82.97% residual activity at 0.01 mM Capra hircus
3.4.22.16 3-(2-hydroxy-3-methylphenyl)-5-(2-hydroxy-3-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.16 3-(2-methylphenyl)-5-(2-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.16 3-(3'-aminophenyl)-5-(3'-aminophenyl)-4-amino-1,2,4-triazole non-competitive inhibition, 16.37% residual activity at 0.01 mM Capra hircus
3.4.22.16 3-(3'-methylphenyl)-5-(3'-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition, 79.45% residual activity at 0.01 mM Capra hircus
3.4.22.16 3-(3'-nitrophenyl)-5-(3'-nitrophenyl)-4-amino-1,2,4-triazole non-competitive inhibition, 45.13% residual activity at 0.01 mM Capra hircus
3.4.22.16 3-(3-aminophenyl)-5-(3-aminophenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.16 3-(3-methylphenyl)-5-(3-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.16 3-(4'-chlorophenyl)-5-(4'-chlorophenyl)-4-amino-1,2,4-triazole non-competitive inhibition, 24.35% residual activity at 0.01 mM Capra hircus
3.4.22.16 3-(4'-methylphenyl)-5-(4'-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition, 89.46% residual activity at 0.01 mM Capra hircus
3.4.22.16 3-(4-chlorophenyl)-5-(4-chlorophenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.16 3-(4-methylphenyl)-5-(4-methylphenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.16 3-phenyl-5-(3-nitrophenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.16 3-phenyl-5-(4'-nitrophenyl)-4-amino-1,2,4-triazole non-competitive inhibition, 78.11% residual activity at 0.01 mM Capra hircus
3.4.22.16 3-phenyl-5-(4-nitrophenyl)-4-amino-1,2,4-triazole non-competitive inhibition Capra hircus
3.4.22.16 4-hydroxybenzohydrazide non-competitive inhibition; non-competitive inhibition, 91.62% residual activity at 0.01 mM Capra hircus
3.4.22.16 4-methoxybenzohydrazide non-competitive inhibition; non-competitive inhibition, 45% residual activity at 0.01 mM Capra hircus
3.4.22.16 Leu-CH2-Cl complete inhibition at 0.01 mM Capra hircus
3.4.22.16 leupeptin complete inhibition at 0.01 mM Capra hircus
3.4.22.16 phenylacetyl hydrazine non-competitive inhibition; non-competitive inhibition, 81.08% residual activity at 0.01 mM Capra hircus

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.1 Capra hircus H9B8T9
-
-
3.4.22.16 Capra hircus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.22.1 liver
-
 Capra hircus
-
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
3.4.22.1 0.01038
-
 pH 5, 37°C Capra hircus
3.4.22.16 0.02256
-
 pH 5, 37°C Capra hircus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.1 N-benzoyl-L-Arg-2-naphthylamide + H2O
-
 Capra hircus N-benzoyl-L-Arg + 2-naphthylamine
-
 ?
3.4.22.16 L-Leu-2-naphthylamide + H2O
-
 Capra hircus L-Leu + 2-naphthylamine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.1 cathepsin B
-
 Capra hircus
3.4.22.16 cathepsin H
-
 Capra hircus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.22.1 37
-
 assay at Capra hircus
3.4.22.16 37
-
 assay at Capra hircus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.22.1 5
-
 assay at Capra hircus
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
3.4.22.1 0.00064
-
 4-methoxybenzohydrazide pH 5, 37°C Capra hircus
3.4.22.1 0.00087
-
 phenylacetyl hydrazine pH 5, 37°C Capra hircus
3.4.22.1 0.00095
-
 3-(3-aminophenyl)-5-(3-aminophenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.1 0.00136
-
 2-chlorobenzohydrazide pH 5, 37°C Capra hircus
3.4.22.1 0.00143
-
 3-phenyl-5-(3-nitrophenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.1 0.0019
-
 4-hydroxybenzohydrazide pH 5, 37°C Capra hircus
3.4.22.1 0.0024
-
 3-(4-chlorophenyl)-5-(4-chlorophenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.1 0.0032
-
 3-(2-hydroxy-3-methylphenyl)-5-(2-hydroxy-3-methylphenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.1 0.0048
-
 3-phenyl-5-(4-nitrophenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.1 0.008
-
 3-(4-methylphenyl)-5-(4-methylphenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.1 0.0127
-
 2-methoxybenzohydrazide pH 5, 37°C Capra hircus
3.4.22.1 0.0149
-
 3-(2-methylphenyl)-5-(2-methylphenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.1 0.0385
-
 3-(3-methylphenyl)-5-(3-methylphenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.1 0.1205
-
 3,5-diphenyl-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.002
-
 3-(3'-aminophenyl)-5-(3'-aminophenyl)-4-amino-1,2,4-triazole at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.002
-
 3-(3-aminophenyl)-5-(3-aminophenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.0033
-
 3-(4'-chlorophenyl)-5-(4'-chlorophenyl)-4-amino-1,2,4-triazole at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0033
-
 3-(4-chlorophenyl)-5-(4-chlorophenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.0082
-
 4-methoxybenzohydrazide at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0082
-
 4-methoxybenzohydrazide pH 5, 37°C Capra hircus
3.4.22.16 0.0086
-
 3-(3'-nitrophenyl)-5-(3'-nitrophenyl)-4-amino-1,2,4-triazole at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0086
-
 3-phenyl-5-(3-nitrophenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.0232
-
 3,5-diphenyl-4-amino-1,2,4-triazole at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0232
-
 3,5-diphenyl-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.0364
-
 3-phenyl-5-(4'-nitrophenyl)-4-amino-1,2,4-triazole at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0364
-
 3-phenyl-5-(4-nitrophenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.0387
-
 3-(3'-methylphenyl)-5-(3'-methylphenyl)-4-amino-1,2,4-triazole at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0387
-
 3-(3-methylphenyl)-5-(3-methylphenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.0425
-
 phenylacetyl hydrazine at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0425
-
 phenylacetyl hydrazine pH 5, 37°C Capra hircus
3.4.22.16 0.0532
-
 3-(2'-methylphenyl)-5-(2'-methylphenyl)-4-amino-1,2,4-triazole at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0532
-
 3-(2-methylphenyl)-5-(2-methylphenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.0781
-
 3-(2'-hydroxy-3'-methylphenyl)-5-(2'-hydroxy-3'-methylphenyl)-4-amino-1,2,4-triazole at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0781
-
 3-(2-hydroxy-3-methylphenyl)-5-(2-hydroxy-3-methylphenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.0901
-
 2-chlorobenzohydrazide at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0901
-
 3-(4'-methylphenyl)-5-(4'-methylphenyl)-4-amino-1,2,4-triazole at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.0901
-
 2-chlorobenzohydrazide pH 5, 37°C Capra hircus
3.4.22.16 0.0901
-
 3-(4-methylphenyl)-5-(4-methylphenyl)-4-amino-1,2,4-triazole pH 5, 37°C Capra hircus
3.4.22.16 0.1123
-
 4-hydroxybenzohydrazide at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.1123
-
 4-hydroxybenzohydrazide pH 5, 37°C Capra hircus
3.4.22.16 0.588
-
 2-methoxybenzohydrazide at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.588
-
 2-methoxybenzohydrazide pH 5, 37°C Capra hircus