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Literature summary extracted from

  • Raghav, N.; Garg, S.
    N-formylpyrazolines and N-benzoylpyrazolines as novel inhibitors of mammalian cathepsin B and cathepsin H (2014), Bioorg. Chem., 57, 43-50.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.1 N-benzoyl-3,5-diphenylpyrazoline
-
 Capra hircus
3.4.22.1 N-benzoyl-5-(2-chloro phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-benzoyl-5-(2-methoxyphenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-benzoyl-5-(2-nitrophenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-benzoyl-5-(3-chloro phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-benzoyl-5-(3-methoxy phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-benzoyl-5-(3-nitrophenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-benzoyl-5-(4-chloro phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-benzoyl-5-(4-methoxy phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-benzoyl-5-(4-nitrophenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-3,5-diphenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-5-(2-chlorophenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-5-(2-methoxyphenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-5-(2-nitrophenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-5-(3-chlorophenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-5-(3-methoxyphenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-5-(3-nitrophenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-5-(4-chlorophenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-5-(4-methoxyphenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.1 N-formyl-5-(4-nitrophenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.16 N-benzoyl-3,5-diphenylpyrazoline 66.19% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-benzoyl-5-(2-chloro phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.16 N-benzoyl-5-(2-chlorophenyl)-3-phenylpyrazoline 55.13% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-benzoyl-5-(2-methoxyphenyl)-3-phenylpyrazoline 79.37% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-benzoyl-5-(2-nitrophenyl)-3-phenylpyrazoline 34.77% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-benzoyl-5-(3-chloro phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.16 N-benzoyl-5-(3-chlorophenyl)-3-phenylpyrazoline 44.2% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-benzoyl-5-(3-methoxy phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.16 N-benzoyl-5-(3-methoxyphenyl)-3-phenylpyrazoline 76.06% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-benzoyl-5-(3-nitrophenyl)-3-phenylpyrazoline 27.49% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-benzoyl-5-(4-chloro phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.16 N-benzoyl-5-(4-chlorophenyl)-3-phenylpyrazoline 62.47% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-benzoyl-5-(4-methoxy phenyl)-3-phenylpyrazoline
-
 Capra hircus
3.4.22.16 N-benzoyl-5-(4-methoxyphenyl)-3-phenylpyrazoline 69.69% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-benzoyl-5-(4-nitrophenyl)-3-phenylpyrazoline 28.77% residual activity at 0.01 mM Capra hircus
3.4.22.16 N-formyl-3,5-diphenylpyrazoline 76.78% residual activity at 10 mM Capra hircus
3.4.22.16 N-formyl-5-(2-chlorophenyl)-3-phenylpyrazoline 61.38% residual activity at 10 mM Capra hircus
3.4.22.16 N-formyl-5-(2-methoxyphenyl)-3-phenylpyrazoline 92.97% residual activity at 0.001 mM Capra hircus
3.4.22.16 N-formyl-5-(2-nitrophenyl)-3-phenylpyrazoline 30.2% residual activity at 0.001 mM Capra hircus
3.4.22.16 N-formyl-5-(3-chlorophenyl)-3-phenylpyrazoline 49.57% residual activity at 0.001 mM Capra hircus
3.4.22.16 N-formyl-5-(3-methoxyphenyl)-3-phenylpyrazoline 86.03% residual activity at 0.001 mM Capra hircus
3.4.22.16 N-formyl-5-(3-nitrophenyl)-3-phenylpyrazoline 14.15% residual activity at 0.001 mM Capra hircus
3.4.22.16 N-formyl-5-(4-chlorophenyl)-3-phenylpyrazoline 69.38% residual activity at 0.001 mM Capra hircus
3.4.22.16 N-formyl-5-(4-methoxyphenyl)-3-phenylpyrazoline 80.06% residual activity at 0.001 mM Capra hircus
3.4.22.16 N-formyl-5-(4-nitrophenyl)-3-phenylpyrazoline 27.64% residual activity at 0.001 mM Capra hircus

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.22.16 ammonium sulfate precipitation, CM Sephadex column chromatography, C-5 column chromatography, DEAE Sephadex A-5 column chromatography, and Sephadex G-1 and gel filtration 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 0.01115
-
 pH 6, 37°C Capra hircus
3.4.22.16 0.02291
-
 pH 7, 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 alpha-N-benzoyl-DL-arginine-2-naphthylamide + H2O
-
 Capra hircus alpha-N-benzoyl-DL-arginine + 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 6
-
 assay at Capra hircus
3.4.22.16 7
-
 assay at Capra hircus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.22.1 0.0000011
-
 N-formyl-5-(3-nitrophenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.0000113
-
 N-formyl-5-(4-nitrophenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.0000141
-
 N-formyl-5-(2-nitrophenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.0000146
-
 N-formyl-5-(3-chlorophenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.000018
-
 N-formyl-5-(2-chlorophenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.0000211
-
 N-formyl-5-(4-chlorophenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.0000227
-
 N-formyl-3,5-diphenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.0000448
-
 N-formyl-5-(4-methoxyphenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.0000455
-
 N-formyl-5-(3-methoxyphenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.0000668
-
 N-formyl-5-(2-methoxyphenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.000195
-
 N-benzoyl-5-(3-nitrophenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.000287
-
 N-benzoyl-5-(4-nitrophenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.000572
-
 N-benzoyl-5-(2-nitrophenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.000677
-
 N-benzoyl-5-(3-chloro phenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.000775
-
 N-benzoyl-5-(2-chloro phenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.000925
-
 N-benzoyl-5-(4-chloro phenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.00115
-
 N-benzoyl-3,5-diphenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.001277
-
 N-benzoyl-5-(4-methoxy phenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.001594
-
 N-benzoyl-5-(3-methoxy phenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.1 0.004901
-
 N-benzoyl-5-(2-methoxyphenyl)-3-phenylpyrazoline pH 6, 37°C Capra hircus
3.4.22.16 0.0000519
-
 N-formyl-5-(3-nitrophenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.0000519
-
 N-formyl-5-(3-nitrophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.000058
-
 N-formyl-5-(4-nitrophenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.000058
-
 N-formyl-5-(4-nitrophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.0000963
-
 N-formyl-5-(2-nitrophenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.0000963
-
 N-formyl-5-(2-nitrophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.00013
-
 N-formyl-5-(3-chlorophenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.00013
-
 N-formyl-5-(3-chlorophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.000135
-
 N-formyl-5-(2-chlorophenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.000135
-
 N-formyl-5-(2-chlorophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.000137
-
 N-formyl-5-(4-chlorophenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.000137
-
 N-formyl-5-(4-chlorophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.000174
-
 N-formyl-3,5-diphenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.000174
-
 N-formyl-3,5-diphenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.000221
-
 N-formyl-5-(4-methoxyphenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.000221
-
 N-formyl-5-(4-methoxyphenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.000272
-
 N-formyl-5-(3-methoxyphenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.000272
-
 N-formyl-5-(3-methoxyphenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.000387
-
 N-formyl-5-(2-methoxyphenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.000387
-
 N-formyl-5-(2-methoxyphenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.00098
-
 N-benzoyl-5-(3-nitrophenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.00098
-
 N-benzoyl-5-(3-nitrophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.00127
-
 N-benzoyl-5-(4-nitrophenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.00127
-
 N-benzoyl-5-(4-nitrophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.00144
-
 N-benzoyl-5-(2-nitrophenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.00144
-
 N-benzoyl-5-(2-nitrophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.00181
-
 N-benzoyl-5-(3-chloro phenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.00181
-
 N-benzoyl-5-(3-chlorophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.00189
-
 N-benzoyl-5-(2-chloro phenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.00189
-
 N-benzoyl-5-(2-chlorophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.00301
-
 N-benzoyl-5-(4-chloro phenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.00301
-
 N-benzoyl-5-(4-chlorophenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.0032
-
 N-benzoyl-3,5-diphenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.0032
-
 N-benzoyl-3,5-diphenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.0041
-
 N-benzoyl-5-(4-methoxy phenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.0041
-
 N-benzoyl-5-(4-methoxyphenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.00503
-
 N-benzoyl-5-(3-methoxy phenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.00503
-
 N-benzoyl-5-(3-methoxyphenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus
3.4.22.16 0.00965
-
 N-benzoyl-5-(2-methoxyphenyl)-3-phenylpyrazoline pH 7, 37°C Capra hircus
3.4.22.16 0.00965
-
 N-benzoyl-5-(2-methoxyphenyl)-3-phenylpyrazoline in 0.1 M acetate buffer, at pH 5.0 and 37°C Capra hircus