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Literature summary extracted from

  • Singh, M.; Raghav, N.
    2,3-Dihydroquinazolin-4(1H)-one derivatives as potential non-peptidyl inhibitors of cathepsins B and H (2015), Bioorg. Chem., 59, 12-22.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.16 1H-spiro(cyclohexane-1,2-quinazolin)-4(3H)-one competitive inhibition, 94.86% residual activity at 0.1 mM Capra hircus
3.4.22.16 2-(4-(dimethylamino)phenyl)-2,3-dihydroquinazolin-4(1H)-one competitive inhibition, 88.37% residual activity at 0.1 mM Capra hircus
3.4.22.16 2-(4-bromophenyl)-2,3-dihydroquinazolin-4(1H)-one competitive inhibition, 91.62% residual activity at 0.1 mM Capra hircus
3.4.22.16 2-(4-chlorophenyl)-2,3-dihydroquinazolin-4(1H)-one competitive inhibition, 98.11% residual activity at 0.1 mM Capra hircus
3.4.22.16 2-(4-fluorophenyl)-2,3-dihydroquinazolin-4(1H)-one competitive inhibition, 94.05% residual activity at 0.1 mM Capra hircus
3.4.22.16 2-(4-methoxyphenyl)-2,3-dihydroquinazolin-4(1H)-one competitive inhibition, 95.94% residual activity at 0.1 mM Capra hircus
3.4.22.16 2-(4-methylphenyl)-2,3-dihydroquinazolin-4(1H)-one competitive inhibition, 39.18% residual activity at 0.1 mM Capra hircus
3.4.22.16 2-(4-nitrophenyl)-2,3-dihydroquinazolin-4(1H)-one competitive inhibition, 81.89% residual activity at 0.1 mM Capra hircus
3.4.22.16 2-phenyl-2,3-dihydroquinazolin-4(1H)-one competitive inhibition, 79.73% residual activity at 0.1 mM Capra hircus

Organism

EC Number Organism UniProt Comment Textmining
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-50 column chromatography, DEAE-Sephadex A-50., and Sephadex G-100, and gel filtration Capra hircus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.22.16 liver
-
 Capra hircus
-

Substrates and Products (Substrate)

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

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.22.16 0.0025
-
 2-(4-methylphenyl)-2,3-dihydroquinazolin-4(1H)-one at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.00818
-
 2-(4-fluorophenyl)-2,3-dihydroquinazolin-4(1H)-one at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.01042
-
 2-(4-nitrophenyl)-2,3-dihydroquinazolin-4(1H)-one at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.01441
-
 2-phenyl-2,3-dihydroquinazolin-4(1H)-one at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.01858
-
 2-(4-(dimethylamino)phenyl)-2,3-dihydroquinazolin-4(1H)-one at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.02325
-
 2-(4-chlorophenyl)-2,3-dihydroquinazolin-4(1H)-one at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.05263
-
 2-(4-bromophenyl)-2,3-dihydroquinazolin-4(1H)-one at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.05682
-
 2-(4-methoxyphenyl)-2,3-dihydroquinazolin-4(1H)-one at pH 7.0 and 37°C Capra hircus
3.4.22.16 0.09009
-
 1H-spiro(cyclohexane-1,2-quinazolin)-4(3H)-one at pH 7.0 and 37°C Capra hircus