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Literature summary for 3.4.22.69 extracted from

  • Konno, H.; Onuma, T.; Nitanai, I.; Wakabayashi, M.; Yano, S.; Teruya, K.; Akaji, K.
    Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor (2017), Bioorg. Med. Chem. Lett., 27, 2746-2751 .
    View publication on PubMed

Protein Variants

Protein Variants Comment Organism
R188I auto-proteolysis resistant mutant Severe acute respiratory syndrome-related coronavirus

Inhibitors

Inhibitors Comment Organism Structure
(R)-N-(E)-3',4',5'-trimethoxy-3-phenylprop-2-enoicserine(benzoyl)cyclohexylamide IC50 value 0.5 mM for cathepsin B, not cytotoxic Severe acute respiratory syndrome-related coronavirus
(R)-N-cinnamoyl serine(benzoyl)cyclohexylamide not inhibitory to cathepsin B at 1 mM, not cytotoxic Severe acute respiratory syndrome-related coronavirus
1,6-di(propan-2-yl)-N-(4-[[4-(prop-2-en-1-yl)-5-sulfanylidene-4,5-dihydro-1H-1,2,4-triazol-3-yl]methyl]-1,3-thiazol-2-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide
-
Severe acute respiratory syndrome-related coronavirus

Organism

Organism UniProt Comment Textmining
Severe acute respiratory syndrome-related coronavirus P0C6X7 human, i.e. SARS-CoV
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.03
-
pH 4.0, temperature not specified in the publication Severe acute respiratory syndrome-related coronavirus (R)-N-cinnamoyl serine(benzoyl)cyclohexylamide
0.043
-
mutant R188I, pH not specified in the publication, temperature not specified in the publication Severe acute respiratory syndrome-related coronavirus 1,6-di(propan-2-yl)-N-(4-[[4-(prop-2-en-1-yl)-5-sulfanylidene-4,5-dihydro-1H-1,2,4-triazol-3-yl]methyl]-1,3-thiazol-2-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide
0.065
-
pH 4.0, temperature not specified in the publication Severe acute respiratory syndrome-related coronavirus (R)-N-(E)-3',4',5'-trimethoxy-3-phenylprop-2-enoicserine(benzoyl)cyclohexylamide