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Literature summary for 3.4.22.28 extracted from

  • Im, I.; Lee, E.S.; Choi, S.J.; Lee, J.Y.; Kim, Y.C.
    Structure-activity relationships of heteroaromatic esters as human rhinovirus 3C protease inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 3632-3636.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Human rhinovirus sp.

Inhibitors

Inhibitors Comment Organism Structure
2-aminopyridin-3-yl furan-2-carboxylate 24% inhibition at 0.001 mM Human rhinovirus sp.
2-carbamoylpyridin-3-yl furan-2-carboxylate 14% inhibition at 0.001 mM Human rhinovirus sp.
2-oxo-1,2-dihydroquinolin-4-yl furan-2-carboxylate 98% inhibition at 0.001 mM Human rhinovirus sp.
3-carbamoylphenyl furan-2-carboxylate 5% inhibition at 0.001 mM Human rhinovirus sp.
5-bromopyridin-3-yl (2E)-3-phenylprop-2-enoate 63% inhibition at 0.001 mM Human rhinovirus sp.
5-bromopyridin-3-yl 3-phenylpropanoate 34% inhibition at 0.001 mM Human rhinovirus sp.
5-bromopyridin-3-yl furan-2-carboxylate most potent inhibitor, 90% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 1H-pyrazole-3-carboxylate 82% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 2-(diphenylmethyl)-4-ethoxy-1,3-oxazole-5-carboxylate 5% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 2-benzyl-4-ethoxy-1,3-oxazole-5-carboxylate 5% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 3-[4-(trifluoromethyl)phenyl]-3H-pyrrole-5-carboxylate 40% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 4-ethoxy-2-(naphthalen-2-yl)-1,3-oxazole-5-carboxylate 34% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 4-ethoxy-2-[(E)-2-phenylethenyl]-1,3-oxazole-5-carboxylate 87% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 5-(4-chlorophenyl)furan-2-carboxylate 89% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 5-(4-methylphenyl)furan-2-carboxylate 79% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 5-(4-nitrophenyl)furan-2-carboxylate 60% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl 5-phenylfuran-2-carboxylate 80% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl benzoate 59% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl furan-2-carboxylate 87% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl naphthalene-1-carboxylate 75% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl naphthalene-2-carboxylate 80% inhibition at 0.001 mM Human rhinovirus sp.
5-chloropyridin-3-yl thiophene-2-carboxylate 64% inhibition at 0.001 mM Human rhinovirus sp.
pyridin-3-yl furan-2-carboxylate 8% inhibition at 0.001 mM Human rhinovirus sp.
rupintrivir AG7088 Human rhinovirus sp.

Organism

Organism UniProt Comment Textmining
Human rhinovirus sp.
-
-
-

Purification (Commentary)

Purification (Comment) Organism
using the IMPACT-CN system Human rhinovirus sp.

Synonyms

Synonyms Comment Organism
3C protease
-
Human rhinovirus sp.
3Cpro
-
Human rhinovirus sp.

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00008
-
in 50 mM Tris (pH 7.6), 1 mM EDTA, at 30°C Human rhinovirus sp. 5-bromopyridin-3-yl furan-2-carboxylate
0.0002
-
in 50 mM Tris (pH 7.6), 1 mM EDTA, at 30°C Human rhinovirus sp. 2-oxo-1,2-dihydroquinolin-4-yl furan-2-carboxylate
0.00029
-
in 50 mM Tris (pH 7.6), 1 mM EDTA, at 30°C Human rhinovirus sp. 5-chloropyridin-3-yl 1H-pyrazole-3-carboxylate
0.00069
-
in 50 mM Tris (pH 7.6), 1 mM EDTA, at 30°C Human rhinovirus sp. 5-chloropyridin-3-yl 4-ethoxy-2-[(E)-2-phenylethenyl]-1,3-oxazole-5-carboxylate
0.00071
-
in 50 mM Tris (pH 7.6), 1 mM EDTA, at 30°C Human rhinovirus sp. 5-chloropyridin-3-yl naphthalene-2-carboxylate