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Literature summary extracted from

  • Chiba, T.; Ohwada, J.; Sakamoto, H.; Kobayashi, T.; Fukami, T.A.; Irie, M.; Miura, T.; Ohara, K.; Koyano, H.
    Design and evaluation of azaindole-substituted N-hydroxypyridones as glyoxalase I inhibitors (2012), Bioorg. Med. Chem. Lett., 22, 7486-7489.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
4.4.1.5 1'-hydroxy-6'-phenyl-3,4'-bipyridin-2'(1'H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-4,6-diphenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-4-phenyl-6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-6-(1-pentyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-6-(1H-indol-5-yl)-4-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-6-phenyl-4-(thiophen-3-yl)pyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-6-phenyl-4-[4-(trifluoromethyl)phenyl]pyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-6-[1-(2-methoxyethyl)-1H-indol-5-yl]-4-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-6-[1-(2-methoxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-4-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-6-[1-(3-methoxypropyl)-1H-indol-5-yl]-4-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 1-hydroxy-6-[1-(3-methoxypropyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-4-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 3-[[5-(1-hydroxy-6-oxo-4-phenyl-1,6-dihydropyridin-2-yl)-1H-indol-1-yl]methyl]benzamide
-
Homo sapiens
4.4.1.5 3-[[5-(1-hydroxy-6-oxo-4-phenyl-1,6-dihydropyridin-2-yl)-1H-pyrrolo[2,3-b]pyridin-1-yl]methyl]benzamide
-
Homo sapiens
4.4.1.5 4,6-diphenyl-N-hydroxypyridone a lead compound for non-peptidic inhibitor screening against glyoxalase I Homo sapiens
4.4.1.5 4-(biphenyl-4-yl)-1-hydroxy-6-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 4-(but-1-yn-1-yl)-1-hydroxy-6-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 4-butyl-1-hydroxy-6-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 6-(1-butyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1-hydroxy-4-phenylpyridin-2(1H)-one
-
Homo sapiens
4.4.1.5 additional information design of 4-(7-azaindole)-substituted 6-phenyl-N-hydroxypyridones, thermodynamic binding parameters, binding modeling using the enzyme's crystal structure, overview. Inhibitory activity of 6-phenyl-N-hydroxypyridones with various substituents at 4-position Homo sapiens
4.4.1.5 S-(p-bromobenzyl)glutathione
-
Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
4.4.1.5 Zn2+ required, zinc enzyme Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
4.4.1.5 glutathione + methylglyoxal Homo sapiens
-
(R)-S-lactoylglutathione
-
?

Organism

EC Number Organism UniProt Comment Textmining
4.4.1.5 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4.4.1.5 glutathione + methylglyoxal
-
Homo sapiens (R)-S-lactoylglutathione
-
?
4.4.1.5 glutathione + methylglyoxal glyoxalase I catalyzes the isomerization of a hemithioacetal, formed from glutathione and methylglyoxal, to lactic acid thioester Homo sapiens (R)-S-lactoylglutathione
-
?

Synonyms

EC Number Synonyms Comment Organism
4.4.1.5 Glo1
-
Homo sapiens
4.4.1.5 glyoxalase I
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
4.4.1.5 0.000011
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-[1-(3-methoxypropyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-4-phenylpyridin-2(1H)-one
4.4.1.5 0.000014
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-[1-(2-methoxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-4-phenylpyridin-2(1H)-one
4.4.1.5 0.00004
-
pH and temperature not specified in the publication Homo sapiens 3-[[5-(1-hydroxy-6-oxo-4-phenyl-1,6-dihydropyridin-2-yl)-1H-pyrrolo[2,3-b]pyridin-1-yl]methyl]benzamide
4.4.1.5 0.00025
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-(1H-indol-5-yl)-4-phenylpyridin-2(1H)-one
4.4.1.5 0.00026
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-[1-(2-methoxyethyl)-1H-indol-5-yl]-4-phenylpyridin-2(1H)-one
4.4.1.5 0.00028
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-4-phenyl-6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyridin-2(1H)-one
4.4.1.5 0.0003
-
pH and temperature not specified in the publication Homo sapiens 6-(1-butyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1-hydroxy-4-phenylpyridin-2(1H)-one
4.4.1.5 0.0003
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-[1-(3-methoxypropyl)-1H-indol-5-yl]-4-phenylpyridin-2(1H)-one
4.4.1.5 0.00048
-
pH and temperature not specified in the publication Homo sapiens 3-[[5-(1-hydroxy-6-oxo-4-phenyl-1,6-dihydropyridin-2-yl)-1H-indol-1-yl]methyl]benzamide
4.4.1.5 0.00051
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-(1-pentyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-phenylpyridin-2(1H)-one
4.4.1.5 0.00119
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-4,6-diphenylpyridin-2(1H)-one
4.4.1.5 0.00152
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-phenyl-4-(thiophen-3-yl)pyridin-2(1H)-one
4.4.1.5 0.00813
-
pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-phenyl-4-[4-(trifluoromethyl)phenyl]pyridin-2(1H)-one
4.4.1.5 0.00828
-
pH and temperature not specified in the publication Homo sapiens 1'-hydroxy-6'-phenyl-3,4'-bipyridin-2'(1'H)-one
4.4.1.5 0.0084
-
pH and temperature not specified in the publication Homo sapiens 4-(biphenyl-4-yl)-1-hydroxy-6-phenylpyridin-2(1H)-one
4.4.1.5 0.01
-
pH and temperature not specified in the publication Homo sapiens 4-(but-1-yn-1-yl)-1-hydroxy-6-phenylpyridin-2(1H)-one
4.4.1.5 0.01
-
pH and temperature not specified in the publication Homo sapiens 4-butyl-1-hydroxy-6-phenylpyridin-2(1H)-one
4.4.1.5 0.021
-
pH and temperature not specified in the publication Homo sapiens S-(p-bromobenzyl)glutathione