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Literature summary for 4.4.1.5 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
Search for more literature for 4.4.1.5

Inhibitors

Inhibitors Comment Organism Structure
1'-hydroxy-6'-phenyl-3,4'-bipyridin-2'(1'H)-one
-
 Homo sapiens
1-hydroxy-4,6-diphenylpyridin-2(1H)-one
-
 Homo sapiens
1-hydroxy-4-phenyl-6-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyridin-2(1H)-one
-
 Homo sapiens
1-hydroxy-6-(1-pentyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-4-phenylpyridin-2(1H)-one
-
 Homo sapiens
1-hydroxy-6-(1H-indol-5-yl)-4-phenylpyridin-2(1H)-one
-
 Homo sapiens
1-hydroxy-6-phenyl-4-(thiophen-3-yl)pyridin-2(1H)-one
-
 Homo sapiens
1-hydroxy-6-phenyl-4-[4-(trifluoromethyl)phenyl]pyridin-2(1H)-one
-
 Homo sapiens
1-hydroxy-6-[1-(2-methoxyethyl)-1H-indol-5-yl]-4-phenylpyridin-2(1H)-one
-
 Homo sapiens
1-hydroxy-6-[1-(2-methoxyethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-4-phenylpyridin-2(1H)-one
-
 Homo sapiens
1-hydroxy-6-[1-(3-methoxypropyl)-1H-indol-5-yl]-4-phenylpyridin-2(1H)-one
-
 Homo sapiens
1-hydroxy-6-[1-(3-methoxypropyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-4-phenylpyridin-2(1H)-one
-
 Homo sapiens
3-[[5-(1-hydroxy-6-oxo-4-phenyl-1,6-dihydropyridin-2-yl)-1H-indol-1-yl]methyl]benzamide
-
 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
-
 Homo sapiens
4,6-diphenyl-N-hydroxypyridone a lead compound for non-peptidic inhibitor screening against glyoxalase I Homo sapiens
4-(biphenyl-4-yl)-1-hydroxy-6-phenylpyridin-2(1H)-one
-
 Homo sapiens
4-(but-1-yn-1-yl)-1-hydroxy-6-phenylpyridin-2(1H)-one
-
 Homo sapiens
4-butyl-1-hydroxy-6-phenylpyridin-2(1H)-one
-
 Homo sapiens
6-(1-butyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1-hydroxy-4-phenylpyridin-2(1H)-one
-
 Homo sapiens
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
S-(p-bromobenzyl)glutathione
-
 Homo sapiens

Metals/Ions

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glutathione + methylglyoxal
-
 Homo sapiens (R)-S-lactoylglutathione
-
 ?
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

Synonyms Comment Organism
Glo1
-
 Homo sapiens
glyoxalase I
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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
0.00025
-
 pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-(1H-indol-5-yl)-4-phenylpyridin-2(1H)-one
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
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
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
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
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
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
0.00119
-
 pH and temperature not specified in the publication Homo sapiens 1-hydroxy-4,6-diphenylpyridin-2(1H)-one
0.00152
-
 pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-phenyl-4-(thiophen-3-yl)pyridin-2(1H)-one
0.00813
-
 pH and temperature not specified in the publication Homo sapiens 1-hydroxy-6-phenyl-4-[4-(trifluoromethyl)phenyl]pyridin-2(1H)-one
0.00828
-
 pH and temperature not specified in the publication Homo sapiens 1'-hydroxy-6'-phenyl-3,4'-bipyridin-2'(1'H)-one
0.0084
-
 pH and temperature not specified in the publication Homo sapiens 4-(biphenyl-4-yl)-1-hydroxy-6-phenylpyridin-2(1H)-one
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
0.01
-
 pH and temperature not specified in the publication Homo sapiens 4-butyl-1-hydroxy-6-phenylpyridin-2(1H)-one
0.021
-
 pH and temperature not specified in the publication Homo sapiens S-(p-bromobenzyl)glutathione