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Literature summary for 2.7.1.1 extracted from

  • Pfefferkorn, J.A.; Lou, J.; Minich, M.L.; Filipski, K.J.; He, M.; Zhou, R.; Ahmed, S.; Benbow, J.; Perez, A.G.; Tu, M.; Litchfield, J.; Sharma, R.; Metzler, K.; Bourbonais, F.; Huang, C.; Beebe, D.A.; Oates, P.J.
    Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle (2009), Bioorg. Med. Chem. Lett., 19, 3247-3252.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
(2R)-2-[4-(cyclopropylsulfonyl)phenyl]-N-(5-fluorothiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide 96% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[3-chloro-4-(ethylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide 26% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-(4,4-difluorocyclohexyl)-N-(5-methylpyridin-2-yl)propanamide 15% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclobutyl-N-(5-methylpyridin-2-yl)propanamide 72% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclohexyl-N-(5-methylpyridin-2-yl)propanamide 46% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyridin-2-yl)propanamide 57% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-4-methyl-N-(5-methylpyridin-2-yl)pentanamide 37% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[3-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)-3-phenylpropanamide 30% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[4-(cyclobutylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyridin-2-yl)propanamide 67% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[4-(cyclobutylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-pyrazin-2-ylpropanamide 66% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[5-chloro-4-(cyclobutylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(1-methyl-1H-pyrazol-3-yl)propanamide 67% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[5-chloro-4-(cyclopropylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(1-methyl-1H-pyrazol-3-yl)propanamide 84% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[5-chloro-4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyridin-2-yl)propanamide 122% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[5-chloro-4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-chloropyridin-2-yl)-3-cyclopentylpropanamide 82% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(1-methyl-1H-pyrazol-3-yl)propanamide 57% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyrazin-2-yl)propanamide 104% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-(5-methylpyridin-2-yl)propanamide 69% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-1,3-thiazol-2-ylpropanamide 42% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-2-[5-chloro-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-3-cyclopentyl-N-1H-pyrazol-3-ylpropanamide 50% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-2-[4-(cyclopropylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide 76% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-2-[4-(cyclopropylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-pyrazin-2-ylpropanamide 94% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-2-[4-(ethylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide 73% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-2-[4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide 65% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-2-[4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-pyridin-2-ylpropanamide 43% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-2-[4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-[5-(trifluoromethyl)pyridin-2-yl]propanamide 35% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-2-[5-methyl-4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide 103% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-2-[5-methyl-4-[(1-methylethyl)sulfonyl]-2-oxopyridin-1(2H)-yl]-N-(5-methylpyridin-2-yl)propanamide 48% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-N-(5-methylpyrazin-2-yl)-2-[4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]propanamide 101% maximum activation above control at 6.5 mM glucose Homo sapiens
(S)-3-cyclopentyl-N-(5-methylpyridin-2-yl)-2-[4-(methylsulfonyl)-2-oxopyridin-1(2H)-yl]propanamide 58% maximum activation above control at 6.5 mM glucose Homo sapiens
2-amino-4-fluoro-5-[(1-methyl-1H-imidazol-2-yl)sulfanyl]-N-(4-methylthiazol-2-yl)benzamide 108% maximum activation above control at 6.5 mM glucose Homo sapiens
6-(3-(((S)-1-methoxypropan-2-yl)oxy)-5-(((S)-1-phenylpropan-2-yl)oxy)benzamido)nicotinic acid 23% maximum activation above control at 6.5 mM glucose Homo sapiens
RO-0281675 81% maximum activation above control at 6.5 mM glucose Homo sapiens
RO-1440 148% maximum activation above control at 6.5 mM glucose Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + D-glucose
-
Homo sapiens ADP + D-glucose 6-phosphate
-
?

Synonyms

Synonyms Comment Organism
glucokinase
-
Homo sapiens
hexokinase IV
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens