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Literature summary for 2.7.1.1 extracted from

  • Grimsby, J.; Berthel, S.J.; Sarabu, R.
    Glucokinase activators for the potential treatment of type 2 diabetes (2008), Curr. Top. Med. Chem., 8, 1524-1532.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
(2R)-3-cyclopentyl-2-[4-(methylsulfonyl)phenyl]-N-(1,3-thiazol-2-yl)propanamide} RO0281675, 1.5fold change in Vmax or kcat at 0.003 mM Homo sapiens
(R)-2-(4-(methylsulfonyl)phenyl)-3-((R)-3-oxocyclopentyl)-N-(pyrazin-2-yl)propanamide piragliatin Homo sapiens
(S)-2-(4-(cyclopropylsulfonyl)phenyl)-N-(5-fluorothiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide PSN-GK1, 1.1fold change in Vmax or kcat at 0.0001 mM Homo sapiens
2-amino-4-fluoro-5-((1-methyl-1H-imidazol-2-yl)thio)-N-(thiazol-2-yl)benzamide 1.6fold change in Vmax or kcat at 0.03 mM Homo sapiens
2-amino-5-((4-methyl-4H-1,2,4-triazol-3-yl)thio)-N-(5-methylthiazol-2-yl)benzamide 1.3fold change in Vmax or kcat at 0.01 mM Homo sapiens
5-({3-(propan-2-yloxy)-5-[2-(thiophen-3-yl)ethoxy]benzoyl}amino)-1,3,4-thiadiazole-2-carboxylic acid
-
Homo sapiens
6-(3-(((S)-1-methoxypropan-2-yl)oxy)-5-(((S)-1-phenylpropan-2-yl)oxy)benzamido)nicotinic acid GKA50, 0.94fold change in Vmax or kcat at 0.03 mM Homo sapiens
6-({3-(propan-2-yloxy)-5-[2-(thiophen-3-yl)ethoxy]benzoyl}amino)pyridine-3-carboxylic acid GKA22 Homo sapiens
6-ethoxy-N-(1-methyl-1H-pyrrol-3-yl)-quinazolin-4-amine 0.95fold change in Vmax or kcat at 0.05 mM Homo sapiens
6-ethoxy-N-(pyridin-2-yl)-quinazolin-4-amine 0.62fold change in Vmax or kcat at 0.05 mM Homo sapiens
6-isopropoxy-N-(1-methyl-1H-pyrrol-3-yl)quinazolin-4-amine 0.8fold change in Vmax or kcat at 0.05 mM Homo sapiens
6-{[3-(2-methylpropoxy)-5-(propan-2-yloxy)benzoyl]amino}pyridine-3-carboxylic acid
-
Homo sapiens
LY-2121260
-
Homo sapiens
RO-0275145
-
Homo sapiens
RO-0281675
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
glucokinase regulatory protein competitive inhibitor Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-
pancreatic beta cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + 2-deoxy-D-glucose
-
Homo sapiens ADP + 2-deoxy-D-glucose 6-phosphate
-
?
ATP + D-fructose
-
Homo sapiens ADP + D-fructose 6-phosphate
-
?
ATP + D-glucose
-
Homo sapiens ADP + D-glucose 6-phosphate
-
?
ATP + D-mannose
-
Homo sapiens ADP + D-mannose 6-phosphate
-
?

Synonyms

Synonyms Comment Organism
ATP: D-glucose 6-phosphotransferase
-
Homo sapiens
glucokinase
-
Homo sapiens
hexokinase D
-
Homo sapiens
hexokinase IV
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens