EC Number   |
Activating Compound |
Reference |
|---|
    2.7.1.1 | (2E)-3-cyclopentyl-2-[4-(cyclopropylsulfonyl)phenyl]-N-[4-(1,2-dihydroxyethyl)-1,3-thiazol-2-yl]prop-2-enamide |
- |
703597 |
| 2.7.1.1 | (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 |
702572 |
| 2.7.1.1 | (2R)-3-cyclopentyl-2-[4-(methylsulfonyl)phenyl]-N-(1,3-thiazol-2-yl)propanamide |
activator associates with glucokinase in a glucose-independent fashion. Kinetic assays reveal a lag in enzyme progress curves that is systematically reduced when the enzyme is preincubated with the activator. Activator binding is enthalpically driven. The kcat value of glucokinase is almost fully limited by product release, both in the presence and absence of activator |
737327 |
| 2.7.1.1 | (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 |
703358 |
| 2.7.1.1 | (6-ethoxyquinazolin-4-yl)(1-methyl-1H-pyrazol-3-yl)amine |
increases glucokinase activity at glucose concentrations up to approximately 20 mM |
702236 |
| 2.7.1.1 | (6-ethoxyquinazolin-4-yl)pyridin-2-ylamine |
increases glucokinase activity at glucose concentrations below approximately 7 mM |
702236 |
| 2.7.1.1 | (6-isopropoxyquinazolin-4-yl)(1-methyl-1H-pyrazol-3-yl)amine |
increases glucokinase activity at glucose concentrations up to approximately 20 mM |
702236 |
| 2.7.1.1 | (R)-2-(4-(methylsulfonyl)phenyl)-3-((R)-3-oxocyclopentyl)-N-(pyrazin-2-yl)propanamide |
piragliatin |
703358 |
| 2.7.1.1 | (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 |
703358 |
| 2.7.1.1 | (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 |
702572 |
