Glucokinase

PF-04991532 is a potent, hepatoselective glucokinase activator with EC50s of 80 and 100 nM in human and rat, respectively.

GKA50 is a potent activator of glucokinase

PF-04937319 is a glucokinase activator (GKA) with EC50 value of 154.4 ?μM, one of the most promising strategies for the treatment of type 2 diabetes mellitus.

Piragliatin is a novel glucokinase activator, lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus

Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.

AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.

MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 has potential in the treatment of type 2 diabetes.

Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM.

AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM.

ML266 (CID-46943215) is a activator of glucocerebrosidase (GCase) that does not inhibit the enzyme??s action but can still facilitates its translocation to the lysosome.

Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes.