PF-04991532 is a novel, potent, hepatoselective glucokinase activator with EC50 of 80 and 100 nM in human and rat, respectively.

Dorzagliatin (RO-5305552; HMS-5552; sinogliatin) is an investigational antidiabetic agent acting as a dual-acting glucokinase activator (GKA) that is able to improves glycaemic control and pancreatic β-cell function in type 2 diabete.

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

AMG-3969 is a potent, novel and metabolically stable disruptor of glucokinase-glucokinase regulatory protein interaction (GK-GKRP) with IC50 of 4 nM.

MK-0941 mesylate, the mesylate salt of MK0941, is a novel, orally bioactive and allosteric glucokinase activator (GKA) with anti-diabetic effects.