GB-88 is a selective, orally available PAR2 antagonist that inhibits PAR2 activated Ca(2+) release with IC50 of 2 uM.

GB-110 is a potent, non-peptidic agonist of PAR2 that selectively induces PAR2-mediated intracellular Ca(2+) release in HT29 cells with EC50 of 0.28 uM.

E5555 shows potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC values of 0.064 and 0.031 μM respectively.

AZ-8838 (AZ8838) is a potent, and selective PAR2 antagonist with Kd of 125 nM.

AC264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation.