Protease-Activated Receptors (PAR)

Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.

ML-161 is an inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets).

I-191 is a potent, selective protease-activated receptor 2 (PAR2) antagonist.

GB110 is a Novel potent non-peptide PAR2 agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.

GB-88 is a novel selective, orally available PAR2 antagonist, inhibits PAR2 activated Ca2+ release with an IC50 of 2 ?M.

UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM).

AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.

AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation.