Parmodulin 2 (ML161),a probe, is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 inhibits platelet aggregation induced by a PAR1 peptide agonist or by thrombin and has shown cytoprotective effects[1, 2].
[1]. Gandhi DM, et al. Characterization of Protease-Activated Receptor (PAR) ligands: Parmodulins are reversible allosteric inhibitors of PAR1-driven calcium mobilization in endothelial cells. Bioorg Med Chem. 2018 May 15;26(9):2514-2529. [2]. Dockendorff C Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1Receptor. ACS Med Chem Lett. 2012 Mar 8;3(3):232-237.
















