UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP)[1]. IC50: 4 nM (PAR4)[1]Kd: 1.4 nM (PAR4)[1]
[1]. Miller MM, et al. Discovery of Potent Protease-Activated Receptor 4 Antagonists with in vivo Antithrombotic Efficacy. J Med Chem. 2019 Jun 27.