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Discovery of Protease-Activated Receptor 4 (PAR4)-Tethered Ligand Antagonists Using Ultralarge Virtual Screening.
Smith ST, Cassada JB, Von Bredow L, Erreger K, Webb EM, Trombley TA, Kalbfleisch JJ, Bender BJ, Zagol-Ikapitte I, Kramlinger VM, Bouchard JL, Mitchell SG, Tretbar M, Shoichet BK, Lindsley CW, Meiler J, Hamm HE. Smith ST, et al. ACS Pharmacol Transl Sci. 2024 Mar 21;7(4):1086-1100. doi: 10.1021/acsptsci.3c00378. eCollection 2024 Apr 12. ACS Pharmacol Transl Sci. 2024. PMID: 38633591
Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against γ-Thrombin.
Temple KJ, Duvernay MT, Young SE, Wen W, Wu W, Maeng JG, Blobaum AL, Stauffer SR, Hamm HE, Lindsley CW. Temple KJ, et al. J Med Chem. 2016 Aug 25;59(16):7690-5. doi: 10.1021/acs.jmedchem.6b00928. Epub 2016 Aug 8. J Med Chem. 2016. PMID: 27482618 Free PMC article.