26960-62-3Relevant articles and documents
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, Kayla J.,Duvernay, Matthew T.,Young, Summer E.,Wen, Wandong,Wu, Wenjun,Maeng, Jae G.,Blobaum, Anna L.,Stauffer, Shaun R.,Hamm, Heidi E.,Lindsley, Craig W.
supporting information, p. 7690 - 7695 (2016/09/04)
Here, we describe the development of a series of highly selective PAR4 antagonists with nanomolar potency and selectivity versus PARI, derived from the indole-based 3. Of these, 9j (PAR4 IC50 = 445 nM, PARI response IC50 > 30 μM) and lOh (PAR4 IC50 = 179 nM, PARI response IC50 > 30 μM) maintained an overall favorable in vitro DMPK profile, encouraging rat/mouse in vivo pharmacokinetics (PK) and activity against γ-thrombin.
