Melagatran is an inhibitor of thrombin (Ki = 0.002 µM) and an active metabolite of the prodrug ximelagatran (Cay-16862). It is selective for thrombin over a variety of serine proteases (Kis = 0.6-10.2 µM) but also inhibits trypsin (Ki = 0.004 µM). Melagatran inhibits thrombin-induced aggregation of isolated washed...