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• W2090045963 abstract "Structurally novel thrombin receptor (protease activated receptor 1, PAR-1) antagonists based on the natural product himbacine are described. The prototypical PAR-1 antagonist 55 showed a Ki of 2.7 nM in the binding assay, making it the most potent PAR-1 antagonist reported. 55 was highly active in several functional assays, showed excellent oral bioavailability in rat and monkey models, and showed complete inhibition of agonist-induced ex vivo platelet aggregation in cynomolgus monkeys after oral administration." @default.
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• W2090045963 date "2005-08-24" @default.
• W2090045963 modified "2023-10-03" @default.
• W2090045963 title "Discovery of Potent Orally Active Thrombin Receptor (Protease Activated Receptor 1) Antagonists as Novel Antithrombotic Agents" @default.
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• W2090045963 doi "https://doi.org/10.1021/jm0502236" @default.
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