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molecules of the month

“Compound 6f”

selective factor XIa serine protease inhibitor

oral in higher species, eff. in thrombosis model

from PK optimization of prior series

J. Med. Chem., May 26, 2020

Bristol Myers Squibb, Princeton, NJ

Structure of compound 6f
1 min read

“Compound 6f” is a potent macrocyclic factor XIa inhibitor (<1 nM) that is highly selective against other serine proteases and has excellent oral PK (high bioavailability, low clearance). The BMS team was able to troubleshoot metabolic instability through met. ID, which revealed a hotspot outside of the macrocycle.


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