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BMS-740808 is a highly potent, selective inhibitor of Factor X, with Ki of 0.03 nM. BMS-740808 is highly potent with a rapid onset of inhibition (2.7 × 107 M-1 s-1), selective (>1000-fold over other proteases), efficacious in the AVShunt thrombosis model. BMS-740808 is synthesized by modification of employing bicyclic pyrazolo-pyridinone scaffold to Razaxaban, a pyrazole based Factor X inhibitor. Especially for BMS-740808, the introduction of a 3(R)-hydroxyl moiety on the pyrrolidine ring results in a significant enhancement in potency. BMS-740808 also shows the high affinity for thrombin.
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