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Optimization of the P4 moiety yielded several potent compounds with IC50 below 1 nM against factor Xa.
The benzoxazinones 41 45 are potent against factor Xa, retain the improved trypsin selectivity of the corresponding aniline-based compounds, and show strong antithrombotic effect dose responsively.
Among them, the piperazinone-based inhibitors were found to be not only active against factor Xa but also selective over thrombin.
Anti-factor D against factor D, the rate limiting step in the alternative pathway has been developed and has been tested in baboons undergoing Cardiopulmonary bypass (CPB) where they were found to inhibit complement and leukocyte activation [93].
MUV548 contains inhibitors of protein kinase A as actives and MUV846 contains inhibitors against factor XIa. Second, we used the mutagenicity data set composed by Kazius et al. [10].
Inhibitor 5e has a KI against factor Xa of 0.12 nM and is greater than 8000- and 2000-fold selective over two related serine proteases, thrombin and trypsin, respectively.
Similar(22)
Dr. Smalley generally slips quickly over the environmental dimensions of competing technologies because the Bush administration has taken such a strong stand against factoring climate change into policy.
Janssen's Kimble was like Camus's Meursault, had he not pulled the trigger: a strange lonely man pushing up against factors far beyond his control.
General Farrisee said the Army had weighed Captain Kalsi's request against factors such as "unit cohesion, morale, discipline, safety and/or health".
Decision makers need to rate two different issues, namely the factor weight carried during the assessment process and the score of the alternative against factors.
Gabor typically encodes facial shape and appearance [17], which makes it robust against factors such as facial expression [4 6], mutilated faces [19], occlusion [7], and pose [3].
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Justyna Jupowicz-Kozak
CEO of Professional Science Editing for Scientists @ prosciediting.com