… This halo-substitution resulted in enhanced specificity … (fXa, this work) with neutral scaffold
and on Ser190 protease (… of the P1 group can result in a potent and selective inhibitor despite …

… In summary, a series of ketopiperazine inhibitors with an azaindole P 4 group and nonbasic
chloroaryl groups have been shown to be potent and selective inhibitors of factor Xa. The X-…

… P1 group gave compound 3 (clinical candidate DPC423). Continued searches for even more
weakly basic or neutral P1 groups and … of basic P1 groups with Asp-189 in the S1 specificity …

… behind the incorporation of neutral P1 motifs (in nonamidines) at … by the chloro group of
nonamidine class of inhibitors, which is … specific D pocket (insertion 60-loop), thrombin inhibitors …

… -containing inhibitor but is unique in that it contains a neutral O-methoxy group in the P1 site
of … position to interact with an aspartic acid group buried deep within the specificity pocket of …

… complex with factor Xa shows the amidine group inserted in … with the S1 and S4 specificity
sites of factor Xa are shown in green … Building on this information, the amidine group in the P1 …

… chose 6 specific small molecule fXa inhibitors of comparable … per group were used for each
inhibitor tested and each group … 2 P1 bezamidines, 1 P1 neutral and 1 P1 aminoisoquinoline. …

… IXa, which subsequently activates factor X to factor Xa in the … class) is a covalent
inhibitor of FXIa because the keto group is … P1 was replaced with a neutral para-chlorophenyltetrazole …

… to take advantage of the larger S1 specificity pocket in FXa (one … basic inhibitor 15a has
been reported by our research group … neutral P1 ligand in our pyrazole series of FXa inhibitors. …

… of the positively charged main inhibitor fragment P1 occurs in this … The interesting nontypical
result is that neutral moieties of … Thus, we can say that two main groups of factor Xa inhibitors …