SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa
Copyright policy )SAR and factor IXa crystal structure of a dual inhibitor of factors IXa and Xa
Modifications to the P4 moiety and pyrazole C3 substituent of factor Xa inhibitor SN-429 provided several new compounds, which are 5-10nM inhibitors of factor IXa. An X-ray crystal structure of one example complexed to factor IXa shows that these compounds adopt a similar binding mode to that previously observed with pyrazole inhibitors in the factor Xa active site both with regard to how the inhibitor binds and the position of Tyr99.
- Bristol-Myers Squibb (Germany) Germany
Models, Molecular, Structure-Activity Relationship, Binding Sites, Molecular Structure, Factor Xa, Humans, Pyrazoles, Benzimidazoles, Crystallography, X-Ray, Factor IXa, Factor Xa Inhibitors
Models, Molecular, Structure-Activity Relationship, Binding Sites, Molecular Structure, Factor Xa, Humans, Pyrazoles, Benzimidazoles, Crystallography, X-Ray, Factor IXa, Factor Xa Inhibitors
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