Table 1

Equilibrium dissociation constants for the binding of EP compounds to antithrombin in I 0.15, pH 7.4 buffer containing 5mM Ca2+ at 25°C

EP compoundKD, nM
Fondaparinux 60 ± 10 
EP42675 30 ± 1 
EP217609 32 ± 4 
EP217609-1 34 ± 4 
EP307138-1 39 ± 3 
EP compoundKD, nM
Fondaparinux 60 ± 10 
EP42675 30 ± 1 
EP217609 32 ± 4 
EP217609-1 34 ± 4 
EP307138-1 39 ± 3 

Dissociation constants for antithrombin–EP compound interactions were measured by fitting fluorescence titrations of antithrombin with the compounds by the quadratic equilibrium binding equation as described in “Binding of EP compounds to antithrombin and thrombin.” Fondaparinux served as a control. Reported dissociation constants are mean ± range from at least 2 titrations.

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