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. Author manuscript; available in PMC: 2014 Jun 27.
Published in final edited form as: J Med Chem. 2013 Jun 13;56(12):5059–5070. doi: 10.1021/jm400369q

Figure 4.

Figure 4

Competition by exosite 2 ligands and Dixon-Webb analysis of the competitive effects. Competitive effect of UFH (A) and H8 (C) on the inhibition of human α-thrombin by 9a in 20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl2 and 0.1 % PEG8000 at 25 °C. Solid lines represent fits using the logistic equation 1 to obtain the apparent IC50 as described in ‘Experimental Procedures’. Comparisons of the predicted and experimentally measured IC50 values in the presence of UFH and H8 at various competitor concentrations are shown in B and D, respectively. Open bars represent the measured values, whereas closed bars are those predicted using Dixon-Webb equation 2.