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. 2014 Nov 17;6(1):89–94. doi: 10.1021/ml500394m

Table 1. Parameters of Kinetic Interaction with VEGFR2a.

compd Kd (nmol/L) kon (s–1 × M–1) koff (s–1) residence time (min)
lenvatinib 2.1 ± 0.1 4.8 × 105 ± 1.4 × 104 9.9 × 10–4 ± 9.0 × 10–5 17 ± 2
sorafenib 33 ± 2.6 7.9 × 103 ± 1.5 × 102 2.6 × 10–4 ± 2.5 × 10–5 64 ± 6
sunitinib 30 ± 1.7 >1.9 × 105 >57 × 10–4 <2.9
a

Kd = equilibrium dissociation constant, calculated by using the Cheng–Prusoff equation from IC50-like values obtained from the percent displacement values at time point, at which system has reached equilibrium; kon = association rate constant; displacement traces at each compound concentration were fitted according to a monoexponential equation to yield kobs. Secondary plot of kobs over compound concentration was linearly fitted to generate kon; koff = dissociation rate constant (= Kd × kon); residence time = 1/koff. From standard errors of IC50 and kon calculated in regression analysis for curve fitting, errors for Kd, koff, and residence time were calculated by Gaussian error propagation.