Table 3. Affinity and Efficiency Metrics of 4-Methoxyanilide Derivatives against MEK1.

^aK_d values are the geometric mean ± SEM of two or more determinations.

^bLE (kcal/(mol HA)): 1.37pK_d/HA (heavy atom count).

^cLipE: pK_d – log D. SPR pK_d in the presence of AMP-PNP used in efficiency metrics. log D measured via shake-flask method in octanol and water at pH 7.4.

^d(μL/(min mg)).

^e(μL/(min 1E6)).

^fP_app: (*1 × 10^–6 cm/s).

^gn.d.: not determined. Compounds were synthesized followed the synthetic route outlined in Scheme 1.