FIGURE 2.

tBPQA competition binding against LEDGF and promotion of IN dimer formation correlate with their antiviral potency. A, diagram of the experimental setup for the IN-LEDGF interaction assay. B, competition dose response of tBPQAs using the IN-LEDGF interaction assay. Data represent the means of two independent experiments done in quadruplicate with standard deviations shown as error bars. C, dimer promotion dose response of tBPQAs. Data represent the means of four independent experiments done in quadruplicate with standard deviations shown as error bars. D, correlation plot between the EC₅₀ of dimer promotion and the IC₅₀ of competition binding against LEDGF for a diverse set of 11 tBPQAs. E, correlation plot between the EC₅₀ of dimer promotion and the antiviral EC₅₀ in MT-4 cells for the same set of 11 tBPQAs.