Figure 4. IC₅₀ values of three representative hits from HTS for inhibition of acylation of PBP 2 by Bocillin-FL.

IC₅₀s of the inhibitors were determined by SDS-PAGE-based concentration-response assays using a 0.05–1000 µM concentration range for the inhibitors with 1 µM PBP 2 and 10 µM of Bocillin-FL. Triton X-100 (0.01%) was included to eliminate promiscuous inhibitors. A. Compound 2 (in Table 2). B. Compound 4. C. Compound 7. In all experiments, the data points represent the mean ± standard deviation for two replicate (compounds 4 and two) or four replicate (compound 7) experiments at each concentration of inhibitor.