Figure 2.
Structure–activity studies of takinib analogs against IRAK-4. a, core aminobenzimidazole scaffold showing regions targeted for modification. b, outline of modifications made during the SAR campaign and corresponding IC50 determined by mean IRAK-4 radioactive [32P]ATP filter-binding assay inhibition from vehicle. c, titrations of takinib analogs against IRAK-4, presented as percentages of inhibition from vehicle control. The data points represent means ± S.E. (n = 2). d, comparison of percentages of inhibition of DMSO, takinib (1 μm), and HS-243 (1 μm) against IRAK-4. e, dose-dependent response of HS-243 compared with commercially available Sigma IRAK-1/4 compound. The data points represent means ± S.E. (n = 2).