Overview of high-throughput screening data. (A) Hit triage from HTS library screen (10,804 compounds), to compounds that are cytotoxic toward parental KB-3-1 cells (1362 compounds), to putative P-gp substrates (90 compounds). (B) Summary of percentage of cytotoxic compounds (orange) vs. nontoxic compounds (blue), both cumulative and represented in each library screened. (C) Area-under-the-curve heatmap of compound activity for screen hits, where red intensity represents magnitude of AUC: Deep red is strongest cytotoxicity, and white represents no cytotoxicity.