Small molecule kinase inhibitor growth assays

The compound screens comprised an in-house library of 80 small molecule inhibitors (0.5, 1, 5, 10, 50, 100, 500 and 1000 nM). Five hundred cells were seeded in 384-well plates. Twenty-four hours post seeding, drug treatment was initiated and cells were continuously exposed to the drugs (6 days), at which point cell viability was estimated using CellTiter-Glo (Promega). Luminescence values were normalised to the median of the per-plate dimethyl sulphoxide (DMSO) negative control wells and the dose–response relationships modelled using three-parameter logistic regression provided by the drc R package. AUC scores are represented as a proportion of the maximum area under curve (calculated as: log10(500000) − log10(500)=3).