Dataset for: RSP1141, a Selective Non-Covalent BTK Inhibitor, Suppresses GPVI-Mediated Platelet Activation

This dataset contains the kinase selectivity profiling summary for RSP1141, a novel non-covalent, reversible Bruton's tyrosine kinase (BTK) inhibitor, generated in support of the manuscript "RSP1141, a Selective Non-Covalent BTK Inhibitor, Suppresses GPVI-Mediated Platelet Activation." RSP1141 was screened against a panel of 370 human protein kinases using the Reaction Biology "HotSpot" radiometric kinase assay platform. The compound was tested in single-dose duplicate mode at a concentration of 1 μM, with all reactions carried out at 1 μM ATP. Staurosporine (and alternate reference inhibitors where appropriate) served as control compounds, tested in 10-dose IC50 mode. The file contains a summary table reporting, for each of the 370 kinases, the percent enzyme activity of RSP1141 relative to DMSO controls (duplicate values and their mean) and the corresponding percent inhibition (100 − % enzyme activity), together with the IC50 values of the reference control compounds. The experimental conditions are described within the file. These data underlie the kinase selectivity analysis presented in the manuscript (Figure 4C) and characterize the target selectivity of RSP1141 across the human kinome, including its activity against BTK and structurally related kinases. Note that the percent-inhibition values reported here were obtained in a cell-free biochemical assay performed at a low ATP concentration (1 μM); as discussed in the manuscript, biochemical inhibition of certain ATP-competitive off-target kinases under these conditions does not necessarily translate to inhibition in intact cells, where physiological ATP concentrations are substantially higher. Assay provider: Reaction Biology (www.reactionbiology.com). Compound synthesis and study design were performed by the authors. These data may be reused under the CC BY 4.0 license with appropriate attribution to the associated publication.