Versatile tool for kinase biology in drug discovery
  • KinomeScout™ works with native proteins in their physiological setting to direct the design of potent and selective small molecule drug candidates
  • The technology is based on a kinase-binding matrix that can be used to measure the potency of compounds of ~300 different kinases and other ATP binding proteins (such as helicases or phospho-diesterases)
  • No label on drug or protein required
  • Target and biomarker discovery: KinomeScout™ can be used to analyse kinase expression in different tissues (e.g. healthy vs. disease). Kinases only present in the disease state are target and biomarker candidates
  • Selectivity profiling: With KinomeScout™ leads and drug candidates can be tested against all kinases in a tissue or cell type in one experiment to identify (unwanted) off-targets


Further reading

Schirle, M., Bantscheff, M., and Kuster, B. (2012). Mass Spectrometry-based Proteomics in Preclinical Drug Discovery, Chem Biol 19(1):72-84. [Link]

Médard, G., Pachl F., Ruprecht, B., Klaeger, S., Heinzlmeir, S., Helm, D., Qiao, H., Ku, X., Wilhelm, M., Kuehne, T., Wu, Z., Dittmann, A., Hopf, C., Kramer, K., and Kuster, B. (2015). Optimized chemical proteomics assay for kinase inhibitor profiling, J Proteome Res. 14(3):1574-86. [Link]

Bantscheff, M., Eberhard, D., Abraham, Y., Bastuck, S., Boesche, M., Hobson, S., Mathieson, T., Perrin, J., Raida, M., Rau, C., Reader, V., Sweetman, G., Bauer, A., Bouwmeester, T., Hopf, C., Kruse, U., Neubauer, G., Ramsden, N., Rick, J., Kuster, B., and Drewes, G. (2007). Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors, Nat Biotechnol. 25(9):1035-44. [Link]


Schematic representation of the KinomeScout technology
Drug binding to around 300 human kinases can be analysed in parallel under physiological conditions