The dissertation termed "When chemical proteomics meets medicinal chemistry: Guided drug discovery towards EPHA2 inhibitors" investigates novel drug targets for the receptor tyrosine kinase EPHA2. Chemical proteomics was used to identify clinical EPHA2 inhibitors, to select a lead structure for medicinal chemistry, and to guide the design and synthesis of EPHA2 inhibitors. The award winning thesis offers new insights EPHA2 inhibition and novel drug tool compounds.