Rogaratinib (BAY 1163877) is a highly potent and selective small-molecule 
pan-fibroblast growth factor receptor (FGFR) inhibitor (FGFR1-4) for oral 
application currently being investigated in phase 1 clinical trials for the 
treatment of cancer. In this publication, we report its discovery by de novo 
structure-based design and medicinal chemistry optimization together with its 
pharmacokinetic profile.