Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen

Journal Article: MedChemCommYear Published: (2019) Volume Number: 10, Article Number: 1361-1369

Authors

Atkinson,Benjamin N; Steadman,David; Zhao,Yuguang; Sipthorp,James; Vecchia,Luca; Ruza,Reinis R; Jeganathan,Fiona; Lines,Georgie; Frew,Sarah; Monaghan,Amy; Kjær,Svend; Bictash,Magda; Jones,E Yvonne; Fish,Paul V

<p>Optimization of fragment hit <bold>3</bold> identified isoquinoline <bold>45</bold> as a potent inhibitor of NOTUM with an unexpected flipped binding mode.</p>

Science Technology Platforms