An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent

por Willis, Nicky J, Bayle, Elliott D, Papageorgiou, George, Steadman, David, Atkinson, Benjamin N, Mahy, William, Fish, Paul V
Publicado 2019

Large-scale synthesis of Notum inhibitor 1-(2,4-dichloro-3-(trifluoromethyl)-phenyl)-1H-1,2,3-triazole (ARUK3001185) employing a modified Sakai reaction as the key step

por Atkinson, Benjamin N., Willis, Nicky J., Smith, Jennifer, Gill, Rebecca, Ali, Jody, Xu, Zhou, Lai, Ping-Shan, Fish, Paul V.
Publicado 2022

Designed switch from covalent to non-covalent inhibitors of carboxylesterase Notum activity

por Atkinson, Benjamin N., Willis, Nicky J., Zhao, Yuguang, Patel, Chandni, Frew, Sarah, Costelloe, Kathryn, Magno, Lorenza, Svensson, Fredrik, Jones, E. Yvonne, Fish, Paul V.
Publicado 2023

Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling

por Bayle, Elliott D., Svensson, Fredrik, Atkinson, Benjamin N., Steadman, David, Willis, Nicky J., Woodward, Hannah L., Whiting, Paul, Vincent, Jean-Paul, Fish, Paul V.
Publicado 2021

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

por 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.
Publicado 2019

Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors

por Atkinson, Benjamin N., Steadman, David, Mahy, William, Zhao, Yuguang, Sipthorp, James, Bayle, Elliott D., Svensson, Fredrik, Papageorgiou, George, Jeganathan, Fiona, Frew, Sarah, Monaghan, Amy, Bictash, Magda, Jones, E. Yvonne, Fish, Paul V.
Publicado 2020

Structural Analysis and Development of Notum Fragment Screening Hits

por Zhao, Yuguang, Mahy, William, Willis, Nicky J., Woodward, Hannah L., Steadman, David, Bayle, Elliott D., Atkinson, Benjamin N., Sipthorp, James, Vecchia, Luca, Ruza, Reinis R., Harlos, Karl, Jeganathan, Fiona, Constantinou, Stefan, Costa, Artur, Kjær, Svend, Bictash, Magda, Salinas, Patricia C., Whiting, Paul, Vincent, Jean-Paul, Fish, Paul V., Jones, E. Yvonne
Publicado 2022

Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit

por Willis, Nicky J., Mahy, William, Sipthorp, James, Zhao, Yuguang, Woodward, Hannah L., Atkinson, Benjamin N., Bayle, Elliott D., Svensson, Fredrik, Frew, Sarah, Jeganathan, Fiona, Monaghan, Amy, Benvegnù, Stefano, Jolly, Sarah, Vecchia, Luca, Ruza, Reinis R., Kjær, Svend, Howell, Steven, Snijders, Ambrosius P., Bictash, Magda, Salinas, Patricia C., Vincent, Jean-Paul, Jones, E. Yvonne, Whiting, Paul, Fish, Paul V.
Publicado 2022