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

An automated high-throughput system for phenotypic screening of chemical libraries on C. elegans and parasitic nematodes

por Partridge, Frederick A., Brown, Anwen E., Buckingham, Steven D., Willis, Nicky J., Wynne, Graham M., Forman, Ruth, Else, Kathryn J., Morrison, Alison A., Matthews, Jacqueline B., Russell, Angela J., Lomas, David A., Sattelle, David B.
Publicado 2017

Dihydrobenz[e][1,4]oxazepin-2(3H)-ones, a new anthelmintic chemotype immobilising whipworm and reducing infectivity in vivo

por Partridge, Frederick A., Murphy, Emma A., Willis, Nicky J., Bataille, Carole J. R., Forman, Ruth, Heyer-Chauhan, Narinder, Marinič, Bruno, Sowood, Daniel J. C., Wynne, Graham M., Else, Kathryn J., Russell, Angela J., Sattelle, David B.
Publicado 2017

2,4-Diaminothieno[3,2-d]pyrimidines, a new class of anthelmintic with activity against adult and egg stages of whipworm

por Partridge, Frederick A., Forman, Ruth, Willis, Nicky J., Bataille, Carole J. R., Murphy, Emma A., Brown, Anwen E., Heyer-Chauhan, Narinder, Marinič, Bruno, Sowood, Daniel J. C., Wynne, Graham M., Else, Kathryn J., Russell, Angela J., Sattelle, David B.
Publicado 2018

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

Structural Requirements for Dihydrobenzoxazepinone Anthelmintics: Actions against Medically Important and Model Parasites: Trichuris muris, Brugia malayi, Heligmosomoides polygyrus...

por Partridge, Frederick A., Bataille, Carole J.R., Forman, Ruth, Marriott, Amy E., Forde-Thomas, Josephine, Häberli, Cécile, Dinsdale, Ria L., O’Sullivan, James D.B., Willis, Nicky J., Wynne, Graham M., Whiteland, Helen, Archer, John, Steven, Andrew, Keiser, Jennifer, Turner, Joseph D., Hoffmann, Karl F., Taylor, Mark J., Else, Kathryn J., Russell, Angela J., Sattelle, David B.
Publicado 2021

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