Steadman D, Atkinson BN, Zhao Y, Willis NJ, Frew S, Monaghan A, Patel C, Armstrong E, Costelloe K, Magno L, Bictash M, Jones EY, Fish PV, Svensson F (2022)
Virtual Screening Directly Identifies New Fragment-Sized Inhibitors of Carboxylesterase Notum with Nanomolar Activity
Journal of Medicinal Chemistry 65: 562
Zhao Y, Mahy W, Willis NJ, Woodward HL, Steadman D, Bayle ED, Atkinson BN, Sipthorp J, Vecchia L, Ruza RR, Harlos K, Jeganathan F, Constantinou S, Costa A, Kjaer S, Bictash M, Salinas PC, Whiting P, Vincent JP, Fish PV, Jones EY (2022)
Structural Analysis and Development of Notum Fragment Screening Hits
ACS Chem Neurosci 13: 2060
Bayle ED, Svensson F, Atkinson BN, Steadman D, Willis NJ, Woodward HL, Whiting P, Vincent JP, Fish PV (2021)
Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling
Journal of Medicinal Chemistry
Zhao Y, Svensson F, Steadman D, Frew S, Monaghan A, Bictash M, Moreira T, Chalk R, Lu W, Fish PV, Jones EY (2021)
Structural Insights into Notum Covalent Inhibition
Journal of Medicinal Chemistry 64: 11354
Mahy W, Patel M, Steadman D, Woodward HL, Atkinson BN, Svensson F, Willis NJ, Flint A, Papatheodorou D, Zhao Y, Vecchia L, Ruza RR, Hillier J, Frew S, Monaghan A, Costa A, Bictash M, Walter MW, Jones EY, Fish PV (2020)
Screening of a Custom-Designed Acid Fragment Library Identifies 1-Phenylpyrroles and 1-Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase Activity
Journal of Medicinal Chemistry 63: 9464
Atkinson BN, Steadman D, Zhao YG, Sipthorp J, Vecchia L, Ruza RR, Jeganathan F, Lines G, Frew S, Monaghan A, Kjaer S, Bictash M, Jones Y, Fish PV, Zhao Y, Jones EY (2019)
Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen
Medchemcomm 10: 1361
Atkinson BN, Steadman D, Mahy W, Zhao Y, Sipthorp J, Bayle ED, Svensson F, Papageorgiou G, Jeganathan F, Frew S, Monaghan A, Bictash M, Jones EY, Fish PV (2019)
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors
Bioorganic & Medicinal Chemistry Lett
Willis NJ, Bayle ED, Papageorgiou G, Steadman D, Atkinson BN, Mahy W, Fish PV (2019)
An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent
Beilstein J Org Chem 15: 2790