Article
作者: Clarke, Jonathan H. ; Edwards, Simon ; Skidmore, John ; Willems, Henriette M. G. ; Andrews, Stephen P. ; Romero, Tamara ; Chawner, Stephen J. ; Winpenny, David ; Boffey, Helen K. ; Green, Christopher
The PI5P4Ks play a central role in regulating cell signalling pathways. ARUK2002821 is reported as a potent and selective PI5P4Kα inhibitor (pIC50 = 8.0). ADMET and target engagement data are provided, with a ligand-protein X-ray structure, optimised to deliver ARUK2002821.