Publications

A GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in vivo Profile

Villemure, E; Volgraf, M; Jiang, Y; Wu G; Ly, C; Yuen, P; Lu, A; Luo, X; Liu, M; Zhang, S; Lupardus, P; Wallweber; H; Liederer, B; Deshmukh, G; Plise, E; Tay, S; Wang, T; Hanson, J; Hackos, D; Scearce-LevieK; Schwarz, J; Sellers, B. ACS Med Chem Letters, 2017, 8, 84-89.

Publications

An investigation into the prediction of in vivo clearance for a range of Flavin-containing monooxygenase substrates

Jones, B; Srivastava, A; Colclough, N; Wilson, J; Reddy, VP; Amberntsson, S.; Li, D. Drug Metabolism and Disposition, 2017, 45(10), 1060-1067.

Publications

Structure-guided design of novel, potent, and selective macrocyclic plasma kallikrein inhibitors

Li, Z; Partridge, J; Silva-Garcia, A; Rademacher, P; Betz, A; Xu, Q; Sham, H; Hu, Y; Shan, Y; Liu, B; Zhang, Y; Shi, H; Xu, Q; Ma, X; Zhang, L. ACS Med Chem Letters, 2017, 8, 185–190.

Publications

Discovery of Pyrazolo[1,5‐a]pyrimidine B‐Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.

McCoull, W; Abrams, R; Anderson, E; Blades, K; Barton, P; Box, M; Burgess, J; Byth, K; Cao, Q; Chuaqui, C; Carbajo, R; Cheung, T; Code, E; Ferguson, A; Fillery, S; Fuller, N; Gangl, E; Gao, N; Grist, M; Hargreaves, D; Howard, M; Hu, J; Kemmitt, P; Nelson, J; O’Connell, N; Prince, D.B; Raubo, P; Rawlins, P; Robb, G; Shi, J; Waring, M; Whittaker, D; Wylot, M; Zhu, X. J Med Chem, 2017, 60, 4386-4402.

Publications

Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.

Ward, R; Bethel, P; Cook, C; Davies, E; Debreczeni, J; Fairley, G; Feron, L; Flemington, V; Graham, M; Greenwood, R; Griffin, N; Hanson, L; Hopcroft, P; Howard, T; Hudson, J; James, M; Jones, C; Jones, C; Lamont, S; Lewis, R; Lindsay, N; Roberts, K; Simpson, I; St-Gallay, S; Swallow, S; Tang, J; Tonge, M; Wang, Z; Zhai, B. J Med Chem, 2017, 60, 3438-3450.