Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4

Authors: Myers, Stephanie M., Miller, Duncan C., Molyneux, Lauren, Arasta, Mercedes, Bawn, Ruth H., Blackburn, Timothy J., Cook, Simon J., Edwards, Noel, Endicott, Jane A., Golding, Bernard T., Griffin, Roger J., Hammonds, Tim, Hardcastle, Ian R., Harnor, Suzannah J., Heptinstall, Amy B., Lochhead, Pamela A., Martin, Mathew P., Martin, Nick C., Newell, David R., Owen, Paul J., Pang, Leon C., Reuillon, Tristan, Rigoreau, Laurent J.M., Thomas, Huw D., Tucker, Julie A., Wang, Lan-Zhen, Wong, Ai-Ching, Noble, Martin E.M., Wedge, Stephen R., Cano, Celine

Source: In European Journal of Medicinal Chemistry 15 September 2019 178:530-543

Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.

Authors: Miller, Duncan C., Reuillon, Tristan, Molyneux, Lauren, Blackburn, Timothy, Cook, Simon J., Edwards, Noel, Endicott, Jane A., Golding, Bernard T., Griffin, Roger J., Hardcastle, Ian, Harnor, Suzannah J., Heptinstall, Amy, Lochhead, Pamela, Martin, Mathew P., Martin, Nick C., Myers, Stephanie, Newell, David R., Noble, Richard A., Phillips, Nicole, Rigoreau, Laurent

Source: Journal of Medicinal Chemistry; 5/12/2022, Vol. 65 Issue 9, p6513-6540, 28p