Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC)

Authors: Richard A. Ward, Mark J. Anderton, Paul A. Bethel, J. Breed, Calum Cook, Emma Jane Davies, Andrew P. Dobson, Zhiqiang Dong, Gary Fairley, Paul Farrington, Lyman J. Feron, Vikki Flemington, Francis D. Gibbons, M. A. Graham, Ryan Greenwood, Lyndsey Hanson, Philip Hopcroft, Rachel Howells, Julian A. Hudson, Michael J. James, Clifford D. Jones, Christopher R. Jones, Yongchao Li, Scott G. Lamont, Richard J. Lewis, Nicola Lindsay, James F. McCabe, Thomas M. McGuire, Philip B. Rawlins, Karen Roberts, Linda C. Sandin, Iain Simpson, Steve Swallow, Jia Tang, Gary Tomkinson, Michael Tonge, Zhenhua Wang, Baochang Zhai - Journal of Medicinal Chemistry 2019 cited by 78

= 6 nM) as well as excellent physicochemical and absorption, distribution, metabolism, and excretion (ADME) properties and has demonstrated encouraging antitumor activity in preclinical models.