6SLG

HUMAN ERK2 WITH ERK1/2 INHIBITOR, AZD0364.

Summary for 6SLG

• Entry DOI: 10.2210/pdb6slg/pdb
• Descriptor: Mitogen-activated protein kinase 1, ERK-tide, (6~{R})-7-[[3,4-bis(fluoranyl)phenyl]methyl]-6-(methoxymethyl)-2-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-5,6-dihydroimidazo[1,2-a]pyrazin-8-one, ... (6 entities in total)
• Functional Keywords: erk2, kinase, inhibitor, oncology, transferase
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 45335.77

Authors

Breed, J.,Phillips, C. (deposition date: 2019-08-19, release date: 2019-11-20, Last modification date: 2024-05-15)

• Primary citation: Ward, R.A.,Anderton, M.J.,Bethel, P.,Breed, J.,Cook, C.,Davies, E.J.,Dobson, A.,Dong, Z.,Fairley, G.,Farrington, P.,Feron, L.,Flemington, V.,Gibbons, F.D.,Graham, M.A.,Greenwood, R.,Hanson, L.,Hopcroft, P.,Howells, R.,Hudson, J.,James, M.,Jones, C.D.,Jones, C.R.,Li, Y.,Lamont, S.,Lewis, R.,Lindsay, N.,McCabe, J.,McGuire, T.,Rawlins, P.,Roberts, K.,Sandin, L.,Simpson, I.,Swallow, S.,Tang, J.,Tomkinson, G.,Tonge, M.,Wang, Z.,Zhai, B.; 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).; J.Med.Chem., 62:11004-11018, 2019; PubMed: 31710489; DOI: 10.1021/acs.jmedchem.9b01295

Experimental method

X-RAY DIFFRACTION (1.33 Å)