5KE0

Discovery of 1-1H-Pyrazolo 4,3-c pyridine-6-yl urea Inhibitors of Extracellular Signal Regulated Kinase ERK for the Treatment of Cancers

Summary for 5KE0

• Entry DOI: 10.2210/pdb5ke0/pdb
• Descriptor: Mitogen-activated protein kinase 1, 1-[3-(2-methylpyridin-4-yl)-1~{H}-pyrazolo[4,3-c]pyridin-6-yl]-3-(phenylmethyl)urea, SULFATE ION, ... (4 entities in total)
• Functional Keywords: transferase, serine/threonine-protein kinase, map kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Rattus norvegicus (Rat)
• Cellular location: Cytoplasm, cytoskeleton, spindle : P63086
• Total number of polymer chains: 1
• Total formula weight: 43200.42

Authors

Hruza, A.,Lim, J. (deposition date: 2016-06-09, release date: 2016-07-06, Last modification date: 2024-03-06)

• Primary citation: Lim, J.,Kelley, E.H.,Methot, J.L.,Zhou, H.,Petrocchi, A.,Chen, H.,Hill, S.E.,Hinton, M.C.,Hruza, A.,Jung, J.O.,Maclean, J.K.,Mansueto, M.,Naumov, G.N.,Philippar, U.,Raut, S.,Spacciapoli, P.,Sun, D.,Siliphaivanh, P.; Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers.; J.Med.Chem., 59:6501-6511, 2016; PubMed: 27329786; DOI: 10.1021/acs.jmedchem.6b00708

Experimental method

X-RAY DIFFRACTION (1.68 Å)