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4U7Z

Mitogen-Activated Protein Kinase Kinase (MEK1) bound to G805

Summary for 4U7Z
Entry DOI10.2210/pdb4u7z/pdb
Related1S9J 4U80 4U81
DescriptorDual specificity mitogen-activated protein kinase kinase 1, MAGNESIUM ION, 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide, ... (5 entities in total)
Functional Keywordskinase, inhibitor, complex, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (Human)
Cellular locationCytoplasm, cytoskeleton, microtubule organizing center, centrosome: Q02750
Total number of polymer chains1
Total formula weight38917.81
Authors
Robarge, K.D.,Ultsch, M.H.,Wiesmann, C. (deposition date: 2014-07-31, release date: 2014-09-24, Last modification date: 2023-09-27)
Primary citationRobarge, K.D.,Lee, W.,Eigenbrot, C.,Ultsch, M.,Wiesmann, C.,Heald, R.,Price, S.,Hewitt, J.,Jackson, P.,Savy, P.,Burton, B.,Choo, E.F.,Pang, J.,Boggs, J.,Yang, A.,Yang, X.,Baumgardner, M.
Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.
Bioorg.Med.Chem.Lett., 24:4714-4723, 2014
Cited by
PubMed: 25193232
DOI: 10.1016/j.bmcl.2014.08.008
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.805 Å)
Structure validation

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