dual specificity mitogen-activated protein kinase kinase 1|ERK activator kinase 1|MAP kinase kinase 1|MAPKK1|MKK1|PRKMK1 Description: X-ray structure of the human mitogen-activated protein kinase kinase 1 (MEK1) in a ternary complex with compound 1, ATP-GS AND MG2P Description: X-ray structure of the human mitogen-activated protein kinase kinase 1 (MEK1) complexed with a potent inhibitor RDEA119 and MgATP Description: Mitogen-activated protein kinase kinase 1 (MEK1) in complex with CH4987655 and MgAMP-PNP. Description: Crystal Structure of the Human Mitogen-activated protein kinase kinase 1 (MEK 1) in complex with ligand and MgATP. Download all structure-activity data for this target as a CSV file Description: Measured in a fluorescence anisotropy assay using recombinant MEK1. Ki approximated from the graph in supplementary figure 1b. Description: Determined in an in vitro biochemical assay, using a kinase-dead ERK mutant as the substrate for hMEK1. Description: Biochemical assay measuring MEK-induced phosphorylation of ERK residues T202 and Y204. EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1 M and 10 M against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5 M against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx Clinically-Relevant Mutations and Pathophysiology Synonyms: Cardiofaciocutaneous syndrome [Orphanet: ORPHA1340] 1. 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Rice KD, Aay N, Anand NK, Blazey CM, Bowles OJ, Bussenius J, Costanzo S, Curtis JK, Defina SC, Dubenko L et al..(2012)Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973). 17. Vollmer S, Cunoosamy D, Lv H, Feng H, Li X, Nan Z, Yang W, Perry MWD.(2020)Design, Synthesis, and Biological Evaluation of MEK PROTACs. 18. Wei J, Hu J, Wang L, Xie L, Jin MS, Chen X, Liu J, Jin J.(2019)Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. 19. Wityak J, Hobbs FW, Gardner DS, Santella 3rd JB, Petraitis JJ, Sun JH, Favata MF, Daulerio AJ, Horiuchi KY, Copeland RA et al..(2004)Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors. 20. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al..(2010)Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. 21. Yamaguchi T, Kakefuda R, Tajima N, Sowa Y, Sakai T.(2011)Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. 22. Yeh TC, Marsh V, Bernat BA, Ballard J, Colwell H, Evans RJ, Parry J, Smith D, Brandhuber BJ, Gross S et al..(2007)Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. STE7 family: mitogen-activated protein kinase kinase 1. Last modified on 20/01/2020. Accessed on 18/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2062.