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TargetDual specificity mitogen-activated protein kinase kinase 1
LigandBDBM50222709
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1584574 (CHEMBL3820565)
IC50 13±n/a nM
Citation Van Dort, MEHong, HWang, HNino, CALombardi, RLBlanks, AEGalbán, SRoss, BD Discovery of Bifunctional Oncogenic Target Inhibitors against Allosteric Mitogen-Activated Protein Kinase (MEK1) and Phosphatidylinositol 3-Kinase (PI3K). J Med Chem59:2512-22 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Dual specificity mitogen-activated protein kinase kinase 1
Name:Dual specificity mitogen-activated protein kinase kinase 1
Synonyms:Dual specificity mitogen-activated protein kinase (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1) | Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase | Dual specificity mitogen-activated protein kinase kinase MEK1/2 | ERK activator kinase 1 | MAP kinase kinase 1 | MAP2K1 | MAPK/ERK kinase 1 | MAPK/ERK kinase 1 (MEK1) | MEK-1 | MEK1 | MP2K1_HUMAN | Mitogen-activated protein kinase 1 (MEK1) | PRKMK1 | VHL-MAP2K1/MAP2K2
Type:Other Protein Type
Mol. Mass.:43439.03
Organism:Homo sapiens (Human)
Description:Full-length human MEK-1 was generated by PCR and purified as a fusion protein from Escherichia coli lysates.
Residue:393
Sequence:
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50222709
n/a
NameBDBM50222709
Synonyms:3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-N-(2-hydroxyethoxy)benzamide | CHEMBL244488 | PD-0316684 | US8575391, 339
TypeSmall organic molecule
Emp. Form.C15H12F3IN2O3
Mol. Mass.452.1671
SMILESOCCONC(=O)c1ccc(F)c(F)c1Nc1ccc(I)cc1F
Structure
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