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TargetDual specificity mitogen-activated protein kinase kinase 1
LigandBDBM1716
Substrate/Competitorn/a
Meas. Tech.ChEMBL_726976
IC50 8.6±n/a nM
Citation Dong, QDougan, DRGong, XHalkowycz, PJin, BKanouni, TO'Connell, SMScorah, NShi, LWallace, MBZhou, F Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Bioorg Med Chem Lett21:1315-9 (2011) [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/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase
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 MEK1/2 | ERK activator kinase 1 | MAP kinase kinase 1 | MAPK/ERK kinase 1 | MAPK/ERK kinase 1 (MEK1) | MEK-1 | Mitogen-activated protein kinase 1 (MEK1)
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
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  Blast E-value cutoff:
BDBM1716
n/a
NameBDBM1716
Synonyms:CHEMBL1684072 | US8470837, 17
Typen/a
Emp. Form.C16H13F2IN4O3
Mol. Mass.474.2007
SMILESCn1c2ncn(CCO)c(=O)c2c(Nc2ccc(I)cc2F)c(F)c1=O
Structure
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