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Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50180564
Substrate
n/a
Meas. Tech.
ChEMBL_327163 (CHEMBL859549)
IC50
6.8±n/a nM
Citation
 Wallace, EM; Lyssikatos, J; Blake, JF; Seo, J; Yang, HW; Yeh, TC; Perrier, M; Jarski, H; Marsh, V; Poch, G; Livingston, MG; Otten, J; Hingorani, G; Woessner, R; Lee, P; Winkler, J; Koch, K Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones. J Med Chem 49:441-4 (2006) [PubMed]  Article 
Target
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:
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAFIKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
  
Inhibitor
Name:
BDBM50180564
Synonyms:
4-(4-bromo-2-fluorophenylamino)-N-(cyclopropylmethoxy)-5-fluoro-1-methyl-6-oxo-1,6-dihydropyridine-3-carboxamide | CHEMBL201629
Type:
Small organic molecule
Emp. Form.:
C17H16BrF2N3O3
Mol. Mass.:
428.228
SMILES:
Cn1cc(C(=O)NOCC2CC2)c(Nc2ccc(Br)cc2F)c(F)c1=O
Structure:
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