Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50180559
Substrate
n/a
Meas. Tech.
ChEMBL_327163 (CHEMBL859549)
IC50
6786±n/a nM
Citation
 Wallace, EMLyssikatos, JBlake, JFSeo, JYang, HWYeh, TCPerrier, MJarski, HMarsh, VPoch, GLivingston, MGOtten, JHingorani, GWoessner, RLee, PWinkler, JKoch, 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:
BDBM50180559
Synonyms:
4-(4-bromo-2-chlorophenylamino)-5-chloro-N-(2-hydroxyethoxy)-6-methoxynicotinamide | CHEMBL201136
Type:
Small organic molecule
Emp. Form.:
C15H14BrClFN3O4
Mol. Mass.:
434.645
SMILES:
COc1ncc(C(=O)NOCCO)c(Nc2ccc(Br)cc2F)c1Cl
Structure:
Search PDB for entries with ligand similarity: