Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM204742
Substrate
n/a
Meas. Tech.
Enzymatic Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
<500±0 nM
Comments
extracted
Citation
 Xiao, DZhu, LHu, YWang, SYu, RHu, WLiang, ZLiu, XHu, Q 6-arylamino pyridone carboxamide as MEK inhibitors US Patent  US9540396 Publication Date 1/10/2017 
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:
BDBM204742
Synonyms:
6-(2-fluoro-4-iodophenylamino)-n-methoxy-5-methyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridine-7-carboxamide | US9540396, 13
Type:
Small organic molecule
Emp. Form.:
C16H13FIN3O4
Mol. Mass.:
457.195
SMILES:
CONC(=O)c1c(Nc2ccc(I)cc2F)n(C)c(=O)c2ccoc12
Structure:
Search PDB for entries with ligand similarity: