Reaction Details Report a problem with these data
Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM204729
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, D; Zhu, L; Hu, Y; Wang, S; Yu, R; Hu, W; Liang, Z; Liu, X; Hu, 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:
BDBM204729
Synonyms:
6-(2-fluoro-4-iodophenylamino)-n-(2-hydroxyethoxy)-2,5-dimethyl-4-oxo-4,5-dihydrofuro[3,2-c]pyridine-7-carboxamide | US9540396, 2
Type:
Small organic molecule
Emp. Form.:
C18H17FIN3O5
Mol. Mass.:
501.2476
SMILES:
Cc1cc2c(o1)c(C(=O)NOCCO)c(Nc1ccc(I)cc1F)n(C)c2=O
Structure:
Search PDB for entries with ligand similarity: