Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50346918
Substrate
n/a
Meas. Tech.
ChEMBL_753058 (CHEMBL1798986)
IC50
>10000±n/a nM
Citation
 Devadas, BSelness, SRXing, LMadsen, HMMarrufo, LDShieh, HMessing, DMYang, JZMorgan, HMAnderson, GDWebb, EGZhang, JDevraj, RVMonahan, JB Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors. Bioorg Med Chem Lett 21:3856-60 (2011) [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:
BDBM50346918
Synonyms:
CHEMBL1738710
Type:
Small organic molecule
Emp. Form.:
C21H18ClF2N3O4
Mol. Mass.:
449.835
SMILES:
Cc1ccc(cc1-n1cnc(OCc2ccc(F)cc2F)c(Cl)c1=O)C(=O)NCCO
Structure:
Search PDB for entries with ligand similarity: