Reaction Details  Report a problem with these data
Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50072154
Substrate
n/a
Meas. Tech.
ChEBML_100238
IC50
300±n/a nM
Citation
 Duncia, JV; Santella, JB; Higley, CA; Pitts, WJ; Wityak, J; Frietze, WE; Rankin, FW; Sun, JH; Earl, RA; Tabaka, AC; Teleha, CA; Blom, KF; Favata, MF; Manos, EJ; Daulerio, AJ; Stradley, DA; Horiuchi, K; Copeland, RA; Scherle, PA; Trzaskos, JM; Magolda, RL; Trainor, GL; Wexler, RR; Hobbs, FW; Olson, RE MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg Med Chem Lett 8:2839-44 (1999) [PubMed]
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:
BDBM50072154
Synonyms:
2,3-Bis-[1-amino-1-(2-hydroxy-phenylsulfanyl)-meth-(Z)-ylidene]-succinonitrile | CHEMBL95069
Type:
Small organic molecule
Emp. Form.:
C18H14N4O2S2
Mol. Mass.:
382.459
SMILES:
Oc1ccccc1SC(=N)C(C#N)C(C#N)C(=N)Sc1ccccc1O
Structure:
Search PDB for entries with ligand similarity: