Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50176581
Substrate
n/a
Meas. Tech.
ChEMBL_330808 (CHEMBL861916)
IC50
241±n/a nM
Citation
 Chen, ZKim, SHBarbosa, SAHuynh, TTortolani, DRLeavitt, KJWei, DDManne, VRicca, CSGullo-Brown, JPoss, MAVaccaro, WSalvati, ME Pyrrolopyridazine MEK inhibitors. Bioorg Med Chem Lett 16:628-32 (2005) [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:
BDBM50176581
Synonyms:
5-methyl-4-(4-phenoxyphenylamino)H-pyrrolo[1,2-b]pyridazine-3-carbonitrile | CHEMBL201203
Type:
Small organic molecule
Emp. Form.:
C21H16N4O
Mol. Mass.:
340.3779
SMILES:
Cc1ccn2ncc(C#N)c(Nc3ccc(Oc4ccccc4)cc3)c12
Structure:
Search PDB for entries with ligand similarity: