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Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50173837
Substrate
n/a
Meas. Tech.
ChEMBL_326808 (CHEMBL860398)
IC50
800±n/a nM
Citation
 Gavrin, LK; Green, N; Hu, Y; Janz, K; Kaila, N; Li, HQ; Tam, SY; Thomason, JR; Gopalsamy, A; Ciszewski, G; Cuozzo, JW; Hall, JP; Hsu, S; Telliez, JB; Lin, LL Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships. Bioorg Med Chem Lett 15:5288-92 (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:
BDBM50173837
Synonyms:
6-(2-morpholinoethylamino)-4-(4-phenoxyphenylamino)-1,7-naphthyridine-3-carbonitrile | 6-[(2-morpholin-4-ylethyl)amino]-4-[(4-phenoxyphenyl)amino]-[1,7]naphthyridine-3-carbonitrile | CHEMBL371095
Type:
Small organic molecule
Emp. Form.:
C27H26N6O2
Mol. Mass.:
466.5343
SMILES:
N#Cc1cnc2cnc(NCCN3CCOCC3)cc2c1Nc1ccc(Oc2ccccc2)cc1
Structure:
Search PDB for entries with ligand similarity: