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Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM28124
Substrate
n/a
Meas. Tech.
ChEMBL_60730 (CHEMBL672143)
IC50
1.1±n/a nM
Citation
 Zhang, N; Wu, B; Eudy, N; Wang, Y; Ye, F; Powell, D; Wissner, A; Feldberg, LR; Kim, SC; Mallon, R; Kovacs, ED; Toral-Barza, L; Kohler, CA MEK (MAPKK) inhibitors. Part 2: structure-activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines. Bioorg Med Chem Lett 11:1407-10 (2001) [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:
BDBM28124
Synonyms:
3-cyanoquinoline, 9 | 6-methoxy-7-[3-(morpholin-4-yl)propoxy]-4-{[4-(phenylsulfanyl)phenyl]amino}quinoline-3-carbonitrile | CHEMBL29714
Type:
Small organic molecule
Emp. Form.:
C30H30N4O3S
Mol. Mass.:
526.649
SMILES:
COc1cc2c(Nc3ccc(Sc4ccccc4)cc3)c(cnc2cc1OCCCN1CCOCC1)C#N
Structure:
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