Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50115298
Substrate
n/a
Meas. Tech.
ChEMBL_123854 (CHEMBL731429)
IC50
>30000±n/a nM
Citation
 Matsuno, KIchimura, MNakajima, TTahara, KFujiwara, SKase, HUshiki, JGiese, NAPandey, AScarborough, RMLokker, NAYu, JCIrie, JTsukuda, EIde, SOda, SNomoto, Y Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 1. Synthesis, structure-activity relationship, and biological effects of a new class of quinazoline derivatives. J Med Chem 45:3057-66 (2002) [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:
BDBM50115298
Synonyms:
4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carboxylic acid (4-bromo-phenyl)-amide | CHEMBL323336
Type:
Small organic molecule
Emp. Form.:
C21H22BrN5O3
Mol. Mass.:
472.335
SMILES:
COc1cc2ncnc(N3CCN(CC3)C(=O)Nc3ccc(Br)cc3)c2cc1OC
Structure:
Search PDB for entries with ligand similarity: