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Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50187857
Substrate
n/a
Meas. Tech.
ChEMBL_383093 (CHEMBL867341)
IC50
350±n/a nM
Citation
 Varaprasad, CV; Barawkar, D; El Abdellaoui, H; Chakravarty, S; Allan, M; Chen, H; Zhang, W; Wu, JZ; Tam, R; Hamatake, R; Lang, S; Hong, Z Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors. Bioorg Med Chem Lett 16:3975-80 (2006) [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:
BDBM50187857
Synonyms:
CHEMBL377592 | methyl 4-(4-(N-(cyclohexylmethyl)carbamimidoyl)-3-hydroxyisothiazol-5-ylamino)benzoate
Type:
Small organic molecule
Emp. Form.:
C19H24N4O3S
Mol. Mass.:
388.484
SMILES:
COC(=O)c1ccc(Nc2s[nH]c(=O)c2C(=N)NCC2CCCCC2)cc1
Structure:
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