| Reaction Details |
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 | Report a problem with these data |
| Target | Dual specificity mitogen-activated protein kinase kinase 1 |
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| Ligand | BDBM1711 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_726976 (CHEMBL1686836) |
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| IC50 | 3.8±n/a nM |
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| Citation |  Dong, Q; Dougan, DR; Gong, X; Halkowycz, P; Jin, B; Kanouni, T; O'Connell, SM; Scorah, N; Shi, L; Wallace, MB; Zhou, F Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Bioorg Med Chem Lett21:1315-9 (2011) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Dual specificity mitogen-activated protein kinase kinase 1 |
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| Name: | Dual specificity mitogen-activated protein kinase kinase 1 |
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| 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 |
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| Type: | Other Protein Type |
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| Mol. Mass.: | 43439.03 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Full-length human MEK-1 was generated by PCR and purified as a fusion protein from Escherichia coli lysates. |
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| Residue: | 393 |
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| Sequence: | MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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| BDBM1711 |
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| n/a |
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| Name | BDBM1711 |
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| Synonyms: | CHEMBL1684067 | US8470837, 8 |
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| Type | n/a |
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| Emp. Form. | C18H18FIN4O4 |
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| Mol. Mass. | 500.2628 |
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| SMILES | Cc1c(Nc2ccc(I)cc2F)c2c(ncn(C[C@@H](O)CO)c2=O)n(C)c1=O |r| |
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| Structure | 
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