| 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 | BDBM50391809 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_850079 (CHEMBL2149502) |
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| IC50 | 44±n/a nM |
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| Citation |  Rice, KD; Aay, N; Anand, NK; Blazey, CM; Bowles, OJ; Bussenius, J; Costanzo, S; Curtis, JK; Defina, SC; Dubenko, L; Engst, S; Joshi, AA; Kennedy, AR; Kim, AI; Koltun, ES; Lougheed, JC; Manalo, JC; Martini, JF; Nuss, JM; Peto, CJ; Tsang, TH; Yu, P; Johnston, S Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973). ACS Med Chem Lett3:416-421 (2012) [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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| BDBM50391809 |
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| n/a |
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| Name | BDBM50391809 |
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| Synonyms: | CHEMBL2146887 |
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| Type | Small organic molecule |
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| Emp. Form. | C16H12F3IN2O2 |
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| Mol. Mass. | 448.1784 |
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| SMILES | OC1CN(C1)C(=O)c1ccc(F)c(F)c1Nc1ccc(I)cc1F |
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| Structure | 
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