Reaction Details |
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Target | Dual specificity mitogen-activated protein kinase kinase 1 |
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Ligand | BDBM50094314 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1503906 (CHEMBL3593139) |
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IC50 | 3400±n/a nM |
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Citation | Ward, RA; Colclough, N; Challinor, M; Debreczeni, JE; Eckersley, K; Fairley, G; Feron, L; Flemington, V; Graham, MA; Greenwood, R; Hopcroft, P; Howard, TD; James, M; Jones, CD; Jones, CR; Renshaw, J; Roberts, K; Snow, L; Tonge, M; Yeung, K Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2. J Med Chem58:4790-801 (2015) [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 |
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: | MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKV
GELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHE
CNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYL
REKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHY
SVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSY
GMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAF
IKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
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BDBM50094314 |
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n/a |
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Name | BDBM50094314 |
Synonyms: | CHEMBL3590108 |
Type | Small organic molecule |
Emp. Form. | C19H22O7 |
Mol. Mass. | 362.3738 |
SMILES | COc1cc(O)c2c(c1)\C=C\C[C@H](O)[C@@H](O)C(=O)\C=C\C[C@H](C)OC2=O |r,t:10,19| |
Structure |
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