| 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 | BDBM50265962 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1700381 (CHEMBL4051363) |
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| IC50 | >10000±n/a nM |
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| Citation |  Ward, RA; Bethel, P; Cook, C; Davies, E; Debreczeni, JE; Fairley, G; Feron, L; Flemington, V; Graham, MA; Greenwood, R; Griffin, N; Hanson, L; Hopcroft, P; Howard, TD; Hudson, J; James, M; Jones, CD; Jones, CR; Lamont, S; Lewis, R; Lindsay, N; Roberts, K; Simpson, I; St-Gallay, S; Swallow, S; Tang, J; Tonge, M; Wang, Z; Zhai, B Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point. J Med Chem60:3438-3450 (2017) [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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| BDBM50265962 |
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| n/a |
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| Name | BDBM50265962 |
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| Synonyms: | CHEMBL4101072 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H24N8O |
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| Mol. Mass. | 428.4897 |
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| SMILES | Cc1cccc(CN2CCn3cc(cc3C2=O)-c2nc(Nc3ccnn3C)ncc2C)n1 |
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| Structure | 
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