Reaction Details |
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Target | Dual specificity mitogen-activated protein kinase kinase 1 |
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Ligand | BDBM50030881 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1441613 (CHEMBL3377059) |
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IC50 | >20000±n/a nM |
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Citation | Deng, Y; Shipps, GW; Cooper, A; English, JM; Annis, DA; Carr, D; Nan, Y; Wang, T; Zhu, HY; Chuang, CC; Dayananth, P; Hruza, AW; Xiao, L; Jin, W; Kirschmeier, P; Windsor, WT; Samatar, AA Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. J Med Chem57:8817-26 (2014) [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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BDBM50030881 |
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n/a |
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Name | BDBM50030881 |
Synonyms: | CHEMBL3356117 |
Type | Small organic molecule |
Emp. Form. | C25H29ClN4O4 |
Mol. Mass. | 484.975 |
SMILES | CC(=O)c1ccc(cc1)N1CCN(CC1)C(=O)CN1CC[C@H](C1)C(=O)Nc1ccc(O)c(Cl)c1 |r| |
Structure |
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