Reaction Details |
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Target | Dual specificity mitogen-activated protein kinase kinase 1 |
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Ligand | BDBM50429867 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_944312 (CHEMBL2344412) |
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IC50 | >3500±n/a nM |
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Citation | Takeuchi, CS; Kim, BG; Blazey, CM; Ma, S; Johnson, HW; Anand, NK; Arcalas, A; Baik, TG; Buhr, CA; Cannoy, J; Epshteyn, S; Joshi, A; Lara, K; Lee, MS; Wang, L; Leahy, JW; Nuss, JM; Aay, N; Aoyama, R; Foster, P; Lee, J; Lehoux, I; Munagala, N; Plonowski, A; Rajan, S; Woolfrey, J; Yamaguchi, K; Lamb, P; Miller, N Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR). J Med Chem56:2218-34 (2013) [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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BDBM50429867 |
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n/a |
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Name | BDBM50429867 |
Synonyms: | CHEMBL2333365 |
Type | Small organic molecule |
Emp. Form. | C23H22FN3O4S |
Mol. Mass. | 455.502 |
SMILES | Cc1c(F)c(ccc1C(=O)N1CCOc2ccc(cc2C1)-c1ccc(N)nc1)S(C)(=O)=O |
Structure |
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