Reaction Details |
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Target | Dual specificity mitogen-activated protein kinase kinase 1 |
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Ligand | BDBM50134969 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1544506 (CHEMBL3750088) |
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IC50 | 37±n/a nM |
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Citation | Hartung, IV; Hammer, S; Hitchcock, M; Neuhaus, R; Scholz, A; Siemeister, G; Bohlmann, R; Hillig, RC; Pühler, F Optimization of allosteric MEK inhibitors. Part 2: Taming the sulfamide group balances compound distribution properties. Bioorg Med Chem Lett26:186-93 (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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BDBM50134969 |
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n/a |
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Name | BDBM50134969 |
Synonyms: | CHEMBL3746923 |
Type | Small organic molecule |
Emp. Form. | C20H17F2IN4O4S |
Mol. Mass. | 574.34 |
SMILES | NC(=O)c1c(Nc2ccc(I)cc2F)cc(F)cc1Oc1cccc(CNS(N)(=O)=O)c1 |
Structure |
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