| 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 | BDBM50141435 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_124012 |
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| IC50 | 255±n/a nM |
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| Citation |  Wityak, J; Hobbs, FW; Gardner, DS; Santella, JB; Petraitis, JJ; Sun, JH; Favata, MF; Daulerio, AJ; Horiuchi, KY; Copeland, RA; Scherle, PA; Jaffe, BD; Trzaskos, JM; Magolda, RL; Trainor, GL; Duncia, JV Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors. Bioorg Med Chem Lett14:1483-6 (2004) [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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| BDBM50141435 |
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| n/a |
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| Name | BDBM50141435 |
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| Synonyms: | (Z)-3-Amino-3-(2-amino-phenylsulfanyl)-2-(3-{hydroxy-[4-(2-trityl-2H-tetrazol-5-yl)-phenyl]-methyl}-phenyl)-acrylonitrile | CHEMBL430731 |
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| Type | Small organic molecule |
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| Emp. Form. | C42H33N7OS |
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| Mol. Mass. | 683.823 |
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| SMILES | Nc1ccccc1SC(=N)C(C#N)c1cccc(c1)C(O)c1ccc(cc1)-c1nnn(n1)C(c1ccccc1)(c1ccccc1)c1ccccc1 |
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| Structure | 
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