Reaction Details |
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Target | Dual specificity mitogen-activated protein kinase kinase 1 |
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Ligand | BDBM50194039 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_420097 (CHEMBL873739) |
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IC50 | 27±n/a nM |
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Citation | El Abdellaoui, H; Varaprasad, CV; Barawkar, D; Chakravarty, S; Maderna, A; Tam, R; Chen, H; Allan, M; Wu, JZ; Appleby, T; Yan, S; Zhang, W; Lang, S; Yao, N; Hamatake, R; Hong, Z Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors. Bioorg Med Chem Lett16:5561-6 (2006) [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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BDBM50194039 |
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n/a |
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Name | BDBM50194039 |
Synonyms: | 5-4-2-chloro-3,5-difluorophenoxy)-3-fluorophenylamino)-3-hydroxy-N-1-hydroxypropan-2-yl)isothiazole-4-carboximidamide | CHEMBL387184 |
Type | Small organic molecule |
Emp. Form. | C19H16ClF3N4O3S |
Mol. Mass. | 472.869 |
SMILES | CC(CO)N=C(N)c1c(Nc2ccc(Oc3cc(F)cc(F)c3Cl)c(F)c2)s[nH]c1=O |w:4.3| |
Structure |
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