Reaction Details |
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Target | Dual specificity mitogen-activated protein kinase kinase 1 |
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Ligand | BDBM50209673 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1633897 (CHEMBL3876689) |
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IC50 | 1300±n/a nM |
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Citation | Tan, L; Gurbani, D; Weisberg, EL; Hunter, JC; Li, L; Jones, DS; Ficarro, SB; Mowafy, S; Tam, CP; Rao, S; Du, G; Griffin, JD; Sorger, PK; Marto, JA; Westover, KD; Gray, NS Structure-guided development of covalent TAK1 inhibitors. Bioorg Med Chem25:838-846 (2017) [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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BDBM50209673 |
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n/a |
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Name | BDBM50209673 |
Synonyms: | CHEMBL3883761 |
Type | Small organic molecule |
Emp. Form. | C25H28N6O3 |
Mol. Mass. | 460.5282 |
SMILES | COc1cnc(Nc2ccc(cc2)N2CCN(C)CC2)nc1Oc1ccccc1NC(=O)C=C |
Structure |
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