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Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM206104
Substrate
n/a
Meas. Tech.
ChEMBL_1654859 (CHEMBL4004225)
IC50
>50000±n/a nM
Citation
Miura, T; Matsuo, A; Muraoka, T; Ide, M; Morikami, K; Kamikawa, T; Nishihara, M; Kashiwagi, H Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries. Bioorg Med Chem Lett 27:1031-1036 (2017) [PubMed] ArticleMore Info.:
Target
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:
MPKKKPTPIQLNPAPDGSAVNGTSSAETNLEALQKKLEELELDEQQRKRLEAFLTQKQKVGELKDDDFEKISELGAGNGGVVFKVSHKPSGLVMARKLIHLEIKPAIRNQIIRELQVLHECNSPYIVGFYGAFYSDGEISICMEHMDGGSLDQVLKKAGRIPEQILGKVSIAVIKGLTYLREKHKIMHRDVKPSNILVNSRGEIKLCDFGVSGQLIDSMANSFVGTRSYMSPERLQGTHYSVQSDIWSMGLSLVEMAVGRYPIPPPDAKELELMFGCQVEGDAAETPPRPRTPGRPLSSYGMDSRPPMAIFELLDYIVNEPPPKLPSGVFSLEFQDFVNKCLIKNPAERADLKQLMVHAFIKRSDAEEVDFAGWLCSTIGLNQPSTPTHAAGV
Inhibitor
Name:
BDBM206104
Synonyms:
US9255110, 17
Type:
Small organic molecule
Emp. Form.:
C17H12N4O2S
Mol. Mass.:
336.368
SMILES:
COc1cc2ncccc2cc1NC(=O)c1csc2cncnc12
Structure:
