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Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50550043
Substrate
n/a
Meas. Tech.
ChEMBL_2026207 (CHEMBL4680020)
Kd
660±n/a nM
Citation
 Di Fruscia, P; Edfeldt, F; Shamovsky, I; Collie, GW; Aagaard, A; Barlind, L; Börjesson, U; Hansson, EL; Lewis, RJ; Nilsson, MK; Öster, L; Pemberton, J; Ripa, L; Storer, RI; Käck, H Fragment-Based Discovery of Novel Allosteric MEK1 Binders. ACS Med Chem Lett 12:302-308 (2021) [PubMed]  Article 
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:
BDBM50550043
Synonyms:
CHEMBL4795273
Type:
Small organic molecule
Emp. Form.:
C12H14N2O3S
Mol. Mass.:
266.316
SMILES:
COc1ccc(NC(=O)[C@H]2SCCNC2=O)cc1 |r|
Structure:
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