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TargetDual specificity mitogen-activated protein kinase kinase 1
LigandBDBM50134969
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1544506 (CHEMBL3750088)
IC50 37±n/a nM
Citation Hartung, IVHammer, SHitchcock, MNeuhaus, RScholz, ASiemeister, GBohlmann, RHillig, RCPühler, F Optimization of allosteric MEK inhibitors. Part 2: Taming the sulfamide group balances compound distribution properties. Bioorg Med Chem Lett26:186-93 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Dual specificity mitogen-activated protein kinase kinase 1
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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  Blast E-value cutoff:
BDBM50134969
n/a
NameBDBM50134969
Synonyms:CHEMBL3746923
TypeSmall organic molecule
Emp. Form.C20H17F2IN4O4S
Mol. Mass.574.34
SMILESNC(=O)c1c(Nc2ccc(I)cc2F)cc(F)cc1Oc1cccc(CNS(N)(=O)=O)c1
Structure
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