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TargetDual specificity mitogen-activated protein kinase kinase 1
LigandBDBM50194027
Substrate/Competitorn/a
Meas. Tech.ChEMBL_420098 (CHEMBL873740)
EC50 37±n/a nM
Citation El Abdellaoui, HVaraprasad, CVBarawkar, DChakravarty, SMaderna, ATam, RChen, HAllan, MWu, JZAppleby, TYan, SZhang, WLang, SYao, NHamatake, RHong, Z Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors. Bioorg Med Chem Lett16:5561-6 (2006) [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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50194027
n/a
NameBDBM50194027
Synonyms:5-3-chloro-4-2-chloro-4-fluorophenoxy)phenylamino)-3-hydroxy-N-1-hydroxypropan-2-yl)isothiazole-4-carboximidamide | CHEMBL384784
TypeSmall organic molecule
Emp. Form.C19H17Cl2FN4O3S
Mol. Mass.471.333
SMILESCC(CO)N=C(N)c1c(Nc2ccc(Oc3ccc(F)cc3Cl)c(Cl)c2)s[nH]c1=O |w:4.3|
Structure
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