Reaction Details Report a problem with these data
Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50341519
Substrate
n/a
Meas. Tech.
ChEMBL_742138 (CHEMBL1769198)
Ki
>1000±n/a nM
Citation
Charrier, JD; Miller, A; Kay, DP; Brenchley, G; Twin, HC; Collier, PN; Ramaya, S; Keily, SB; Durrant, SJ; Knegtel, RM; Tanner, AJ; Brown, K; Curnock, AP; Jimenez, JM Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors. J Med Chem 54:2341-50 (2011) [PubMed] Article
More 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:
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:
BDBM50341519
Synonyms:
(S)-3-(4-(2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl)benzoylamino)-5-(6-(methylamino)pyrazin-2-yl)-(1H)-pyridin-2-one | CHEMBL1765781
Type:
Small organic molecule
Emp. Form.:
C26H31N7O2
Mol. Mass.:
473.57
SMILES:
CNc1cncc(n1)-c1c[nH]c(=O)c(NC(=O)c2ccc(cc2)N2CCC[C@H]2CN2CCCC2)c1 |r|