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Target
Dual specificity mitogen-activated protein kinase kinase 1
Ligand
BDBM50014412
Substrate
n/a
Meas. Tech.
ChEMBL_1350728 (CHEMBL3266113)
IC50
1.8±n/a nM
Citation
 Lu, H; Tu, W; Fei, H; Xu, G; Hu, Q; Zhang, L; Lin, B; Yuan, J; Yin, J; Gong, A; Wan, M; Wang, D; Zhu, X; Feng, J; Wang, Q; Sun, P Structure-based design and synthesis of bicyclic fused-pyridines as MEK inhibitors. Bioorg Med Chem Lett 24:2555-9 (2014) [PubMed]  Article 
Target
Name:
Dual specificity mitogen-activated protein kinase kinase 1
Synonyms:
ERK activator kinase 1 | Mitogen-activated protein kinase 1 (MEK1) | MAPK/ERK kinase 1 (MEK1) | Dual specificity mitogen-activated protein kinase kinase 1 (MEK) | MEK-1 | MAP kinase kinase 1 | MAPK/ERK kinase 1 | Dual specificity mitogen-activated protein kinase (MEK) | Dual specificity mitogen-activated protein kinase kinase MEK1/2 | Dual specificity mitogen-activated protein kinase kinase 1 (MEK1) | MP2K1_HUMAN | MAP2K1 | MEK1 | PRKMK1 | VHL-MAP2K1/MAP2K2 | Dual specificity mitogen-activated protein kinase kinase 1/Mitogen-activated protein kinase 1/RAF proto-oncogene serine/threonine-protein kinase
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:
BDBM50014412
Synonyms:
Pimasertib | US11147816, Pimasertib (AS703026) | US11701360, Pimasertib
Type:
Small organic molecule
Emp. Form.:
C15H15FIN3O3
Mol. Mass.:
431.01
SMILES:
c1cc(c(cc1I)F)Nc2cnccc2C(=O)NC[C@@H](CO)O
Structure:
Search PDB for entries with ligand similarity: