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Target
Mitogen-activated protein kinase 1
Ligand
BDBM5718
Substrate
Substrate Peptide T669
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
27000±n/a nM
Citation
 Wang, Z; Canagarajah, BJ; Boehm, JC; Kassisa, S; Cobb, MH; Young, PR; Abdel-Meguid, S; Adams, JL; Goldsmith, EJ Structural basis of inhibitor selectivity in MAP kinases. Structure 6:1117-28 (1998) [PubMed]  Article 
Target
Name:
Mitogen-activated protein kinase 1
Synonyms:
ERK-2 | ERT1 | Erk2 | Extracellular signal-regulated kinase 2 | MAP kinase 2 | MAPK 2 | MK01_RAT | Mapk | Mapk1 | Mitogen-activated protein kinase 2 | Prkm1 | p42-MAPK
Type:
Enzyme
Mol. Mass.:
41278.65
Organism:
Rattus norvegicus (rat)
Description:
MAP Kinase is the rat ERK-2 isoform containing a polyhistidine tag at the N-terminus produced in E.coli. and activated by phosphorylation with MEK1 prior to purification.
Residue:
358
Sequence:
MAAAAAAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNLNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
  
Inhibitor
Name:
BDBM5718
Synonyms:
2,6,9-Trisubstituted purine deriv. 26 | 2-{[6-(benzylamino)-9-methyl-9H-purin-2-yl]amino}ethan-1-ol | 2-{[6-(benzylamino)-9-methyl-9H-purin-2-yl]amino}ethanol | 6-(benzylamino)-2-[(2-hydroxyethyl)amino]-9-methylpurine | CHEMBL280074 | Olomoucine | purine deriv. 5
Type:
Small organic molecule
Emp. Form.:
C15H18N6O
Mol. Mass.:
298.343
SMILES:
Cn1cnc2c(NCc3ccccc3)nc(NCCO)nc12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Substrate Peptide T669
Synonyms:
epidermal growth factor receptor (EGFR) derived peptide T669
Type:
Peptide
Mol. Mass.:
2317.55
Organism:
n/a
Description:
n/a
Residue:
21
Sequence:
ERELVEPLTPSGEAPNQALLR