Reaction Details Report a problem with these data
Target
Mitogen-activated protein kinase 1
Ligand
BDBM15239
Substrate
Substrate Peptide T669
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
18000±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:
BDBM15239
Synonyms:
4-[4-(4-fluorophenyl)-1-(piperidin-4-yl)-1H-imidazol-5-yl]pyrimidin-2-amine | 4-[5-(4-fluorophenyl)-3-(4-piperidyl)imidazol-4-yl]pyrimidin-2-amine | CHEMBL274064 | SB220025 | SB4
Type:
Small organic molecule
Emp. Form.:
C18H19FN6
Mol. Mass.:
338.3821
SMILES:
Nc1nccc(n1)-c1c(ncn1C1CCNCC1)-c1ccc(F)cc1
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