Target
Mitogen-activated protein kinase 1
Ligand
BDBM50292406
Substrate
n/a
Meas. Tech.
ChEMBL_875247 (CHEMBL2187129)
IC50
>10000±n/a nM
Citation
 Tahtouh, TElkins, JMFilippakopoulos, PSoundararajan, MBurgy, GDurieu, ECochet, CSchmid, RSLo, DCDelhommel, FOberholzer, AEPearl, LHCarreaux, FBazureau, JPKnapp, SMeijer, L Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. J Med Chem 55:9312-30 (2012) [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:
BDBM50292406
Synonyms:
CHEMBL485053 | leucettamine B
Type:
Small organic molecule
Emp. Form.:
C12H11N3O3
Mol. Mass.:
245.234
SMILES:
CN1C(N)=NC(=Cc2ccc3OCOc3c2)C1=O |w:6.6,c:3|
Structure:
Search PDB for entries with ligand similarity: