Reaction Details
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Mitogen-activated protein kinase 1
Ligand
BDBM100152
Substrate
n/a
Meas. Tech.
ChEMBL_875247 (CHEMBL2187129)
IC50
>30000±n/a nM
Citation
Tahtouh, T; Elkins, JM; Filippakopoulos, P; Soundararajan, M; Burgy, G; Durieu, E; Cochet, C; Schmid, RS; Lo, DC; Delhommel, F; Oberholzer, AE; Pearl, LH; Carreaux, F; Bazureau, JP; Knapp, S; Meijer, 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 More Info.:
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:
BDBM100152
Synonyms:
7-methoxy-1-methyl-9H-beta-carboline;hydrochloride | 7-methoxy-1-methyl-9H-pyrido[3,4-b]indole;hydrochloride | HARMINE | Harmine hydrochloride | MLS002153910 | SMR001233259 | cid_5359389
Type:
Small organic molecule
Emp. Form.:
C13H12N2O
Mol. Mass.:
212.2472
SMILES:
COc1ccc2c(c1)[nH]c1c(C)nccc21
Structure:
