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Target
Mitogen-activated protein kinase 1
Ligand
BDBM157161
Substrate
n/a
Meas. Tech.
ChEMBL_1923496 (CHEMBL4426452)
IC50
0.500000±n/a nM
Citation
 Lim, J; Kelley, EH; Methot, JL; Zhou, H; Petrocchi, A; Chen, H; Hill, SE; Hinton, MC; Hruza, A; Jung, JO; Maclean, JK; Mansueto, M; Naumov, GN; Philippar, U; Raut, S; Spacciapoli, P; Sun, D; Siliphaivanh, P Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers. J Med Chem 59:6501-11 (2016) [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:
BDBM157161
Synonyms:
US9023865, 5
Type:
Small organic molecule
Emp. Form.:
C21H20N6O
Mol. Mass.:
372.4231
SMILES:
Cc1cc(ccn1)-c1n[nH]c2cc(NC(=O)NCCc3ccccc3)ncc12
Structure:
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