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Target
Mitogen-activated protein kinase 1
Ligand
BDBM6878
Substrate
ERK-2 Peptide Substrate
Meas. Tech.
Kinase Inhibition Assay
IC50
1000±n/a nM
Citation
 Lin, R; Connolly, PJ; Huang, S; Wetter, SK; Lu, Y; Murray, WV; Emanuel, SL; Gruninger, RH; Fuentes-Pesquera, AR; Rugg, CA; Middleton, SA; Jolliffe, LK 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem 48:4208-11 (2005) [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:
BDBM6878
Synonyms:
1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3n | 5-amino-N-(2,6-difluorophenyl)-3-[(4-sulfamoylphenyl)amino]-1H-1,2,4-triazole-1-carbothioamide
Type:
Small organic molecule
Emp. Form.:
C15H13F2N7O2S2
Mol. Mass.:
425.436
SMILES:
Nc1nc(Nc2ccc(cc2)S(N)(=O)=O)nn1C(=S)Nc1c(F)cccc1F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
ERK-2 Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1969.25
Organism:
n/a
Description:
n/a
Residue:
18
Sequence:
ITINAPRTPGGRRAMIDE