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Target
Mitogen-activated protein kinase 1
Ligand
BDBM50456345
Substrate
n/a
Meas. Tech.
ChEMBL_1755344 (CHEMBL4190104)
IC50
76000±n/a nM
Citation
 Heightman, TD; Berdini, V; Braithwaite, H; Buck, IM; Cassidy, M; Castro, J; Courtin, A; Day, JEH; East, C; Fazal, L; Graham, B; Griffiths-Jones, CM; Lyons, JF; Martins, V; Muench, S; Munck, JM; Norton, D; O'Reilly, M; Palmer, N; Pathuri, P; Reader, M; Rees, DC; Rich, SJ; Richardson, C; Saini, H; Thompson, NT; Wallis, NG; Walton, H; Wilsher, NE; Woolford, AJ; Cooke, M; Cousin, D; Onions, S; Shannon, J; Watts, J; Murray, CW Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem 61:4978-4992 (2018) [PubMed]  Article 
Target
Name:
Mitogen-activated protein kinase 1
Synonyms:
ERK2 | ERT1 | Extracellular signal-regulated kinase 2 | Extracellular signal-regulated kinase 2 (ERK-2) | Extracellular signal-regulated kinase 2 (ERK2) | MAP Kinase 2/ERK2 | MAPK 2 | MAPK1 | MK01_HUMAN | Mitogen activated kinase 1 (ERK-2) | Mitogen-activated protein kinase 1 (ERK-2) | Mitogen-activated protein kinase 1 (ERK2) | Mitogen-activated protein kinase 2 | PRKM1 | PRKM2 | p42-MAPK
Type:
Ser/Thr Protein Kinase
Mol. Mass.:
41392.76
Organism:
Homo sapiens (Human)
Description:
P28482
Residue:
360
Sequence:
MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
  
Inhibitor
Name:
BDBM50456345
Synonyms:
CHEMBL4210146
Type:
Small organic molecule
Emp. Form.:
C10H13N5
Mol. Mass.:
203.2437
SMILES:
Cc1c(Nc2ncc(C)cn2)cnn1C
Structure:
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