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Target
Mitogen-activated protein kinase 1
Ligand
BDBM418188
Substrate
n/a
Meas. Tech.
ERK2 In Vitro Inhibition Assay
IC50
1.30±n/a nM
Citation
 Berdini, V; Buck, IM; Day, JE; Griffiths-Jones, CM; Heightman, TD; Howard, S; Murray, CW; Norton, D; O Reilly, M; Woolford, AJ; Cooke, ML; Cousin, D; Onions, ST; Shannon, JM; Watts, JP Benzolactam compounds as protein kinase inhibitors US Patent  US10457669 Publication Date 10/29/2019 
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:
BDBM418188
Synonyms:
2-[(1R)-5-{5-chloro-2-[(oxan-4- yl)amino]pyrimidin-4-yl}-1-methoxy-3- oxo-2,3-dihydro-1H-isoindol-2-yl]-N- [(1S)-1-(3-fluoro-5-methoxyphenyl)-2- hydroxyethyl]acetamide | US10457669, Example 947 | US11001575, Example 947
Type:
Small organic molecule
Emp. Form.:
C29H31ClFN5O6
Mol. Mass.:
600.038
SMILES:
CO[C@H]1N(CC(=O)N[C@H](CO)c2cc(F)cc(OC)c2)C(=O)c2cc(ccc12)-c1nc(NC2CCOCC2)ncc1Cl |r|
Structure:
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