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Target
Mitogen-activated protein kinase 1
Ligand
BDBM418307
Substrate
n/a
Meas. Tech.
ERK2 In vitro Inhibition Assay
IC50
1.50±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  US11001575 Publication Date 5/11/2021 
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:
BDBM418307
Synonyms:
(2R)-2-(6-}5-chloro-2-[(oxetan-3- yl)amino]pyrimidin-4-yl}-1-oxo-2,3- dihydro-1H-isoindol-2-yl)-N-[(1R)-1-[3- fluoro-5-(4-methylpiperazin-1- yl)phenyl]ethyl]propanamide | US10457669, Example 1114 | US11001575, Example 1114
Type:
Small organic molecule
Emp. Form.:
C31H35ClFN7O3
Mol. Mass.:
608.106
SMILES:
C[C@@H](NC(=O)[C@@H](C)N1Cc2ccc(cc2C1=O)-c1nc(NC2COC2)ncc1Cl)c1cc(F)cc(c1)N1CCN(C)CC1 |r|
Structure:
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