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Target
Mitogen-activated protein kinase 1
Ligand
BDBM418192
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  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:
BDBM418192
Synonyms:
2-{6-[5-chloro-2- (methylamino)pyrimidin-4-yl]-1-oxo- 2,3-dihydro-1H-isoindol-2-yl}-N-[1-(3- fluoro-5-methylphenyl)-2- hydroxybutyl]acetamide | US10457669, Example 952 | US10457669, Example 953 | US11001575, Example 952
Type:
Small organic molecule
Emp. Form.:
C26H27ClFN5O3
Mol. Mass.:
511.976
SMILES:
CCC(O)C(NC(=O)CN1Cc2ccc(cc2C1=O)-c1nc(NC)ncc1Cl)c1cc(C)cc(F)c1
Structure:
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