Target
Mitogen-activated protein kinase 1
Ligand
BDBM418230
Substrate
n/a
Meas. Tech.
ERK2 In vitro Inhibition Assay
IC50
1.40±n/a nM
Citation
 Berdini, VBuck, IMDay, JEGriffiths-Jones, CMHeightman, TDHoward, SMurray, CWNorton, DO''Reilly, MWoolford, AJCooke, MLCousin, DOnions, STShannon, JMWatts, 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:
BDBM418230
Synonyms:
(2R)-2-(6-{5-chloro-2-[(oxan-4- yl)amino]pyrimidin-4-yl}-1-oxo-2,3- dihydro-1H-isoindol-2-yl)-N-[(1S)-1-[3- chloro-6-(4-methylpiperazin-1- yl)pyridin-2-yl]-2- hydroxyethyl]propanamide | US10457669, Example 997 | US11001575, Example 997
Type:
Small organic molecule
Emp. Form.:
C32H38Cl2N8O4
Mol. Mass.:
669.601
SMILES:
C[C@@H](N1Cc2ccc(cc2C1=O)-c1nc(NC2CCOCC2)ncc1Cl)C(=O)N[C@H](CO)c1nc(ccc1Cl)N1CCN(C)CC1 |r|
Structure:
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