Target
Mitogen-activated protein kinase 1
Ligand
BDBM418273
Substrate
n/a
Meas. Tech.
ERK2 In vitro Inhibition Assay
IC50
1.70±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:
Human
Description:
P28482
Residue:
360
Sequence:
MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFEHQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQHLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHKRIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
  
Inhibitor
Name:
BDBM418273
Synonyms:
(2R)-2-(6-{5-chloro-2-[(2-methyl-2H- 1,2,3-triazol-4-yl)amino]pyrimidin-4- yl}-1-oxo-2,3-dihydro-1H-isoindol-2- yl)-N-[(1S)-146-(dimethylamino)-3- fluoropyridin-2-yl]-2- hydroxyethyl]propanamide | US10457669, Example 1058 | US11001575, Example 1058
Type:
Small organic molecule
Emp. Form.:
C27H28ClFN10O3
Mol. Mass.:
595.028
SMILES:
C[C@@H](N1Cc2ccc(cc2C1=O)-c1nc(Nc2cnn(C)n2)ncc1Cl)C(=O)N[C@H](CO)c1nc(ccc1F)N(C)C |r|
Structure:
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