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Target
Mitogen-activated protein kinase 1
Ligand
BDBM418160
Substrate
n/a
Meas. Tech.
ERK2 In Vitro Inhibition Assay
IC50
1.80±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
More Info.:
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:
BDBM418160
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)-1-(2-fluoro-5- methoxyphenyl)-2- hydroxyethyl]propanamide | US10457669, Example 909 | US11001575, Example 909
Type:
Small organic molecule
Emp. Form.:
C27H26ClFN8O4
Mol. Mass.:
580.998
SMILES:
COc1ccc(F)c(c1)[C@@H](CO)NC(=O)[C@@H](C)N1Cc2ccc(cc2C1=O)-c1nc(Nc2cnn(C)n2)ncc1Cl |r|