Reaction Details |
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Target | Mitogen-activated protein kinase 1 |
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Ligand | BDBM50456356 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1755344 (CHEMBL4190104) |
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IC50 | 2.5±n/a nM |
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Citation | Heightman, TD; Berdini, V; Braithwaite, H; Buck, IM; Cassidy, M; Castro, J; Courtin, A; Day, JEH; East, C; Fazal, L; Graham, B; Griffiths-Jones, CM; Lyons, JF; Martins, V; Muench, S; Munck, JM; Norton, D; O'Reilly, M; Palmer, N; Pathuri, P; Reader, M; Rees, DC; Rich, SJ; Richardson, C; Saini, H; Thompson, NT; Wallis, NG; Walton, H; Wilsher, NE; Woolford, AJ; Cooke, M; Cousin, D; Onions, S; Shannon, J; Watts, J; Murray, CW Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem61:4978-4992 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Mitogen-activated protein kinase 1 |
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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: | MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFE
HQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQH
LSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDH
TGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHI
LGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHK
RIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
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BDBM50456356 |
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n/a |
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Name | BDBM50456356 |
Synonyms: | CHEMBL4209691 | US11001575, Example 674 |
Type | Small organic molecule |
Emp. Form. | C28H30ClN5O4 |
Mol. Mass. | 536.022 |
SMILES | C[C@@H](N1Cc2ccc(cc2C1=O)-c1nc(NC2CCOCC2)ncc1Cl)C(=O)N[C@H](CO)c1ccccc1 |r| |
Structure |
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