| Reaction Details |
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 | Report a problem with these data |
| Target | Mitogen-activated protein kinase 1 |
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| Ligand | BDBM417517 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2121006 (CHEMBL4830153) |
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| IC50 | 25±n/a nM |
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| Citation |  Heightman, TD; Berdini, V; Bevan, L; Buck, IM; Carr, MG; Courtin, A; Coyle, JE; Day, JEH; East, C; Fazal, L; Griffiths-Jones, CM; Howard, S; Kucia-Tran, J; Martins, V; Muench, S; Munck, JM; Norton, D; O'Reilly, M; Palmer, N; Pathuri, P; Peakman, TM; Reader, M; Rees, DC; Rich, SJ; Shah, A; Wallis, NG; Walton, H; Wilsher, NE; Woolford, AJ; Cooke, M; Cousin, D; Onions, S; Shannon, J; Watts, J; Murray, CW Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem64:12286-12303 (2021) [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 |
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| 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 |
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| Type: | Ser/Thr Protein Kinase |
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| Mol. Mass.: | 41392.76 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P28482 |
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| Residue: | 360 |
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| Sequence: | MAAAAAAGAGPEMVRGQVFDVGPRYTNLSYIGEGAYGMVCSAYDNVNKVRVAIKKISPFE
HQTYCQRTLREIKILLRFRHENIIGINDIIRAPTIEQMKDVYIVQDLMETDLYKLLKTQH
LSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLLNTTCDLKICDFGLARVADPDHDH
TGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHI
LGILGSPSQEDLNCIINLKARNYLLSLPHKNKVPWNRLFPNADSKALDLLDKMLTFNPHK
RIEVEQALAHPYLEQYYDPSDEPIAEAPFKFDMELDDLPKEKLKELIFEETARFQPGYRS
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| BDBM417517 |
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| n/a |
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| Name | BDBM417517 |
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| Synonyms: | N-benzyl-2-(6-{5-chloro- 2-[(oxan-4-yl)amino] pyrimidin-4-yl}- 1-oxo-2,3-dihydro-1H- isoindol-2-yl)-N- methylacetamide | US10457669, Example 131 | US11001575, Example 131 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H28ClN5O3 |
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| Mol. Mass. | 505.996 |
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| SMILES | CN(Cc1ccccc1)C(=O)CN1Cc2ccc(cc2C1=O)-c1nc(NC2CCOCC2)ncc1Cl |
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| Structure | 
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