| Reaction Details |
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 | Report a problem with these data |
| Target | Mitogen-activated protein kinase 1 |
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| Ligand | BDBM418315 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_2121006 (CHEMBL4830153) |
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| IC50 | 2.8±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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| BDBM418315 |
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| n/a |
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| Name | BDBM418315 |
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| Synonyms: | (2R)-2-(3-{5-chloro-2-[(oxan-4- yl)amino]pyrimidin-4-yl}-5-oxo- 5H,6H,7H-pyrrolo[3,4-b]pyridin-6-yl)- N-[(1S)-1-(3-fluoro-5-methoxyphenyl)- 2-hydroxyethyl]propanamide | US10457669, Example 1126 | US11001575, Example 1126 |
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| Type | Small organic molecule |
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| Emp. Form. | C28H30ClFN6O5 |
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| Mol. Mass. | 585.026 |
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| SMILES | COc1cc(F)cc(c1)[C@@H](CO)NC(=O)[C@@H](C)N1Cc2ncc(cc2C1=O)-c1nc(NC2CCOCC2)ncc1Cl |r| |
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| Structure | 
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