Reaction Details |
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Target | Mitogen-activated protein kinase 1 |
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Ligand | BDBM418273 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ERK2 In Vitro Inhibition Assay |
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IC50 | 1.70±n/a nM |
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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 |
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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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BDBM418273 |
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n/a |
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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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