Reaction Details |
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Target | Mitogen-activated protein kinase 1/3 |
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Ligand | BDBM50419247 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_772881 (CHEMBL1838284) |
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IC50 | 79±n/a nM |
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Citation | Liddle, J; Atkinson, FL; Barker, MD; Carter, PS; Curtis, NR; Davis, RP; Douault, C; Dickson, MC; Elwes, D; Garton, NS; Gray, M; Hayhow, TG; Hobbs, CI; Jones, E; Leach, S; Leavens, K; Lewis, HD; McCleary, S; Neu, M; Patel, VK; Preston, AG; Ramirez-Molina, C; Shipley, TJ; Skone, PA; Smithers, N; Somers, DO; Walker, AL; Watson, RJ; Weingarten, GG Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. Bioorg Med Chem Lett21:6188-94 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Mitogen-activated protein kinase 1/3 |
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Name: | Mitogen-activated protein kinase 1/3 |
Synonyms: | Mitogen-activated protein kinase; ERK1/ERK2 | pERK1/2 | t-ERK1/2 |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 124147 |
Components: | This complex has 2 components. |
Component 1 |
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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Component 2 |
Name: | Mitogen-activated protein kinase 3 |
Synonyms: | ERK1 | ERK1/ERK2 | Extracellular signal-regulated kinase 1 | Extracellular signal-regulated kinase 1 (ERK1) | MAP kinase ERK1 | MAPK3 | MAPK3/MAPK7 | MK03_HUMAN | Mitogen-activated protein kinase | Mitogen-activated protein kinase 3 | PRKM3 |
Type: | Protein |
Mol. Mass.: | 43136.58 |
Organism: | Homo sapiens (Human) |
Description: | curated by PDB 4QTB |
Residue: | 379 |
Sequence: | MAAAAAQGGGGGEPRRTEGVGPGVPGEVEMVKGQPFDVGPRYTQLQYIGEGAYGMVSSAY
DHVRKTRVAIKKISPFEHQTYCQRTLREIQILLRFRHENVIGIRDILRASTLEAMRDVYI
VQDLMETDLYKLLKSQQLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLINTTCDL
KICDFGLARIADPEHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLS
NRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINMKARNYLQSLPSKTKVAWAKLFPKSD
SKALDLLDRMLTFNPNKRITVEEALAHPYLEQYYDPTDEPVAEEPFTFAMELDDLPKERL
KELIFQETARFQPGVLEAP
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BDBM50419247 |
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n/a |
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Name | BDBM50419247 |
Synonyms: | CHEMBL1835071 | US8470835, 1 |
Type | Small organic molecule |
Emp. Form. | C17H22N6O2 |
Mol. Mass. | 342.3956 |
SMILES | Cc1ccc(Nc2nc(N[C@@H]3CCOC[C@@H]3N)ncc2C(N)=O)cc1 |r| |
Structure |
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