| Reaction Details |
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 | Report a problem with these data |
| Target | MAP kinase-activated protein kinase 5 |
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| Ligand | BDBM50359359 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_793916 (CHEMBL1932889) |
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| IC50 | >30000±n/a nM |
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| Citation |  Moffett, K; Konteatis, Z; Nguyen, D; Shetty, R; Ludington, J; Fujimoto, T; Lee, KJ; Chai, X; Namboodiri, H; Karpusas, M; Dorsey, B; Guarnieri, F; Bukhtiyarova, M; Springman, E; Michelotti, E Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD). Bioorg Med Chem Lett21:7155-65 (2011) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| MAP kinase-activated protein kinase 5 |
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| Name: | MAP kinase-activated protein kinase 5 |
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| Synonyms: | MAP kinase-activated protein kinase 5 (PRAK) | MAPK-Activated Protein Kinase 5 (MK5) | MAPK-activated protein kinase 5 | MAPK5_HUMAN | MAPKAP kinase 5 | MAPKAPK5 | PRAK | p38-regulated/activated protein kinase | p38-regulated/activated protein kinase (PRAK) |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 54229.92 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant MAPKAPK5 was phosphorylated by incubation with active p38alpha before assays. |
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| Residue: | 473 |
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| Sequence: | MSEESDMDKAIKETSILEEYSINWTQKLGAGISGPVRVCVKKSTQERFALKILLDRPKAR
NEVRLHMMCATHPNIVQIIEVFANSVQFPHESSPRARLLIVMEMMEGGELFHRISQHRHF
TEKQASQVTKQIALALRHCHLLNIAHRDLKPENLLFKDNSLDAPVKLCDFGFAKIDQGDL
MTPQFTPYYVAPQVLEAQRRHQKEKSGIIPTSPTPYTYNKSCDLWSLGVIIYVMLCGYPP
FYSKHHSRTIPKDMRRKIMTGSFEFPEEEWSQISEMAKDVVRKLLKVKPEERLTIEGVLD
HPWLNSTEALDNVLPSAQLMMDKAVVAGIQQAHAEQLANMRIQDLKVSLKPLHSVNNPIL
RKRKLLGTKPKDSVYIHDHENGAEDSNVALEKLRDVIAQCILPQAGKGENEDEKLNEVMQ
EAWKYNRECKLLRDTLQSFSWNGRGFTDKVDRLKLAEIVKQVIEEQTTSHESQ
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| BDBM50359359 |
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| n/a |
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| Name | BDBM50359359 |
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| Synonyms: | CHEMBL1929238 |
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| Type | Small organic molecule |
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| Emp. Form. | C25H33Cl2N5O3S |
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| Mol. Mass. | 554.532 |
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| SMILES | CN(C)CCN1CCN(CCC1=O)C(=O)c1cc(sc1NC(=O)Nc1cccc(Cl)c1Cl)C(C)(C)C |
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| Structure | 
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