Reaction Details |
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Target | MAP kinase-activated protein kinase 5 |
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Ligand | BDBM50365791 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_806119 (CHEMBL1960722) |
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IC50 | 1420±n/a nM |
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Citation | Andrews, MJ; Clase, JA; Bar, G; Tricarico, G; Edwards, PJ; Brys, R; Chambers, M; Schmidt, W; MacLeod, A; Hirst, K; Allen, V; Birault, V; Le, J; Harris, J; Self, A; Nash, K; Dixon, G Discovery of a series of imidazopyrazine small molecule inhibitors of the kinase MAPKAPK5, that show activity using in vitro and in vivo models of rheumatoid arthritis. Bioorg Med Chem Lett22:2266-70 (2012) [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 |
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) |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 54229.92 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant MAPKAPK5 was phosphorylated by incubation with active p38alpha before assays. |
Residue: | 473 |
Sequence: | MSEESDMDKAIKETSILEEYSINWTQKLGAGISGPVRVCVKKSTQERFALKILLDRPKAR
NEVRLHMMCATHPNIVQIIEVFANSVQFPHESSPRARLLIVMEMMEGGELFHRISQHRHF
TEKQASQVTKQIALALRHCHLLNIAHRDLKPENLLFKDNSLDAPVKLCDFGFAKIDQGDL
MTPQFTPYYVAPQVLEAQRRHQKEKSGIIPTSPTPYTYNKSCDLWSLGVIIYVMLCGYPP
FYSKHHSRTIPKDMRRKIMTGSFEFPEEEWSQISEMAKDVVRKLLKVKPEERLTIEGVLD
HPWLNSTEALDNVLPSAQLMMDKAVVAGIQQAHAEQLANMRIQDLKVSLKPLHSVNNPIL
RKRKLLGTKPKDSVYIHDHENGAEDSNVALEKLRDVIAQCILPQAGKGENEDEKLNEVMQ
EAWKYNRECKLLRDTLQSFSWNGRGFTDKVDRLKLAEIVKQVIEEQTTSHESQ
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BDBM50365791 |
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n/a |
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Name | BDBM50365791 |
Synonyms: | CHEMBL1956570 |
Type | Small organic molecule |
Emp. Form. | C21H20N6O2S |
Mol. Mass. | 420.487 |
SMILES | NC(=O)c1ccc(s1)-c1cnc(Nc2ccc(cc2)N2CCOCC2)c2nccn12 |
Structure |
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