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TargetMAP kinase-activated protein kinase 5
LigandBDBM50365798
Substrate/Competitorn/a
Meas. Tech.ChEMBL_806118 (CHEMBL1960721)
IC50 702±n/a nM
Citation Andrews, MJClase, JABar, GTricarico, GEdwards, PJBrys, RChambers, MSchmidt, WMacLeod, AHirst, KAllen, VBirault, VLe, JHarris, JSelf, ANash, KDixon, 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
More Info.:Get all data from this article,  Assay Method
 
MAP kinase-activated protein kinase 5
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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  Blast E-value cutoff:
BDBM50365798
n/a
NameBDBM50365798
Synonyms:CHEMBL1956685
TypeSmall organic molecule
Emp. Form.C21H20N6O3
Mol. Mass.404.4219
SMILESNC(=O)c1cc(co1)-c1cnc(Nc2ccc(cc2)N2CCOCC2)c2nccn12
Structure
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