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Target
MAP kinase-activated protein kinase 5
Ligand
BDBM50365787
Substrate
n/a
Meas. Tech.
ChEMBL_806119 (CHEMBL1960722)
IC50
2390±n/a nM
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 Lett 22:2266-70 (2012) [PubMed] Article
More Info.:
Target
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:
Human
Description:
Recombinant MAPKAPK5 was phosphorylated by incubation with active p38alpha before assays.
Residue:
473
Sequence:
MSEESDMDKAIKETSILEEYSINWTQKLGAGISGPVRVCVKKSTQERFALKILLDRPKARNEVRLHMMCATHPNIVQIIEVFANSVQFPHESSPRARLLIVMEMMEGGELFHRISQHRHFTEKQASQVTKQIALALRHCHLLNIAHRDLKPENLLFKDNSLDAPVKLCDFGFAKIDQGDLMTPQFTPYYVAPQVLEAQRRHQKEKSGIIPTSPTPYTYNKSCDLWSLGVIIYVMLCGYPPFYSKHHSRTIPKDMRRKIMTGSFEFPEEEWSQISEMAKDVVRKLLKVKPEERLTIEGVLDHPWLNSTEALDNVLPSAQLMMDKAVVAGIQQAHAEQLANMRIQDLKVSLKPLHSVNNPILRKRKLLGTKPKDSVYIHDHENGAEDSNVALEKLRDVIAQCILPQAGKGENEDEKLNEVMQEAWKYNRECKLLRDTLQSFSWNGRGFTDKVDRLKLAEIVKQVIEEQTTSHESQ