Reaction Details Report a problem with these data
Target
MAP kinase-activated protein kinase 5
Ligand
BDBM50365800
Substrate
n/a
Meas. Tech.
ChEMBL_806118 (CHEMBL1960721)
IC50
2608±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 
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:
Homo sapiens (Human)
Description:
Recombinant MAPKAPK5 was phosphorylated by incubation with active p38alpha before assays.
Residue:
473
Sequence:
MSEESDMDKAIKETSILEEYSINWTQKLGAGISGPVRVCVKKSTQERFALKILLDRPKARNEVRLHMMCATHPNIVQIIEVFANSVQFPHESSPRARLLIVMEMMEGGELFHRISQHRHFTEKQASQVTKQIALALRHCHLLNIAHRDLKPENLLFKDNSLDAPVKLCDFGFAKIDQGDLMTPQFTPYYVAPQVLEAQRRHQKEKSGIIPTSPTPYTYNKSCDLWSLGVIIYVMLCGYPPFYSKHHSRTIPKDMRRKIMTGSFEFPEEEWSQISEMAKDVVRKLLKVKPEERLTIEGVLDHPWLNSTEALDNVLPSAQLMMDKAVVAGIQQAHAEQLANMRIQDLKVSLKPLHSVNNPILRKRKLLGTKPKDSVYIHDHENGAEDSNVALEKLRDVIAQCILPQAGKGENEDEKLNEVMQEAWKYNRECKLLRDTLQSFSWNGRGFTDKVDRLKLAEIVKQVIEEQTTSHESQ
  
Inhibitor
Name:
BDBM50365800
Synonyms:
CHEMBL1956687
Type:
Small organic molecule
Emp. Form.:
C18H18N8O
Mol. Mass.:
362.3885
SMILES:
C1CN(CCO1)c1ccc(Nc2ncc(-c3cn[nH]c3)n3ncnc23)cc1
Structure:
Search PDB for entries with ligand similarity: