Target
MAP kinase-activated protein kinase 5
Ligand
BDBM50365786
Substrate
n/a
Meas. Tech.
ChEMBL_806119 (CHEMBL1960722)
IC50
>10000±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 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:
BDBM50365786
Synonyms:
CHEMBL1956565
Type:
Small organic molecule
Emp. Form.:
C22H22N6O3S
Mol. Mass.:
450.513
SMILES:
NS(=O)(=O)c1ccc(cc1)-c1cnc(Nc2ccc(cc2)N2CCOCC2)c2nccn12
Structure:
Search PDB for entries with ligand similarity: