Target
MAP kinase-activated protein kinase 5
Ligand
BDBM30185
Substrate
HSP27 Peptide
Meas. Tech.
Kinase Selectivity Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
81±n/a nM
Citation
 Anderson, DRMeyers, MJVernier, WFMahoney, MWKurumbail, RGCaspers, NPoda, GISchindler, JFReitz, DBMourey, RJ Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem 50:2647-54 (2007) [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:
BDBM30185
Synonyms:
CHEMBL226403 | Pyrrolopyridine, 16
Type:
Small organic molecule
Emp. Form.:
C21H16N4O
Mol. Mass.:
340.3779
SMILES:
O=C1NCCc2[nH]c(cc12)-c1ccnc(c1)-c1cnc2ccccc2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
HSP27 Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1389.69
Organism:
n/a
Description:
n/a
Residue:
13
Sequence:
KKKALSRNLSVAA