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Target
MAP kinase-activated protein kinase 5
Ligand
BDBM50499634
Substrate
n/a
Meas. Tech.
ChEMBL_1542785 (CHEMBL3742675)
IC50
>10000±n/a nM
Citation
 Hobson, AD; Harris, CM; van der Kam, EL; Turner, SC; Abibi, A; Aguirre, AL; Bousquet, P; Kebede, T; Konopacki, DB; Gintant, G; Kim, Y; Larson, K; Maull, JW; Moore, NS; Shi, D; Shrestha, A; Tang, X; Zhang, P; Sarris, KK Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders. J Med Chem 58:9154-70 (2015) [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:
BDBM50499634
Synonyms:
CHEMBL3741589
Type:
Small organic molecule
Emp. Form.:
C18H17Cl2NO3
Mol. Mass.:
366.238
SMILES:
OC(=O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C1
Structure:
Search PDB for entries with ligand similarity: