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TargetMAP kinase-activated protein kinase 5
LigandBDBM50031747
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1432592 (CHEMBL3388151)
IC50>10000±n/a nM
Citation Menet, CJFletcher, SRVan Lommen, GGeney, RBlanc, JSmits, KJouannigot, NDeprez, Pvan der Aar, EMClement-Lacroix, PLepescheux, LGalien, RVayssiere, BNelles, LChristophe, TBrys, RUhring, MCiesielski, FVan Rompaey, L Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. J Med Chem57:9323-42 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
MAP kinase-activated protein kinase 5
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:
MSEESDMDKAIKETSILEEYSINWTQKLGAGISGPVRVCVKKSTQERFALKILLDRPKAR
NEVRLHMMCATHPNIVQIIEVFANSVQFPHESSPRARLLIVMEMMEGGELFHRISQHRHF
TEKQASQVTKQIALALRHCHLLNIAHRDLKPENLLFKDNSLDAPVKLCDFGFAKIDQGDL
MTPQFTPYYVAPQVLEAQRRHQKEKSGIIPTSPTPYTYNKSCDLWSLGVIIYVMLCGYPP
FYSKHHSRTIPKDMRRKIMTGSFEFPEEEWSQISEMAKDVVRKLLKVKPEERLTIEGVLD
HPWLNSTEALDNVLPSAQLMMDKAVVAGIQQAHAEQLANMRIQDLKVSLKPLHSVNNPIL
RKRKLLGTKPKDSVYIHDHENGAEDSNVALEKLRDVIAQCILPQAGKGENEDEKLNEVMQ
EAWKYNRECKLLRDTLQSFSWNGRGFTDKVDRLKLAEIVKQVIEEQTTSHESQ
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50031747
n/a
NameBDBM50031747
Synonyms:CHEMBL3360318
TypeSmall organic molecule
Emp. Form.C17H16N4O2
Mol. Mass.308.3345
SMILESCOc1ccc(cc1)-c1cccc2nc(NC(=O)C3CC3)nn12
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: