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TargetMAP kinase-activated protein kinase 5
LigandBDBM50363167
Substrate/Competitorn/a
Meas. Tech.ChEMBL_801403 (CHEMBL1948133)
IC50 1700±n/a nM
Citation Huber, KBrault, LFedorov, OGasser, CFilippakopoulos, PBullock, ANFabbro, DTrappe, JSchwaller, JKnapp, SBracher, F 7,8-dichloro-1-oxo-ß-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. J Med Chem55:403-13 (2012) [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
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  Blast E-value cutoff:
BDBM50363167
n/a
NameBDBM50363167
Synonyms:CHEMBL1945559
TypeSmall organic molecule
Emp. Form.C17H16Cl2N4O
Mol. Mass.363.241
SMILESCn1c2c(C(C#N)C3(CCNCC3)NC2=O)c2ccc(Cl)c(Cl)c12
Structure
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