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Target
MAP kinase-activated protein kinase 5
Ligand
BDBM50330262
Substrate
n/a
Meas. Tech.
ChEMBL_676347 (CHEMBL1273648)
IC50
>10000±n/a nM
Citation
 Cho, YS; Borland, M; Brain, C; Chen, CH; Cheng, H; Chopra, R; Chung, K; Groarke, J; He, G; Hou, Y; Kim, S; Kovats, S; Lu, Y; O'Reilly, M; Shen, J; Smith, T; Trakshel, G; Vögtle, M; Xu, M; Xu, M; Sung, MJ 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6. J Med Chem 53:7938-57 (2010) [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:
BDBM50330262
Synonyms:
CHEMBL1272171 | N*6'*-[4-(5-Isopropyl-3-trifluoromethyl-1H-pyrazol-4-yl)-pyrimidin-2-yl]-N*4*,N*4*-dimethyl-3,4,5,6-tetrahydro-2H-[1,3']-bipyridinyl-4,6'-diamine
Type:
Small organic molecule
Emp. Form.:
C23H29F3N8
Mol. Mass.:
474.5252
SMILES:
CC(C)c1[nH]nc(c1-c1ccnc(Nc2ccc(cn2)N2CCC(CC2)N(C)C)n1)C(F)(F)F
Structure:
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