Reaction Details Report a problem with these data
Target
MAP kinase-activated protein kinase 5
Ligand
BDBM175242
Substrate
n/a
Meas. Tech.
IMAP Assay
pH
7.5±n/a
IC50
8.1e+3±n/a nM
Comments
extracted
Citation
 Hockerman, SL; Monahan, JB; Selness, SR Methyl/fluoro-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds and fluoro-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds US Patent  US9115089 Publication Date 8/25/2015 
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:
BDBM175242
Synonyms:
US11844801, Compound (M)-I | US9115089, 49
Type:
Small organic molecule
Emp. Form.:
C25H22ClF2N5O3
Mol. Mass.:
513.924
SMILES:
Cc1cnc(cc1-n1c(C)cc(OCc2ncc(F)cc2F)c(Cl)c1=O)-c1ccnc(n1)C(C)(C)O |(3.33,-1.54,;2,-2.31,;2,-3.85,;.67,-4.62,;-.67,-3.85,;-.67,-2.31,;.67,-1.54,;.67,,;2,.77,;3.33,,;2,2.31,;.67,3.08,;.67,4.62,;2,5.39,;3.33,4.62,;3.33,3.08,;4.67,2.31,;6,3.08,;7.34,2.31,;6,4.62,;4.67,5.39,;4.67,6.93,;-.67,2.31,;-2,3.08,;-.67,.77,;-2,,;-2,-4.62,;-2,-6.16,;-3.33,-6.93,;-4.67,-6.16,;-4.67,-4.62,;-3.33,-3.85,;-6,-3.85,;-6.77,-2.52,;-5.23,-2.52,;-7.34,-4.62,)|
Structure:
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