Target
MAP kinase-activated protein kinase 5
Ligand
BDBM50215481
Substrate
n/a
Meas. Tech.
ChEMBL_456530 (CHEMBL922896)
IC50
24000±n/a nM
Citation
 Trujillo, JIMeyers, MJAnderson, DRHegde, SMahoney, MWVernier, WFBuchler, IPWu, KKYang, SYang, SHartmann, SJReitz, DB Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg Med Chem Lett 17:4657-63 (2007) [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:
BDBM50215481
Synonyms:
5-methoxy-9,12-diazatetracyclo[10.2.1.0^{2,10}.0^{3,8}]pentadeca-2(10),3,5,7-tetraene-11-carboxylic acid | CHEMBL392876
Type:
Small organic molecule
Emp. Form.:
C15H16N2O3
Mol. Mass.:
272.2991
SMILES:
COc1ccc2[nH]c3C(N4CCC(C4)c3c2c1)C(O)=O |w:12.12,8.20,TEB:17:8:13:11.10|
Structure:
Search PDB for entries with ligand similarity: