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Target
MAP kinase-activated protein kinase 2
Ligand
BDBM30324
Substrate
Hsp27 Substrate Peptide
Meas. Tech.
MK2 Enzyme Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
82±n/a nM
Citation
 Schlapbach, A; Feifel, R; Hawtin, S; Heng, R; Koch, G; Moebitz, H; Revesz, L; Scheufler, C; Velcicky, J; Waelchli, R; Huppertz, C Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity. Bioorg Med Chem Lett 18:6142-6 (2008) [PubMed]  Article 
Target
Name:
MAP kinase-activated protein kinase 2
Synonyms:
MAP kinase-activated protein kinase 2 (MAPKAPK2) | MAP kinase-activated protein kinase 2 (MK2) | MAP kinase-activated protein kinase 2 (p38/MK2) | MAPK-Activated Protein Kinase 2 (MK2) | MAPK-activated protein kinase 2 | MAPK2_HUMAN | MAPKAP kinase 2 | MAPKAPK-2 | MAPKAPK2 | MK2
Type:
Serine/threonine-protein kinase
Mol. Mass.:
45579.87
Organism:
Homo sapiens (Human)
Description:
P49137
Residue:
400
Sequence:
MLSNSQGQSPPVPFPAPAPPPQPPTPALPHPPAQPPPPPPQQFPQFHVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSHNSLTTPCYTPYYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGYPPFYSNHGLAISPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKEDKERWEDVKEEMTSALATMRVDYEQIKIKKIEDASNPLLLKRRKKARALEAAALAH
  
Inhibitor
Name:
BDBM30324
Synonyms:
Pyrrolo-pyrimidone, 17
Type:
Small organic molecule
Emp. Form.:
C23H23N5O2
Mol. Mass.:
401.461
SMILES:
CN(C)CCOc1ccc(C=Cc2cc(ccn2)-c2cc3c(nc[nH]c3=O)[nH]2)cc1 |w:10.9|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Hsp27 Substrate Peptide
Synonyms:
n/a
Type:
Biotinylated peptide
Mol. Mass.:
2940.84
Organism:
n/a
Description:
n/a
Residue:
26
Sequence:
ITINYLAYSRALSRQLSSGVSEIRCH