Target
MAP kinase-activated protein kinase 2 [41-364]
Ligand
BDBM30266
Substrate
Biotinylated GST-LSP1
Meas. Tech.
Dissociation-Enhanced Lanthanide Fluorescent Immunoassay (DELFIA)
IC50
35±n/a nM
Citation
 Wu, JPWang, JAbeywardane, AAndersen, DEmmanuel, MGautschi, EGoldberg, DRKashem, MALukas, SMao, WMartin, LMorwick, TMoss, NPargellis, CPatel, URPatnaude, LPeet, GWSkow, DSnow, RJWard, YWerneburg, BWhite, A The discovery of carboline analogs as potent MAPKAP-K2 inhibitors. Bioorg Med Chem Lett 17:4664-9 (2007) [PubMed]  Article 
Target
Name:
MAP kinase-activated protein kinase 2 [41-364]
Synonyms:
MAPK-Activated Protein Kinase 2 (MK2) | MAPK2_HUMAN | MAPKAP kinase 2 | MAPKAPK-2 | MAPKAPK2
Type:
Serine/threonine-protein kinase
Mol. Mass.:
37477.48
Organism:
Homo sapiens (Human)
Description:
MK2 was activated with p38alpha MAPK and re-purified by GSH affinity chromatography.
Residue:
324
Sequence:
QQFPQFHVKSGLQIKKNAIIDDYKVTSQVLGLGINGKVLQIFNKRTQEKFALKMLQDCPKARREVELHWRASQCPHIVRIVDVYENLYAGRKCLLIVMECLDGGELFSRIQDRGDQAFTEREASEIMKSIGEAIQYLHSINIAHRDVKPENLLYTSKRPNAILKLTDFGFAKETTSHNSLTTPCYTPYYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGYPPFYSNHGLAISPGMKTRIRMGQYEFPNPEWSEVSEEVKMLIRNLLKTEPTQRMTITEFMNHPWIMQSTKVPQTPLHTSRVLKEDKERWEDVKEEMTSALATMR
  
Inhibitor
Name:
BDBM30266
Synonyms:
carboline analog, 78
Type:
Small organic molecule
Emp. Form.:
C22H26N6O3S
Mol. Mass.:
454.545
SMILES:
CC1CNC(=O)c2[nH]c3ccc(cc3c12)C(=O)Nc1nc(cs1)C(=O)NCCCN(C)C
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated GST-LSP1
Synonyms:
lymphocyte-specific protein 1
Type:
Other Protein Type
Mol. Mass.:
17410.08
Organism:
n/a
Description:
The GST-LSP1 179-339 substrate of MK2 was biotinylated with a 70-fold molar excess of PEO-iodoacetyl biotin (Pierce), followed by quenching with excess DTT and purification by Sephadex G-25 gel filtration.
Residue:
161
Sequence:
LVLEGTIEQSSPPLSPTTKLIDRTESLNRSIEKSNSVKKSQPDLPISKIDQWLEQYTQAIETAGRTPKLARQASIELPSMAVASTKSRWETGEVQAQSAAKTPSCKDIVAGDMSKKSLWEQKGGSKTSSTIKSTPSGKRYKFVATGHGKYEKVLVEGGPAP