Reaction Details Report a problem with these data
Target
MAP kinase-activated protein kinase 2 [41-364]
Ligand
BDBM30211
Substrate
Biotinylated GST-LSP1
Meas. Tech.
Dissociation-Enhanced Lanthanide Fluorescent Immunoassay (DELFIA)
pH
7.6±n/a
Temperature
298.15±n/a K
IC50
>40000±n/a nM
Citation
Wu, JP; Wang, J; Abeywardane, A; Andersen, D; Emmanuel, M; Gautschi, E; Goldberg, DR; Kashem, MA; Lukas, S; Mao, W; Martin, L; Morwick, T; Moss, N; Pargellis, C; Patel, UR; Patnaude, L; Peet, GW; Skow, D; Snow, RJ; Ward, Y; Werneburg, B; White, 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:
BDBM30211
Synonyms:
carboline analog, 24
Type:
Small organic molecule
Emp. Form.:
C12H12N2O2
Mol. Mass.:
216.2359
SMILES:
CC1CNC(=O)c2[nH]c3ccc(O)cc3c12
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