Reaction Details
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MAP kinase-activated protein kinase 2 [41-364]
Ligand
BDBM30301
Substrate
Biotinylated GST-LSP1
Meas. Tech.
Dissociation-Enhanced Lanthanide Fluorescent Immunoassay (DELFIA)
IC50
320±n/a nM
Citation
Xiong, Z; Gao, DA; Cogan, DA; Goldberg, DR; Hao, MH; Moss, N; Pack, E; Pargellis, C; Skow, D; Trieselmann, T; Werneburg, B; White, A Synthesis and SAR studies of indole-based MK2 inhibitors. Bioorg Med Chem Lett 18:1994-9 (2008) [PubMed] Article More Info.:
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:
BDBM30301
Synonyms:
indole-based 7-membered lactam, 25d
Type:
Small organic molecule
Emp. Form.:
C19H18N4O2
Mol. Mass.:
334.3718
SMILES:
CC1CNC(=O)c2cc3ccc(cc3n2C1)C(=O)Nc1cccnc1
Structure:
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