Target
MAP kinase-activated protein kinase 2
Ligand
BDBM50434494
Substrate
n/a
Meas. Tech.
ChEMBL_961826 (CHEMBL2389966)
IC50
4.9±n/a nM
Citation
 Xiao, DPalani, AHuang, XSofolarides, MZhou, WChen, XAslanian, RGuo, ZFossetta, JTian, FTrivedi, PSpacciapoli, PWhitehurst, CELundell, D Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors. Bioorg Med Chem Lett 23:3262-6 (2013) [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:
BDBM50434494
Synonyms:
CHEMBL2385542
Type:
Small organic molecule
Emp. Form.:
C36H31N5O3
Mol. Mass.:
581.663
SMILES:
COc1cncc(c1)-c1ccccc1CN1c2ccc(cc2Cc2cc(oc2C1=O)-c1ccc(cc1)C#N)N1CCNCC1
Structure:
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