MK2a inhibitor [Ligand Id: 6009] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL235658
  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Mouse [ChEMBL: CHEMBL2336] [GtoPdb: 1499] [UniProtKB: P47811]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
GtoPdb - - 6.48 pKi 330 nM Ki Bioorg Med Chem Lett (2007) 17: 6832-5 [PMID:17964780]
ChEMBL Inhibition of MK2 in human TERT immortalised HCA2 cells assessed as inhibition of anisomycin-induced HSP27 phosphorylation at 2.5 uM by ELISA B 6.48 pKi 330 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6832-6835 [PMID:17964780]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2336] [GtoPdb: 1499] [UniProtKB: P47811]
ChEMBL Inhibition of mouse N-terminal 5His-tagged p38alpha assessed as decrease in 6His-tagged MK2a (51 to 400 residues) phosphorylation in presence of [gamma-33P]-ATP by scintillation counting method B 6.48 pIC50 330 nM IC50 Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]