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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]