ERK inhibitor II [Ligand Id: 5966] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL259551 (FR-180204)
  • mitogen-activated protein kinase 3/MAP kinase ERK1 in Human [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361]
GtoPdb - - 6.39 pKi 410 nM Ki Biochem Biophys Res Commun (2005) 336: 357-63 [PMID:16139248]
ChEMBL Inhibition of ERK1 B 6.51 pKi 310 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Binding affinity to ERK1 B 6.51 pKi 310 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
ChEMBL Binding affinity to ERK2 (unknown origin) by isothermal titration calorimetry B 6.07 pKd 850 nM Kd J. Med. Chem. (2013) 56: 2155-2159 [PMID:23419007]
ChEMBL Inhibition of ERK2 B 6.51 pKi 310 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Binding affinity to ERK2 B 6.51 pKi 310 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
GtoPdb - - 6.85 pKi 140 nM Ki Biochem Biophys Res Commun (2005) 336: 357-63 [PMID:16139248]
ChEMBL Inhibitory activity against human ERK2 B 5.72 pIC50 1900 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 55-58 [PMID:16242327]
ChEMBL Inhibition of phosphorylated ERK2 (unknown origin) using myelin basic protein as substrate after 2 hrs in presence of ATP by ADP-glo assay B 5.92 pIC50 1200 nM IC50 ACS Med Chem Lett (2017) 8: 726-731 [PMID:28740606]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of p38alpha B 6.51 pKi 310 nM Ki Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]

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]