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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  • mitogen-activated protein kinase 6/Mitogen-activated protein kinase 6 in Human [ChEMBL: CHEMBL5121] [GtoPdb: 2092] [UniProtKB: Q16659]
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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]
mitogen-activated protein kinase 6/Mitogen-activated protein kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5121] [GtoPdb: 2092] [UniProtKB: Q16659]
ChEMBL Binding affinity to LPP-dephosphorylated recombinant wild-type ERK3 (9 to 327 residues) (unknown origin) expressed in Escherichia coli by microscale thermophoresis assay B 5 pKd >10000 nM Kd Bioorg Med Chem Lett (2020) 30: 127551-127551 [PMID:32927028]

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]