IKK-2 inhibitor IV [Ligand Id: 5986] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL257167
  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate B 5.71 pIC50 1967 nM IC50 HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa B kinase beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920]
ChEMBL Inhibition of IKK-beta B 7.7 pIC50 19.95 nM IC50 Bioorg Med Chem Lett (2011) 21: 2255-2258 [PMID:21429745]
ChEMBL Inhibition of IKK-beta B 7.71 pIC50 19.5 nM IC50 J Med Chem (2008) 51: 7898-7914 [PMID:19035792]
ChEMBL Inhibition of IKK beta at 300 uM by K-ELISA B 7.74 pIC50 18 nM IC50 J Nat Prod (2008) 71: 106-111 [PMID:18088098]
ChEMBL Inhibition of IKK-beta by TR-FRET assay B 7.74 pIC50 18 nM IC50 Bioorg Med Chem (2009) 17: 2759-2766 [PMID:19285872]
GtoPdb FRET measurement using recombinant human IKK2 (residues 1-756) - 7.75 pIC50 17.9 nM IC50 J Pharmacol Exp Ther (2005) 312: 373-81 [PMID:15316093]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 6.6 pIC50 250 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Binding affinity to human JAK2 B 7.66 pKd 22 nM Kd J Med Chem (2008) 51: 7898-7914 [PMID:19035792]
ChEMBL Inhibition of JAK2 B 8.3 pKi 5 nM Ki J Med Chem (2008) 51: 7898-7914 [PMID:19035792]
Venus kinase receptor 2 in Schistosoma mansoni (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5169215] [UniProtKB: D5JEH1]
ChEMBL Binding affinity to Schistosoma mansoni N-terminal His6-tagged full-length VKR2 kinase domain expressed in baculovirus infected Sf9 insect cells in presence of ATPgammaS by SPR analysis B 4.8 pKd 16000 nM Kd ACS Med Chem Lett (2022) 13: 1715-1722 [PMID:36385939]

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]