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

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ChEMBL ligand: CHEMBL257167
  • 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
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]

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]