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Summary
Inhibition of IKKa (unknown origin) at 1 uM relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Selectivity interaction (KinomeScan (DiscoverX)) EUB0000749a CHUK
SummaryRelated BioAssays by Target
Selectivity interaction (Enzymatic assay) EUB0000624a CHUK
Selectivity interaction (Kinase panel (enzymatic assay)) EUB0000153b CHUK
Inhibition of human full length recombinant IKKalpha assessed as residual activity at 1 uM using peptide as substrate incubated for 40 mins in presence of [gamma 33P]-ATP by radiometric scintillation counting assay relative to control
Inhibition of full length human recombinant IKKalpha expressed in baculovirus infected Sf9 cells at 1 uM incubated for 60 mins in presence of [gamma33P]ATP by microplate scintillation counter relative to control
Inhibition of IKKalpha/beta phosphorylation at Ser176/180 in LPS-induced mouse C8D1A cells at 0.75 to 3 uM pretreated for 4 hrs followed by LPS stimulation measured after 24 hrs by Western blotting analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
IKK-alpha DiscoveRx kinase panel
IKKalpha(h) Kinase panel
IKK?(h) Millipore kinase panel
Inhibition of IKKalpha (unknown origin) at 1 uM
Inhibition of TNFalpha-induced IkKalpha in human SUM149PT cells at 0.5 to 2 uM by ELISA assay
Inhibition of human recombinant IKKalpha assessed as reduction in substrate phosphorylation at 50 to 500 nM using ATP and Ulight-IkappaB-alpha as substrate incubated for 30 min by LANCE detection method
Biological Assay from US Patent US9981963: "3-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-c]pyridine derivatives as NIK inhibitors"
Assay data:29 Active, 29 Activity ≤ 1 µM, 29 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
IKK Kinase Inhibition Assay from Article 10.1021/jm9000117: "Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta)."
Assay data:25 Active, 12 Activity ≤ 1 µM, 26 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
IKK Enzymatic Activity Assay from Article 10.1021/jm8015816: "Novel tricyclic inhibitors of IkappaB kinase."
Assay data:29 Active, 27 Activity ≤ 1 µM, 29 Tested
IKK Kinase Inhibition Assay from Article 10.1016/j.bmcl.2007.04.088: "The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases."
Assay data:23 Active, 14 Activity ≤ 1 µM, 33 Tested
IKK Kinase Inhibition Assay from Article 10.1016/j.bmcl.2006.09.018: "5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase."
Assay data:14 Active, 6 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
IKK Inhibition Assay from Article 10.1016/j.bmcl.2007.05.031: "Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors."
Assay data:49 Active, 50 Activity ≤ 1 µM, 50 Tested
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