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Selectivity interaction (Kinase panel (literature)) EUB0001623a GSK3A
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (Reporter displacement assay) EUB0001623a CDK9
Selectivity interaction (Reporter displacement assay) EUB0001623a CDK8
Affinity Biochemical interaction: (FRET-based Lanthascreen binding competition assay) EUB0001623a CDK8
Affinity On-target Cellular interaction: (7dF3 WNT-specific reporter gene assay) EUB0001623a CDK8
Affinity Phenotypic Cellular interaction: (Reporter-based luciferase assay (in PA-1 cell line bearing activating WNT-pathway mutations)) EUB0001623a CDK8
Affinity Phenotypic Cellular interaction: (Reporter-based luciferase assay (in COLO205 (APC mutant) bearing activating WNT-pathway mutations)) EUB0001623a CDK8
Affinity Phenotypic Cellular interaction: (Western Blot assay (inhibition of STAT1 phosphorylation at Ser727 in SW620 cells)) EUB0001623a CDK8
Inhibition of human CDK8 in human Jurkat cells assessed as inhibition of STAT1 phosphorylation at S727 residue measured after 24 hrs by Western blot assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Primary qHTS for inhibitors of nuclear receptor binding SET domain protein 2 (NSD2) in an RCH-ACV wild type WT cells (2C)
Assay data:2970 Active, 9 Activity ≤ 1 nM, 1016 Activity ≤ 1 µM, 10037 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of GSK-3alpha (unknown origin)
Binding affinity to human CDK19 (1 to 502 residues)/cyclin C (1 to 283 residues) by reporter displacement assay
Binding affinity to human CDK8 (1 to 464 residues)/cyclin C (1 to 283 residues) by reporter displacement assay
Inhibition of CDK8 in human PA1 cells assessed as suppression of WNT3a ligand-induced WNT pathway by luciferase reporter gene assay
Inhibition of CDK8 in human COLO205 cells expressing APC mutant assessed as suppression of WNT pathway by luciferase reporter gene assay
Inhibition of CDK8 in human LS174T cells expressing beta-catenin mutant assessed as suppression of WNT pathway by luciferase reporter gene assay
Inhibition of CDK8 in human SW620 cells assessed as decrease in STAT1 phosphorylation at Ser727
Inhibition of CDK8 in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24 hrs by luciferase reporter gene assay
Assay data:23 Active, 1 Activity ≤ 1 nM, 20 Activity ≤ 1 µM, 24 Tested
Inhibition of Alexa647 tracer binding to full length recombinant human His-tagged CDK8/cyclin C expressed in Baculovirus expression system preincubated for 20 mins followed by tracer addition and incubated in dark for 60 mins by FRET-based Lanthascreen assay
Assay data:24 Active, 23 Activity ≤ 1 µM, 24 Tested
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