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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 (CEREP panel (binding assay, receptors and ion channels)) EUB0001623a DRD2
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated 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 CDK8 in human SW620 cells assessed as reduction in STAT1 phosphorylation at Ser727 residue at 5 to 30 uM after 24 hrs by Western blot analysis
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of GSK-3alpha (unknown origin)
In vivo inhibition of CDK8-mediated STAT1 phosphorylation at Ser727 in human SW620 cells xenografted in NCr athymic mouse at 50 mg/kg, po bid administered for 16 days measured 2 to 24 hrs post last dose by immunoassay
SummaryCompounds, ActivePubMed Citation
In vivo inhibition of CDK8-mediated STAT1 phosphorylation at Ser727 in human SW620 cells xenografted in NCr athymic mouse at 100 mg/kg, po qd administered for 16 days measured 2 to 24 hrs post last dose by immunoassay
Displacement of [3H]BTCP from human recombinant dopamine transporter expressed in CHO cells after 120 mins by scintillation counting method
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
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