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Dual reporter qHTS for antagonist of Pregnane X Receptor (hPXR) against the NCATS DSHEA and TCM libraries: Fluorescence Readout
Assay data:28 Active, 4 Activity ≤ 1 µM, 964 Tested
SummaryPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Dual reporter qHTS for antagonist of Pregnane X Receptor (hPXR) against the NCATS DSHEA and TCM libraries: Luminescence Readout
Assay data:11 Active, 8 Activity ≤ 1 µM, 964 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Dual reporter qHTS for agonist of Pregnane X Receptor (hPXR) against the NCATS DSHEA and TCM libraries: Luminescence readout
Assay data:82 Active, 964 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Dual reporter qHTS for agonist of Pregnane X Receptor (hPXR) against the NCATS DSHEA and TCM libraries: Fluorescence readout
Assay data:1 Active, 3 Activity ≤ 1 µM, 964 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Agonist activity at human PXR transfected in human LS180 cells cotransfected with luciferase reporter plasmid p2A4-Luc assessed as transcriptional activity incubated for 24 hrs by luciferase reporter assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Displacement of fluorescence labeled ligand from human PXR ligand binding domain by Lanthascreen TR-FRET assay
Transactivation of human PXR transfected in HepG2 cells assessed as CYP450 induction by measuring fold activation at 10 uM by luciferase reporter gene assay
Assay data:13 Tested
Agonist activity at PXR (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Transactivation of Gal4-tagged human PXR transfected in human HeLa cells preincubated for 16 hrs followed by luciferin addition and measured after 10 mins by luminescence method
Assay data:6 Active, 2 Activity ≤ 1 µM, 13 Tested
Binding affinity to human PXR-LBD assessed as change in melting temperature at 100 uM incubated for 30 mins by thermal shift assay
Assay data:8 Tested
Activation of PXR (unknown origin) at 10 uM
Induction of PXR degradation in PXR knock in human SNU-C4 cells at 0.0001 to 1 uM measured after 24 hrs by Western blot analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Induction of PXR degradation in PXR knock in human SNU-C4 cells at 5 uM measured after 12 hrs by Western blot analysis relative to control
Displacement of BODIPY FL vindoline from recombinant human GST-tagged PXR LBD (111 to 434 residues) expressed in baculovirus infected insect cells by TR-FRET assay
Induction of PXR degradation in PXR knock in human SNU-C4 cells at 10 uM measured after 2 to 48 hrs by Western blot analysis
Induction of PXR degradation in PXR knock in human SNU-C4 cells at 10 uM measured after 24 hrs in presence of proteasome inhibitor MG-132 by Western blot analysis
Induction of PXR degradation in PXR knock in human SNU-C4 cells measured after 24 hrs by Western blot analysis
Assay data:2 Tested
Transactivation of PXR (unknown origin) relative to refampicin
Assay data:3 Active, 18 Tested
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