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Activation of VDR (unknown origin) at 10 uM
Assay data:1 Tested
SummaryRelated BioAssays by Target
Effect on VDR activity in GeneBLAzer VDR-UAS-bla HEK 293T cells by fluorescence based analysis
Assay data:2 Tested
Inhibition of VDR (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Agonist activity at VDR (unknown origin)
Agonist activity at Vitamin D receptor (unknown origin) by fluorescence polarization assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at VDR in human BE2C cells assessed as reduction in cyclin-D expression at 1 uM incubated for 24 hrs by western blot analysis relative to control
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at VDR in human BE2C cells assessed as reduction in MYCN expression at 1 uM incubated for 24 hrs by western blot analysis relative to control
Antagonist activity at VDR in human 2008 cells assessed as suppression of importin-4 expression at 250 nM incubated for 12 to 18 hrs by western blot analysis relative to control
Antagonist activity at VDR in human 2008 cells assessed as suppression of RXR-alpha expression at 250 nM incubated for 18 hrs by western blot analysis relative to control
Antagonist activity at VDR LBD (unknown origin) transfected in HEK-293T cells assessed as inhibition of 1,25(OH)2D3-induced receptor transactivation incubated for 16 hrs by Bright-Glo luciferase assay
Assay data:3 Tested
Agonist activity at VDR LBD (unknown origin) using Alexa Fluor 647-labeled SRC2-3 as substrate incubated for 2 hrs by fluorescence polarization assay
Antagonist activity at VDR LBD (unknown origin) using Alexa Fluor 647-labeled SRC2-3 as substrate incubated for 2 hrs in presence of calcitriol by fluorescence polarization assay
Assay data:1 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Displacement of fluorescent tracer from VDR (unknown origin) by fluorescence polarisation competition assay
Competitive binding affinity to His-tagged human VDR LBD (156 to 453 residues) expressed in Escherichia coli BL23 (DE3) cells at 0.1 to 100 nM in presence of 1,25D3 by fluorescent polarization assay relative to (1R,3S)-5-(2-((1R,3aS,7aR)-1-((R)-6-hydroxy-6-methylheptan-2-yl)-7a-methyloctahydro-4H-inden-4-ylidene)ethylidene)-4-methylenecyclohexane-1,3-diol
Competitive binding affinity to His-tagged human VDR LBD (156 to 453 residues) expressed in Escherichia coli BL23 (DE3) cells in presence of 1,25D3 by fluorescent polarization assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Partial agonist activity at GAL4-tagged human VDR LBD expressed in HEK293T cells at 3 uM incubated for 12 to 14 hrs by dual-Glo luciferase assay
Assay data:4 Active, 4 Tested
Antagonist activity at VDR in human HeLa cells assessed as reduction in CYP27B1 mRNA expression at 10 uM in presence of calcitriol measured after 4 hrs by western blot analysis
Antagonist activity at VDR in human HeLa cells assessed as decrease in mTOR phosphorylation at Ser2448 residue at 100 nM in presence or absence of calcitriol measured after 4 hrs by western blot analysis
Antagonist activity at VDR in human HeLa cells assessed as decrease in p62 expression at 100 nM in presence or absence of calcitriol measured after 4 hrs by western blot analysis
Assay data:1 Active, 1 Tested
Antagonist activity at VDR in human HeLa cells assessed as increase in ratio of LC3-II to LC-I at 100 nM in presence or absence of calcitriol measured after 4 hrs by western blot analysis
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