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Displacement of [3H]-1-alpha,25-(OH)2D3 from bovine thymus VDR incubated for 18 hrs by competitive binding assay
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human VDR
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 2 Tested
Agonist activity at human VDR expressed in HOS cells co-expressing human RXR by Dual-Glo luciferase reporter gene assay
Assay data:9 Active, 2 Activity ≤ 1 nM, 9 Activity ≤ 1 µM, 9 Tested
Transrepression of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-NCoR and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in NCoR recruitment by beta-galactosidase reporter gene based mammalian two-hybrid assay
Assay data:3 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Transactivation of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-SRC-1 and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in SRC-1 recruitment by beta-galactosidase reporter gene based mammalian two-hybrid assay
Assay data:1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Transactivation of VP16-tagged VDR (unknown origin) expressed in HEK293 cells harboring pCMX-GAL4-RXRalpha and MH100(UAS) X 4tk-LUC reporter plasmid assessed as increase in interaction with RXRalpha by beta-galactosidase reporter gene based mammalian two-hybrid assay
Assay data:2 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Displacement of [3H]-1,25D3 from C-terminal GST-tagged human recombinant VDR LBD expressed in Escherichia coli BL21 (DE3) after 16 hrs by radioligand binding assay
Assay data:5 Active, 1 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 5 Tested
Displacement of [3H]-1,25-(OH)2D3 from N-terminal GST-tagged human recombinant vitamin D receptor ligand binding domain expressed in Escherichia coli BL21 (DE3) pLys S after 16 hrs
Assay data:9 Active, 1 Activity ≤ 1 nM, 9 Activity ≤ 1 µM, 9 Tested
Agonist activity at GAL4 DNA-binding domain fused VDR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay
Agonist activity at VDR expressed in human HuH7 cells after 24 hrs by pDR3-luciferase reporter gene assay
Assay data:3 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 4 Tested
Growth inhibition of human SK-MEL-188 cells measured after 48 hrs by MTS/PMS assay
Assay data:5 Active, 5 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Transactivation of VDR in rat osteosarcoma cells assessed as 24-hydroxylase transcriptional activity by luciferase reporter gene assay
Assay data:6 Active, 6 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
Displacement of [3H]1alpha,25-(OH)2D3 from full-length recombinant rat VDR by scintillation counter
Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with NCoR assessed as decrease in NCoR recruitment by two-hybrid assay
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Agonist activity at VDR (unknown origin) expressed in HEK293 cells cotransfected with RXRalpha assessed as RXRalpha recruitment by two-hybrid assay
Assay data:4 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 4 Tested
Agonist activity at VDR in human HEK293 cells assessed as transcriptional activity after 16 to 24 hrs by luciferase reporter gene assay
Displacement of [3H]-1,25(OH)2D3 from recombinant human VDR ligand binding domain
Displacement of [3H]-1alpha,25-dihydroxyvitamin D3 from recombinant human VDR LBD expressed in Escherichia coli BL21 (DE3) pLysS after 16 hrs
Assay data:5 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 5 Tested
BK Channel Variant Modulator Selectivity Assay
Assay data:286 Active, 904 Activity ≤ 1 nM, 951 Activity ≤ 1 µM, 951 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Displacement of [3H]-1alpha25-(OH)2D3 from full length recombinant rat vitamin D receptor by scintillation counting analysis
Assay data:4 Active, 2 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 7 Tested
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