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ALPHA Screen Assay with TLX LBD from US Patent US20240067625: "SMALL-MOLECULE MODULATORS OF THE ORPHAN NUCLEAR RECEPTOR TLX"
Assay data:43 Active, 41 Activity ≤ 1 nM, 41 Activity ≤ 1 µM, 43 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inverse agonist activity at TLX (unknown origin) assessed as fold activation
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inverse agonist activity at TLX (unknown origin)
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of tlx (unknown origin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at human full length Gal4-fused TLX transfected in human HEK293T cells coexpressing pFR-TAE-Luc assessed as repressor activity of receptor by measuring decrease in reporter activity at 0.03 to 30 uM by dual-glo luciferase assay
Assay data:1 Tested
Agonist activity at human full length Gal4-fused TLX transfected in human HEK293T cells coexpressing pFR-TAE-Luc assessed as repressor activity of receptor by measuring decrease in reporter activity at 0.1 to 30 uM by dual-glo luciferase assay
Agonist activity at human Gal4-fused TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP16 assessed as repressor activity of receptor by measuring decrease in reporter activity at 0.03 to 30 uM measured after 14 hrs by Dual-Glo Luciferase assay
Agonist activity at human Gal4-fused TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP16 assessed as repressor activity of receptor by measuring decrease in reporter activity at 0.1 to 30 uM measured after 14 hrs by Dual-Glo Luciferase assay
Agonist activity at TLX in human T98G cells assessed as upregulation of SIRT1 mRNA expression at 30 uM measured after 8 hrs by qRT-PCR analysis
Destabilization of recombinant TLX LBD (unknown origin) assessed as change in entropy at 100 uM by isothermal titration calorimetry
Agonist activity at human Gal4-fused TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP16 assessed as repressor activity of receptor by measuring decrease in reporter activity at 30 uM measured after 14 hrs by Dual-Glo Luciferase assay
Agonist activity at TLX in human T98G cells assessed as upregulation of SIRT1 mRNA expression at 3 uM measured after 8 hrs by qRT-PCR analysis
Agonist activity at TLX in human T98G cells assessed as upregulation of SIRT1 mRNA expression at 10 uM measured after 8 hrs by qRT-PCR analysis
Agonist activity at TLX (unknown origin) assessed as induction of receptor oligomerization using sGFP-labeled TLX LBD as acceptor and biotin TLX LBD as donor measured after 20 hrs incubation at RT and 2 hrs at 37 degC by HTRF assay
Destabilization of recombinant TLX LBD (unknown origin) assessed as change in enthalpy at 100 uM by isothermal titration calorimetry
Binding affinity to recombinant TLX LBD (unknown origin) by differential scanning fluorometry
Destabilization of recombinant TLX LBD (unknown origin) assessed as change in melting temperature at 100 uM by isothermal titration calorimetry
Agonist activity at human full length Gal4-fused TLX transfected in human HEK293T cells coexpressing pFR-TAE-Luc assessed as repressor activity of receptor by measuring decrease in reporter activity by dual-glo luciferase assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Agonist activity at human Gal4-fused TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP16 assessed as repressor activity of receptor by measuring decrease in reporter activity measured after 14 hrs by Dual-Glo Luciferase assay
Assay data:5 Active, 2 Activity ≤ 1 µM, 7 Tested
Agonist activity at full length TLX activating element expressed in human HEK293T cells coexpressing human full-length TLX/Gal4-VP 16 assessed as fold increase in reporter activity at 100 uM by luciferase reporter gene assay relative to control
Assay data:6 Tested
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