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THR/RXR Heterodimer Assay for Thyroid Hormone Receptor Agonist Screening from US Patent US20240059682: "THYROID HORMONE RECEPTOR BETA AGONIST COMPOUNDS"
Assay data:26 Active, 25 Activity ≤ 1 µM, 26 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay for Thyroid Hormone Receptor Agonist Screening from US Patent US20240059682: "THYROID HORMONE RECEPTOR BETA AGONIST COMPOUNDS"
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
THR Reporter Gene Method from US Patent US20240059676: "THYROID HORMONE RECEPTOR b SELECTIVE AGONIST COMPOUND, PHARMACEUTICAL COMPOSITION AND USE THEREOF"
Assay data:32 Active, 21 Activity ≤ 1 µM, 38 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Agonist activity at human RXR-alpha assessed as receptor transactivation at 500 to 20000 nM incubated for 24 hrs by luciferase reporter gene assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human RXR-alpha assessed as receptor transactivation incubated for 24 hrs by luciferase reporter gene assay
Activation of RXRalpha (unknown origin) at 10 uM
Agonist activity at human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21 (DE3) assessed as increase in fluorescein labeled D22 coactivator peptide recruitment at 3000 nM incubated for 2 hrs by fluorescence polarization assay
Assay data:3 Active, 4 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21 (DE3) assessed as increase in fluorescein labeled PGC-1alpha coactivator peptide recruitment at 3000 nM incubated for 2 hrs by fluorescence polarization assay
Agonist activity at human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21 (DE3) assessed as increase in fluorescein labeled SRC1-2 coactivator peptide recruitment at 3000 nM incubated for 2 hrs by fluorescence polarization assay
Displacement of CU-6PMN from human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21 (DE3) assessed as fold change incubated for 30 mins by fluorospectrometer relative to NEt-3IB
Assay data:2 Tested
Displacement of CU-6PMN from human PPARgamma-LBD (206 to 477 residues)/human RXRalpha-LBD (224 to 462 residues) heterodimer assessed as fold change incubated for 30 mins by fluorospectrometer relative to NEt-3IB
Displacement of CU-6PMN from human PPARgamma-LBD (206 to 477 residues)/human RXRalpha-LBD (224 to 462 residues) heterodimer incubated for 30 mins by fluorospectrometer
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to human PPARgamma-LBD (206 to 477 residues)/human RXRalpha-LBD (224 to 462 residues) heterodimer assessed as change in entropy using PGC-1alpha as coactivator peptide by isothermal titration calorimetry analysis
Binding affinity to human PPARgamma-LBD (206 to 477 residues)/human RXRalpha-LBD (224 to 462 residues) heterodimer assessed as change in enthalpy using PGC-1alpha as coactivator peptide by isothermal titration calorimetry analysis
Binding affinity to human PPARgamma-LBD (206 to 477 residues)/human RXRalpha-LBD (224 to 462 residues) heterodimer assessed as gibbs free energy change using PGC-1alpha as coactivator peptide by isothermal titration calorimetry analysis
Binding affinity to human PPARgamma-LBD (206 to 477 residues)/human RXRalpha-LBD (224 to 462 residues) heterodimer assessed as dissociation constant using PGC-1alpha as coactivator peptide by isothermal titration calorimetry analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21 (DE3) assessed as change in entropy using PGC-1alpha as coactivator peptide by isothermal titration calorimetry analysis
Assay data:3 Tested
Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21 (DE3) assessed as change in entropy using SRC1 as coactivator peptide by isothermal titration calorimetry analysis
Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21 (DE3) assessed as change in enthalpy using PGC-1alpha as coactivator peptide by isothermal titration calorimetry analysis
Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21 (DE3) assessed as change in enthalpy using SRC1 as coactivator peptide by isothermal titration calorimetry analysis
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