| Assay ID | Title | Year | Journal | Article |
|---|
| AID254851 | Inhibitory concentration against cloned human thyroid hormone receptor alpha 1 | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
| A new class of high affinity thyromimetics containing a phenyl-naphthylene core. |
| AID386175 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in serum TSH level at 0.1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID340059 | Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells at 0.001 uM by TRE-luciferase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands. |
| AID235409 | Ratio of ED50TSH to that of ED50chol was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID299567 | Ratio of ED15 for heart rate in cholesterol-fed rat to ED50 for cholesterol level in cholesterol-fed rat | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID386168 | Toxic cardiac effect in Sprague-Dawley rat assessed as increase in first derivative of left ventricular pressure at 1 mg/kg/day, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386173 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in total 3,5,3',5'-triiodo-L-thyronine level at 0.1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID385932 | Effect on malic enzyme mRNA expression in po dosed Sprague-Dawley rat liver | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID385931 | Effect on CYP7A mRNA expression in po dosed Sprague-Dawley rat liver | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID255360 | Ratio of IC50 of thyroid hormone receptor alpha 1 to that of thyroid hormone receptor beta 1 | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
| A new class of high affinity thyromimetics containing a phenyl-naphthylene core. |
| AID385867 | Reduction in total 3,5,3',5'-tetraiodo-L-thyronine level in po dosed diet-induced obese C57BL/6 mouse | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID385859 | Effect on hepatic LDLR mRNA level in wild-type C57BL/6 mouse at 0.5 mg/kg/day once daily for 7 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386167 | Toxic cardiac effect in Sprague-Dawley rat assessed as increase in heart rate at 1 mg/kg/day, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID385608 | Displacement of [125I]T3 from recombinant thyroid hormone receptor beta expressed in sf9 cells by scintillation proximity assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID345696 | Displacement of [125I]3,5,3'-triiodo-L-thyronine His-tagged human recombinant TRbeta1 by scintillation proximity assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. |
| AID386171 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in total 3,5,3',5'-tetraiodo-L-thyronine level at 0.1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID213163 | Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor alpha) was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID345694 | Selectivity for human TRbeta1 over human TRalpha1 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. |
| AID299561 | Binding affinity at human thyroid hormone receptor beta-1 expressed in CHOK1 cells | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID386178 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in free 3,5,3',5'-tetraiodo-L-thyronine level at 1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386166 | Toxic cardiac effect on Sprague-Dawley rat assessed as increase in systolic aortic pressure at >= 1 mg/kg/day, po for 7 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID299948 | Inhibition of human thyroid hormone receptor beta 1 | 2007 | Bioorganic & medicinal chemistry, Aug-01, Volume: 15, Issue:15
| QSAR study of selective ligands for the thyroid hormone receptor beta. |
| AID299566 | Decrease in cholesterol in po dosed cholesterol-fed rat | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID1139982 | Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay relative to T3 | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys |
| AID386164 | Toxic cardiac effect on Sprague-Dawley rat assessed as increase in first derivative of left ventricular pressure at >= 1 mg/kg/day, po for 7 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID715455 | Binding affinity to TRalpha1 | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia. |
| AID231783 | Ratio of concentration required to inhibit 50% of I-T3 binding to hTR-alpha1 to that of concentration required to inhibit 50% of I-T3 binding to hTR-beta1 was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID299569 | Ratio of ED30 for TSH in cholesterol-fed rat to ED50 for cholesterol level in cholesterol-fed rat | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID385607 | Displacement of [125I]T3 from recombinant thyroid hormone receptor alpha expressed in sf9 cells by scintillation proximity assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID385872 | Reduction in blood glucose level in po dosed diet-induced obese C57BL/6 mouse | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID177494 | Effect upon subcutaneous administration on TSH suppression in rat was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID213174 | Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor beta and an alkaline phosphate reporter gene downstream thyroid response element TRAF-beta1 was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID299562 | Selectivity ratio of IC50 for thyroid hormone receptor alpha-1 to IC50 for thyroid hormone receptor beta-1 | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID231769 | Ratio of chronic administration on TRAF alpha-1 receptor to that of chronic administration on TRAF beta-1 receptor was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID340056 | Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells at 0.001 uM by TRE-luciferase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands. |
| AID173635 | Effect upon subcutaneous administration on the heart rate in rat was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID715456 | Binding affinity to TRbeta1 | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia. |
| AID385632 | Decrease in cholesterol level in LDLR deficient C57BL/6 mouse at 0.5 mg/kg/day once daily for 7 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID1139981 | Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys |
| AID299560 | Binding affinity at human thyroid hormone receptor alpha 1 expressed in CHOK1 cells | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID345695 | Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. |
| AID385853 | Effect on hepatic LDLR mRNA level in LDLR deficient C57BL/6 mouse at 0.5 mg/kg/day once daily for 7 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386182 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in TSH-beta mRNA level at 1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID311017 | Inhibition of thyroid hormone receptor beta | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
| 2D QSAR studies on thyroid hormone receptor ligands. |
| AID213162 | Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor alpha (TRalpha1) and an alkaline phosphate reporter gene downstream thyroid response element TRAF-alpha1 was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID1139979 | Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys |
| AID385935 | Effect on type 1 iodothyronine deiodinase mRNA expression in po dosed Sprague-Dawley rat liver | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386172 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in free 3,5,3',5'-tetraiodo-L-thyronine level at 0.1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386181 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in serum TSH level at 1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386176 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in TSH-beta mRNA level at 0.1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID385609 | Ratio of Ki for recombinant thyroid hormone receptor alpha to Ki for recombinant thyroid hormone receptor beta | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID299563 | Activity against TRAF-alpha-1 expressed in CHOK1 cells by alkaline phosphatase reporter gene assay | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID385636 | Decrease in body weight in diet-induced obese C57BL/6 mouse at 0.03 mg/kg, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID340057 | Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells at 0.01 uM by TRE-luciferase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands. |
| AID340064 | Selectivity ratio of EC50 for human thyroid hormone receptor beta over EC50 for human thyroid hormone receptor alpha by TRE-luciferase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands. |
| AID340058 | Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells at 1 uM by TRE-luciferase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands. |
| AID340061 | Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells at 1 uM by TRE-luciferase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands. |
| AID299568 | Decrease in TSH in po dosed cholesterol-fed rat | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID385874 | Increase in heart weight in po dosed diet-induced obese C57BL/6 mouse | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID340062 | Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells by TRE-luciferase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands. |
| AID385934 | Effect on LDLR mRNA expression in po dosed Sprague-Dawley rat liver | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386174 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in free 3,5,3',5'-triiodo-L-thyronine level at 0.1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID299565 | Increase in heart rate in po dosed cholesterol-fed rat | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID1140054 | Selectivity ratio of EC50 for recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) to EC50 for recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) relative to T3 | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys |
| AID385933 | Effect on SREBP-1c mRNA expression in po dosed Sprague-Dawley rat liver | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID311016 | Inhibition of thyroid hormone receptor alpha | 2007 | Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
| 2D QSAR studies on thyroid hormone receptor ligands. |
| AID385930 | Reduction in plasma cholesterol level in cholesterol fed Sprague-Dawley rat | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386169 | Toxic cardiac effect in Sprague-Dawley rat assessed as increase in heart weight at 1 mg/kg/day, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID340060 | Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells at 0.01 uM by TRE-luciferase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands. |
| AID386179 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by assessed as decrease in total 3,5,3',5'-triiodo-L-thyronine level at 1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID385634 | Decrease in cholesterol level in LDLR deficient C57BL/6 mouse at 5 mg/kg/day once daily for 7 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID177495 | Effect upon subcutaneous administration on cholesterol in rat was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID299564 | Activity against TRAFbeta expressed in CHOK1 cells by alkaline phosphatse reporter gene assay | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID226476 | Ratio of ED15HR to that of ED50chol was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID213175 | Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor beta) was determined | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID385629 | Decrease in liver triglyceride level in po dosed diet-induced obese C57BL/6 mouse after 14 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID340063 | Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells by TRE-luciferase assay | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands. |
| AID385626 | Decrease in cholesterol level in wild-type C57BL/6 mouse at 5 mg/kg/day once daily for 7 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386180 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in free 3,5,3',5'-triiodo-L-thyronine level at 1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386177 | Toxicity in Sprague-Dawley rat assessed as suppression of thyroid hormone axis measured by decrease in total 3,5,3',5'-tetraiodo-L-thyronine level at 1 mg/kg, po after 7 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID715458 | Selectivity ratio of Ki for TRalpha1 to Ki for TRbeta1 | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia. |
| AID385637 | Decrease in cholesterol level in wild-type C57BL/6 mouse at 0.5 mg/kg/day once daily for 7 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID385868 | Reduction in total 3,5,3',5'-triiodo-L-thyronine level in po dosed diet-induced obese C57BL/6 mouse | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386162 | Toxic cardiac effect on Sprague-Dawley rat assessed as increase in heart rate at >= 1 mg/kg/day, po for 7 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID385635 | Decrease in liver weight in po dosed diet-induced obese C57BL/6 mouse after 14 days | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386417 | Reduction in plasma cholesterol level in po dosed diet-induced obese C57BL/6 mouse after 2 weeks | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID386170 | Toxic cardiac effect on Sprague-Dawley rat assessed as decrease in body weight gain at 1 mg/kg/day, po | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Sep-25, Volume: 104, Issue:39
| Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. |
| AID254845 | Inhibitory concentration against cloned human thyroid hormone receptor beta 1 | 2005 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
| A new class of high affinity thyromimetics containing a phenyl-naphthylene core. |
| AID1139980 | Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay relative to T3 | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys |
| AID1797797 | TRalpha-Binding Assay. from Article 10.1016/j.bmcl.2004.04.032: \\Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.\\ | 2004 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13
| Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta. |
| AID1797786 | TRalpha-Binding Assay and Thyroid Response Element (TRAFalpha1) Reporter Assay. from Article 10.1016/j.bmcl.2007.05.049: \\Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacolog | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID1797785 | TRbeta-Binding Assay and Thyroid Response Element (TRAFbeta1) Reporter Assay. from Article 10.1021/jm021080f: \\Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.\\ | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID1797787 | TRbeta-Binding Assay and Thyroid Response Element (TRAFbeta1) Reporter Assay. from Article 10.1016/j.bmcl.2007.05.049: \\Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacologic | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141. |
| AID1797795 | TRalpha-Binding Assay. from Article 10.1016/j.bmcl.2005.11.002: \\Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.\\ | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta. |
| AID1797796 | TRbeta-Binding Assay from Article 10.1016/j.bmcl.2005.11.002: \\Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.\\ | 2006 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
| Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta. |
| AID1797783 | TRalpha-Binding Assay and Thyroid Response Element (TRAFalpha1) Reporter Assay. from Article 10.1021/jm021080f: \\Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.\\ | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID1346752 | Human Thyroid hormone receptor-beta (1A. Thyroid hormone receptors) | 2003 | Proceedings of the National Academy of Sciences of the United States of America, Aug-19, Volume: 100, Issue:17
| Selective thyroid hormone receptor-beta activation: a strategy for reduction of weight, cholesterol, and lipoprotein (a) with reduced cardiovascular liability. |
| AID1346773 | Human Thyroid hormone receptor-alpha (1A. Thyroid hormone receptors) | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2012 | Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
| Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |