| Assay ID | Title | Year | Journal | Article |
|---|
| AID1140033 | Toxicity in hypercholesterolemic rabbit model assessed as effect on central thyroid axis | 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 |
| AID1139995 | Inhibition of CYP3A4 (unknown origin) | 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 |
| AID1140013 | Half life in rat at 5 mg/kg, po | 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 |
| AID1140051 | Plasma concentration in thyroidectomized rat at 20 mg/kg, ip measured after 6 hrs | 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 |
| AID1910212 | Agonist activity at human TR beta LBD (202 to 461 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1910222 | Inhibition of lipid metabolism in human HepG2 assessed as reduction in intracellular tryglyceride level at 1 to 10 uM incubated for 24 hrs | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1675039 | Selectivity index, ratio of EC50 for THRalpha (unknown origin) to EC50 for THRbeta (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Selective thyroid hormone receptor β agonists with oxadiazolone acid isosteres. |
| AID1140014 | Oral bioavailability in rat at 5 mg/kg | 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 |
| AID1139994 | Inhibition of human ERG | 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 |
| AID1910228 | Induction of mitochondrial uncoupled respiration in human HepG2 cells assessed as increase in oxygen consumption rate at 10 uM measured after 24 hrs by Seahorse XFe96 flux analyzer | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1140041 | Toxicity in healthy human with mildly elevated LDL-C level assessed as effect on vital signs at 5 to 200 mg, po qd for 2 weeks by multiple ascending dose study | 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 |
| AID1140045 | Toxicity in healthy human with mildly elevated LDL-C level assessed as effect on free T3 level at 100 to 200 mg, po qd for 2 weeks | 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 |
| AID1140047 | Antidyslipidemic activity in healthy human with mildly elevated LDL-C level assessed as reduction in LDL-C at 50 to 200 mg, po qd for 2 weeks by multiple ascending dose study relative to placebo control | 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 |
| AID1910227 | Induction of mitochondrial basal respiration in human HepG2 cells assessed as increase in oxygen consumption rate at 10 uM measured after 24 hrs by Seahorse XFe96 flux analyzer | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1140010 | AUC in rat at 5 mg/kg, po | 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 |
| AID1140002 | Time-dependent inhibition of CYP2C9 (unknown origin) | 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 |
| AID1139996 | Inhibition of CYP3A5 (unknown origin) | 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 |
| AID1140036 | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as lowering glucose level to near normal level | 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 |
| AID1140028 | Toxicity in hypercholesterolemic rat model assessed as effect on TSH level | 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 |
| AID1140000 | Time-dependent inhibition of CYP3A5 (unknown origin) | 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 |
| AID1910211 | Agonist activity at wild type human TR alpha LBD expressed in Escherichia coli BL21 (DE3) assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1140034 | Antidyslipidemic activity in hypercholesterolemic rabbit model assessed as reduction in lipid level in coadministered with atorvastatin | 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 |
| AID1140029 | Toxicity in hypercholesterolemic rat model assessed as effect on central thyroid axis | 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 |
| AID1140053 | Fraction unbound in human | 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 |
| 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 |
| AID1910226 | Inhibition of lipid metabolism in human HepG2 cells assessed as reduction in total lipid accumulation at 10 uM incubated for 24 hrs by oil red O staining based inverted microscopic analysis | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1139997 | Inhibition of CYP2C19 (unknown origin) | 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 |
| AID1140044 | Toxicity in healthy human with mildly elevated LDL-C level assessed as reversible reduction in free T4 level at 100 mg, po qd for 2 weeks | 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 |
| 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 |
| AID1910224 | Inhibition of lipid metabolism in mouse primary hepatocytes assessed as reduction in intracellular total cholesterol level at 10 uM incubated for 24 hrs | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1139991 | Toxicity in thyroidectomized rat assessed as T3 activity at 37.5 mg/kg, ip measured after 6 hrs | 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 |
| AID1140008 | Volume of distribution at steady state in rat at 5 mg/kg, iv | 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 |
| AID1140030 | Antidyslipidemic activity in hypercholesterolemic rabbit model assessed as reduction in non-HDL-C level | 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 |
| AID1140055 | Antidyslipidemic activity in human assessed as reduction in LDL-C at 200 ug, po qd relative to control | 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 |
| AID1675041 | Agonist activity at recombinant hexa-His-tagged THRbeta LBD (148 to 410 residues) (unknown origin)/recombinant human EE-tagged RXRalpha LBD (225 to 462 residues) assessed as increase in biotinylated GRIP1 peptide recruitment preincubated for 30 mins follo | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Selective thyroid hormone receptor β agonists with oxadiazolone acid isosteres. |
| AID1675040 | Agonist activity at recombinant hexa-His-tagged THRalpha LBD (202 to 461 residues) (unknown origin)/recombinant human EE-tagged RXRalpha LBD (225 to 462 residues) assessed as increase in biotinylated GRIP1 peptide recruitment preincubated for 30 mins foll | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21
| Selective thyroid hormone receptor β agonists with oxadiazolone acid isosteres. |
| AID1140012 | Cmax in rat at 5 mg/kg, po | 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 |
| AID1140035 | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as improvement of insulin sensitivity | 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 |
| AID1140004 | Permeability from apical to basolateral side of human Caco2 cells | 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 |
| 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 |
| AID1140001 | Time-dependent inhibition of CYP2C19 (unknown origin) | 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 |
| AID1140026 | Antidyslipidemic activity in hypercholesterolemic rat model assessed as reduction in non-HDL-C level | 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 |
| AID1140049 | Antidyslipidemic activity in healthy human with mildly elevated LDL-C level assessed as reduction in lipids at 80 mg, po qd | 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 |
| AID1140003 | Solubility of the compound at pH 7.4 | 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 |
| AID1140048 | Antidyslipidemic activity in healthy human with mildly elevated LDL-C level assessed as reduction in triglyceride at 50 to 200 mg, po qd for 2 weeks by multiple ascending dose study relative to placebo control | 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 |
| AID1910220 | Binding affinity to human TR alpha LBD assessed as change in melting temperature at 10 uM by thermal shift assay | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1139985 | Plasma concentration in thyroidectomized rat at 37.5 mg/kg, ip measured after 6 hrs | 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 |
| AID1140050 | Permeability from basolateral to apical side of human Caco2 cells | 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 |
| AID1140005 | Efflux ratio of permeability in human Caco2 cells | 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 |
| AID1140017 | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as reduction in liver triglycerides at 0.3 to 10 mg/kg, po administered daily for 23 days | 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 |
| AID1139998 | Inhibition of CYP2C9 (unknown origin) | 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 |
| AID1140039 | Toxicity in healthy human with mildly elevated LDL-C level assessed as effect on heart rate at 5 to 200 mg, po qd for 2 weeks by multiple ascending dose study | 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 |
| AID1140032 | Toxicity in hypercholesterolemic rabbit model assessed as effect on TSH level | 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 |
| AID1140020 | Toxicity in diet-induced obese C57Bl/6J mouse model assessed as effect on kidney size at 0.3 to 10 mg/kg, po administered daily for 23 days | 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 |
| AID1140040 | Toxicity in healthy human with mildly elevated LDL-C level assessed as effect on QT interval at 5 to 200 mg, po qd for 2 weeks by multiple ascending dose study | 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 |
| AID1910216 | Selectivity ratio of EC50 for agonist activity at wild type human TR alpha LBD expressed in Escherichia coli BL21 (DE3) to EC50 for agonist activity at human TR beta LBD (202 to 461 residues) expressed in Escherichia coli BL21 (DE3) cells | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1140011 | Tmax in rat at 5 mg/kg, po | 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 |
| AID1910223 | Inhibition of lipid metabolism in human HepG2 assessed as reduction in intracellular total cholesterol level at 1 to 10 uM incubated for 24 hrs | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1139986 | Plasma concentration in thyroidectomized rat at 5 mg/kg, ip measured after 6 hrs | 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 |
| AID1140015 | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as reduction in cholesterol level at 0.3 to 10 mg/kg, po administered daily for 23 days | 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 |
| 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 |
| AID1140027 | Antidyslipidemic activity in hypercholesterolemic rat model assessed as reduction in liver triglycerides | 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 |
| AID1140007 | Clearance in rat at 5 mg/kg, iv | 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 |
| AID1140006 | AUC in rat at 5 mg/kg, iv | 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 |
| AID1140046 | Toxicity in healthy human with mildly elevated LDL-C level assessed as effect on TSH level at 100 to 200 mg, po qd for 2 weeks | 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 |
| AID1139999 | Time-dependent inhibition of CYP3A4 (unknown origin) | 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 |
| AID1910225 | Inhibition of lipid metabolism in mouse primary hepatocytes assessed as reduction in intracellular tryglyceride level at 10 uM incubated for 24 hrs | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1140009 | Half life in rat at 5 mg/kg, iv | 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 |
| AID1140038 | Toxicity in healthy human with mildly elevated LDL-C level assessed as central thyroid axis dysfunction at 5 to 200 mg, po qd for 2 weeks by multiple ascending dose study | 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 |
| AID1140042 | Toxicity in healthy human with mildly elevated LDL-C level assessed as effect on effect on liver enzymes at 5 to 200 mg, po qd for 2 weeks by multiple ascending dose study | 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 |
| AID1140037 | Toxicity in healthy human with mildly elevated LDL-C level assessed as adverse events at 5 to 200 mg, po qd for 2 weeks by multiple ascending dose study | 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 |
| 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 |
| AID1140043 | Toxicity in healthy human with mildly elevated LDL-C level assessed as reversible reduction in free T4 level at 200 mg, po qd for 2 weeks | 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 |
| AID1140019 | Toxicity in diet-induced obese C57Bl/6J mouse model assessed as effect on heart size at 0.3 to 10 mg/kg, po administered daily for 23 days | 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 |
| AID1140018 | Toxicity in diet-induced obese C57Bl/6J mouse model assessed as effect on bone mineral density at 0.3 to 10 mg/kg, po administered daily for 23 days | 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 |
| AID1910218 | Agonist activity at human TR beta LBD (202 to 461 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay relative to control | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1140031 | Antidyslipidemic activity in hypercholesterolemic rabbit model assessed as reduction in liver triglycerides | 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 |
| AID1140052 | Ratio of drug uptake in liver to plasma in diet-induced obese C57Bl/6J mouse model | 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 |
| AID1139983 | Cardiotoxicity in thyroidectomized rat assessed as induction of alpha-MHC hnRNA expression in cardiac myocyte at 5 to 37.5 mg/kg, ip measured after 6 hrs | 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 |
| AID1910217 | Agonist activity at wild type human TR alpha LBD expressed in Escherichia coli BL21 (DE3) assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay relative to control | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10
| Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. |
| AID1139993 | Intrinsic clearance in human hepatocytes assessed per million cells | 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 |
| AID1140016 | Antidyslipidemic activity in diet-induced obese C57Bl/6J mouse model assessed as reduction in liver size at 0.3 to 10 mg/kg, po administered daily for 23 days | 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 |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |