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Agonist activity at human THRbeta transfected in Huh7 cells co-transfected with luciferase reporter plasmid assessed as reduction in luciferase activity incubated for 16 hrs by Steady-Glo luciferase assay
Assay data:15 Active, 15 Activity ≤ 1 µM, 20 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human THRalpha transfected in Huh7 cells co-transfected with luciferase reporter plasmid assessed as reduction in luciferase activity incubated for 16 hrs by Steady-Glo luciferase assay
Assay data:15 Active, 1 Activity ≤ 1 nM, 13 Activity ≤ 1 µM, 20 Tested
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
Assay data:28 Active, 28 Activity ≤ 1 µM, 32 Tested
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
Assay data:21 Active, 20 Activity ≤ 1 µM, 28 Tested
Agonist activity at human THR-beta expressed in CHO-K1 cells by PathHunter assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Agonist activity at human THR-alpha expressed in CHO-K1 cells by PathHunter assay
transactivation assay from US Patent US10544075: "Derivatives of sobetirome"
Assay data:4 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
TR Receptor Ligand Binding Assay from Article 10.1016/s1074-5521(98)90168-5: "A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor."
Assay data:3 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Transactivation Assay in HeLa cells from Article 10.1021/cb600311v: "Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist."
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Transactivation Assay in U2OS cells from Article 10.1021/cb600311v: "Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist."
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
Competition Binding Assay from Article 10.1021/cb600311v: "Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist."
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
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."
Assay data:41 Active, 7 Activity ≤ 1 nM, 41 Activity ≤ 1 µM, 41 Tested
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."
Assay data:9 Active, 2 Activity ≤ 1 nM, 9 Activity ≤ 1 µM, 9 Tested
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."
Assay data:9 Active, 1 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 9 Tested
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 pharmacological selectivity compared with KB-141."
Assay data:15 Active, 6 Activity ≤ 1 nM, 13 Activity ≤ 1 µM, 15 Tested
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 pharmacological selectivity compared with KB-141."
Assay data:15 Active, 1 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 15 Tested
TRbeta-Binding Assay from Article 10.1021/jm021080f: "Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1."
Assay data:6 Active, 5 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
TRalpha-Binding Assay. from Article 10.1021/jm021080f: "Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1."
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 followed by peptide addition and measured after 30 mins by HTRF assay
Assay data:17 Active, 14 Activity ≤ 1 µM, 18 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
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 followed by peptide addition and measured after 30 mins by HTRF assay
Assay data:13 Active, 6 Activity ≤ 1 µM, 18 Tested
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