Target family: 1A. Thyroid hormone receptors (type: nhr)
Target: Thyroid hormone receptor-&beta;

Ligand: VK2809 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.529999732971191 pKi
Reference (Journal): Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
Published in: J Med Chem

Ligand: T4 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2000)
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2 products to bind T3.
Published in: Mol Endocrinol

Ligand: triiodothyronine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1956)
Primary target: yes
Median affinity: 10.100000381469727 pKd
Reference (Journal): Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
Published in: J Med Chem

Ligand: tiratricol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 10.7 pKd
Reference (Journal): Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2 products to bind T3.
Published in: Mol Endocrinol

Ligand: sobetirome (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 10.17 pKd
Reference (Journal): A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.
Published in: Chem Biol

Ligand: sobetirome (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 10.17 pKd
Reference (Journal): Opiate-dependent modulation of adenylate cyclase.
Published in: Proc Natl Acad Sci USA

Ligand: rT3 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.34 pKd
Reference (Journal): Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2 products to bind T3.
Published in: Mol Endocrinol

Ligand: resmetirom (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 6.679999828338623 pEC50
Reference (Journal): 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 dyslipidemia.
Published in: J Med Chem

Ligand: NH-3 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.03 pKd
Reference (Journal): Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
Published in: J Med Chem

Ligand: KB-141 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.96 pIC50
Reference (Journal): Selective thyroid hormone receptor-beta activation: a strategy for reduction of weight, cholesterol, and lipoprotein (a) with reduced cardiovascular liability.
Published in: Proc Natl Acad Sci USA

Ligand: dextrothyroxine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity:  -
Reference (Journal): Effects of dextrothyroxine on the pituitary-thyroid axis in hypercholesterolemic children and goitrous adults.
Published in: J Clin Endocrinol Metab

Ligand: compound 16g [PMID: 35507418] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.679999828338623 pEC50
Reference (Journal): Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.
Published in: J Med Chem