Target family: 1B. Retinoic acid receptors (type: nhr)
Target: Retinoic acid receptor-&beta;

Ligand: TTNPB (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Activation of retinoid X receptors induces apoptosis in HL-60 cell lines.
Published in: Mol Cell Biol

Ligand: TTNPB (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Different agonist- and antagonist-induced conformational changes in retinoic acid receptors analyzed by protease mapping.
Published in: Mol Cell Biol

Ligand: TTNPB (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.
Published in: J Mol Biol

Ligand: TTNPB (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Therapeutic applications for ligands of retinoid receptors.
Published in: Curr Pharm Des

Ligand: trifarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 6.900000095367432 pEC50
Reference (Journal): Structure-based design of Trifarotene (CD5789), a potent and selective RARγ agonist for the treatment of acne.
Published in: Bioorg Med Chem Lett

Ligand: tretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 9.399999618530273 pKi
Reference (Journal): Therapeutic applications for ligands of retinoid receptors.
Published in: Curr Pharm Des

Ligand: tretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 9.399999618530273 pKi
Reference (Journal): Different agonist- and antagonist-induced conformational changes in retinoic acid receptors analyzed by protease mapping.
Published in: Mol Cell Biol

Ligand: tretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 9.399999618530273 pKi
Reference (Journal): Activation of retinoid X receptors induces apoptosis in HL-60 cell lines.
Published in: Mol Cell Biol

Ligand: tretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 9.399999618530273 pKi
Reference (Journal): Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.
Published in: J Mol Biol

Ligand: tretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 7.920000076293945 pEC50
Reference (Journal): Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.
Published in: Bioorg Med Chem Lett

Ligand: tazarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 9.100000381469727 pEC50
Reference (Journal): Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.
Published in: Bioorg Med Chem Lett

Ligand: tamibarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: no
Median affinity: 6.630000114440918 pEC50
Reference (Journal): Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Published in: J Med Chem

Ligand: [3H]9-cis-retinoic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKd
Reference (Journal): Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids.
Published in: Proc Natl Acad Sci USA

Ligand: Ro 40-6055 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.069999694824219 pEC50
Reference (Journal): Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.
Published in: Bioorg Med Chem Lett

Ligand: KCL-286 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.720000267028809 pEC50
Reference (Journal): Discovery and lead optimisation of a potent, selective and orally bioavailable RAR&#x3b2; agonist for the potential treatment of nerve injury.
Published in: Bioorg Med Chem Lett

Ligand: CD666 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.64 pKd
Reference (Journal): Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma.
Published in: Biochem Biophys Res Commun

Ligand: BMS641 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): Rational design of RAR-selective ligands revealed by RARbeta crystal stucture.
Published in: EMBO Rep

Ligand: BMS493 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.54 pIC50
Reference (Journal): Co-regulator recruitment and the mechanism of retinoic acid receptor synergy.
Published in: Nature

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 9.699999809265137 pKi
Reference (Journal): Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.
Published in: J Mol Biol

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 9.699999809265137 pKi
Reference (Journal): Activation of retinoid X receptors induces apoptosis in HL-60 cell lines.
Published in: Mol Cell Biol

Ligand: AGN193109 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Recruitment of nuclear receptor corepressor and coactivator to the retinoic acid receptor by retinoid ligands. Influence of DNA-heterodimer interactions.
Published in: J Biol Chem

Ligand: AGN193109 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Identification and functional separation of retinoic acid receptor neutral antagonists and inverse agonists.
Published in: J Biol Chem

Ligand: AGN193109 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Therapeutic applications for ligands of retinoid receptors.
Published in: Curr Pharm Des

Ligand: adapalene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 7.46999979019165 pKi
Reference (Journal): Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes.
Published in: J Med Chem

Ligand: AC55649 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor beta ligands.
Published in: J Med Chem

Ligand: AC55649 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.
Published in: J Med Chem

Ligand: AC261066 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.
Published in: J Med Chem