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

Ligand: TTNPB (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.44 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: 7.44 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: 7.44 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: 7.44 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: 6.300000190734863 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 pKd
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 pKd
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 pKd
Reference (Journal): Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids.
Published in: Proc Natl Acad Sci USA

Ligand: tretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: yes
Median affinity: 9.399999618530273 pKd
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: 7.769999980926514 pEC50
Reference (Journal): Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.
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 pKd
Reference (Journal): Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.
Published in: J Mol Biol

Ligand: tazarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 7.199999809265137 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: yes
Median affinity: 6.900000095367432 pIC50
Reference (Journal): Retinobenzoic acids. 1. Structure-activity relationships of aromatic amides with retinoidal activity.
Published in: J Med Chem

Ligand: tamibarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity: 7.349999904632568 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: tamibarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity: 6.900000095367432 pIC50
Reference (Journal): Activation of retinoid X receptors induces apoptosis in HL-60 cell lines.
Published in: Mol Cell Biol

Ligand: tamibarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Primary target: yes
Median affinity: 6.900000095367432 pIC50
Reference (Journal): Therapeutic applications for ligands of retinoid receptors.
Published in: Curr Pharm Des

Ligand: [3H]9-cis-retinoic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKd
Reference (Journal): Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids.
Published in: Proc Natl Acad Sci USA

Ligand: Ro 41-5253 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Different agonist- and antagonist-induced conformational changes in retinoic acid receptors analyzed by protease mapping.
Published in: Mol Cell Biol

Ligand: Ro 41-5253 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): A retinoic acid receptor alpha antagonist selectively counteracts retinoic acid effects.
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:  pKd
Reference (Journal): Selective high affinity retinoic acid receptor alpha or beta-gamma ligands.
Published in: Mol Pharmacol

Ligand: Ro 40-6055 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.520000457763672 pEC50
Reference (Journal): Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.
Published in: Bioorg Med Chem Lett

Ligand: CD666 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.65 pKd
Reference (Journal): Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma.
Published in: Biochem Biophys Res Commun

Ligand: BMS753 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.
Published in: Chem Biol

Ligand: BMS614 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Crystal structure of a heterodimeric complex of RAR and RXR ligand-binding domains.
Published in: Mol Cell

Ligand: BMS614 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Co-regulator recruitment and the mechanism of retinoic acid receptor synergy.
Published in: Nature

Ligand: BMS614 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists.
Published in: Chem Biol

Ligand: BMS493 (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): Co-regulator recruitment and the mechanism of retinoic acid receptor synergy.
Published in: Nature

Ligand: BMS-189532 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.570000171661377 pKd
Reference (Journal): Identification of highly potent retinoic acid receptor alpha-selective antagonists.
Published in: J Med Chem

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 9.5 pKd
Reference (Journal): Retinobenzoic acids. 1. Structure-activity relationships of aromatic amides with retinoidal activity.
Published in: J Med Chem

Ligand: AGN193836 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.4 pKd
Reference (Journal): Synthesis and biological activity of retinoic acid receptor-alpha specific amides.
Published in: Bioorg Med Chem Lett

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 9.5 pKd
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: no
Median affinity: 5.960000038146973 pKi
Reference (Journal): Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes.
Published in: J Med Chem