Target family: 2B. Retinoid X receptors (type: nhr)
Target: Retinoid X receptor-&alpha;

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Median affinity:  pIC50
Reference (Journal): Characterization of three RXR genes that mediate the action of 9-cis retinoic acid.
Published in: Genes Dev

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Median affinity:  pIC50
Reference (Journal): 9-cis retinoic acid is a high affinity ligand for the retinoid X receptor.
Published in: Cell

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Median affinity:  pIC50
Reference (Journal): Activation of specific RXR heterodimers by an antagonist of RXR homodimers.
Published in: Nature

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Median affinity:  pIC50
Reference (Journal): 9-cis retinoic acid stereoisomer binds and activates the nuclear receptor RXR alpha.
Published in: Nature

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Median affinity:  pIC50
Reference (Journal): Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids.
Published in: Proc Natl Acad Sci USA

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Median affinity:  pIC50
Reference (Journal): Activation of retinoid X receptors induces apoptosis in HL-60 cell lines.
Published in: Mol Cell Biol

Ligand: bexarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2001)
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells.
Published in: J Med Chem

Ligand: bexarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2001)
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Synthesis and structure-activity relationships of novel retinoid X receptor-selective retinoids.
Published in: J Med Chem

Ligand: bexarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2001)
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Therapeutic applications for ligands of retinoid receptors.
Published in: Curr Pharm Des

Ligand: CD3254 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): Co-regulator recruitment and the mechanism of retinoic acid receptor synergy.
Published in: Nature

Ligand: compound 28 [Heitel et al., 2019] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.019999980926514 pKd
Reference (Journal): Computer-Assisted Discovery and Structural Optimization of a Novel Retinoid X Receptor Agonist Chemotype.
Published in: ACS Med Chem Lett

Ligand: compound 28 [Heitel et al., 2019] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 pEC50
Reference (Journal): Computer-Assisted Discovery and Structural Optimization of a Novel Retinoid X Receptor Agonist Chemotype.
Published in: ACS Med Chem Lett

Ligand: docosahexaenoic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Phytanic acid and docosahexaenoic acid increase the metabolism of all-trans-retinoic acid and CYP26 gene expression in intestinal cells.
Published in: Biochim Biophys Acta

Ligand: docosahexaenoic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Peroxisome proliferator-activated receptors: nuclear control of metabolism.
Published in: Endocr Rev

Ligand: fluorobexarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.369999885559082 pEC50
Reference (Journal): Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene).
Published in: J Med Chem

Ligand: fluorobexarotene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pKi
Reference (Journal): Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene).
Published in: J Med Chem

Ligand: HX 531 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.050000190734863 pIC50
Reference (Journal): Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure.
Published in: Bioorg Med Chem Lett

Ligand: K-80003 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.619999885559082 pIC50
Reference (Journal): NSAID sulindac and its analog bind RXRalpha and inhibit RXRalpha-dependent AKT signaling.
Published in: Cancer Cell

Ligand: LG100268 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Therapeutic applications for ligands of retinoid receptors.
Published in: Curr Pharm Des

Ligand: LG100268 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Activation of specific RXR heterodimers by an antagonist of RXR homodimers.
Published in: Nature

Ligand: LG100268 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Synthesis of high specific activity [3H]-9-cis-retinoic acid and its application for identifying retinoids with unusual binding properties.
Published in: J Med Chem

Ligand: LG100754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo.
Published in: Mol Endocrinol

Ligand: methoprene acid (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): Activation of mammalian retinoid X receptors by the insect growth regulator methoprene.
Published in: Proc Natl Acad Sci USA

Ligand: PA451 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions.
Published in: J Med Chem

Ligand: PA452 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.110000133514404 pA2
Reference (Journal): Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related to RXR Agonist NEt-3IB.
Published in: ACS Med Chem Lett

Ligand: phytanic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Phytanic acid is a retinoid X receptor ligand.
Published in: Eur J Biochem

Ligand: phytanic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Phytanic acid and docosahexaenoic acid increase the metabolism of all-trans-retinoic acid and CYP26 gene expression in intestinal cells.
Published in: Biochim Biophys Acta

Ligand: SR11237 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pEC50
Reference (Journal): Retinoids selective for retinoid X receptor response pathways.
Published in: Science

Ligand: sulindac (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1978)
Primary target: no
Median affinity: 4.099999904632568 pIC50
Reference (Journal): NSAID sulindac and its analog bind RXRalpha and inhibit RXRalpha-dependent AKT signaling.
Published in: Cancer Cell

Ligand: [3H]9-cis-retinoic acid (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pKd
Reference (Journal): Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids.
Published in: Proc Natl Acad Sci USA

Ligand: UVI3003 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Characterization of the interaction between retinoic acid receptor/retinoid X receptor (RAR/RXR) heterodimers and transcriptional coactivators through structural and fluorescence anisotropy studies.
Published in: J Biol Chem