Target family: 1H. Liver X receptor-like receptors (type: nhr)
Target: Farnesoid X receptor

Ligand: 22R-hydroxycholesterol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): Oxysterol 22(R)-hydroxycholesterol induces the expression of the bile salt export pump through nuclear receptor farsenoid X receptor but not liver X receptor.
Published in: J Pharmacol Exp Ther

Ligand: BMS-986318 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.28000020980835 pEC50
Reference (Journal): Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Published in: ACS Med Chem Lett

Ligand: BMS-986339 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.46999979019165 pEC50
Reference (Journal): Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Published in: J Med Chem

Ligand: chenodeoxycholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1983), EMA (2017)
Primary target: yes
Median affinity: 5.300000190734863 pEC50
Reference (Journal): Bile acids: natural ligands for an orphan nuclear receptor.
Published in: Science

Ligand: chenodeoxycholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1983), EMA (2017)
Primary target: yes
Median affinity: 5.300000190734863 pEC50
Reference (Journal): Endogenous bile acids are ligands for the nuclear receptor FXR/BAR.
Published in: Mol Cell

Ligand: cholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA (2013), FDA (2015)
Median affinity:  pEC50
Reference (Journal): Endogenous bile acids are ligands for the nuclear receptor FXR/BAR.
Published in: Mol Cell

Ligand: cholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA (2013), FDA (2015)
Median affinity:  pEC50
Reference (Journal): Bile acids: natural ligands for an orphan nuclear receptor.
Published in: Science

Ligand: cilofexor (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pEC50
Reference (Patent): FXR (NR1H4) binding and activity modulating compounds

Ligand: compound 25 [PMID: 32687365] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.03000020980835 pEC50
Reference (Journal): Design and Structural Optimization of Dual FXR/PPARδ Activators.
Published in: J Med Chem

Ligand: compound 3f [Festa et al., 2019] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.239999771118164 pIC50
Reference (Journal): Investigation around the Oxadiazole Core in the Discovery of a New Chemotype of Potent and Selective FXR Antagonists.
Published in: ACS Med Chem Lett

Ligand: deoxycholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2015)
Median affinity: 4 pEC50
Reference (Journal): U50,488, a kappa opioid receptor agonist, attenuates cocaine-induced increases in extracellular dopamine in the nucleus accumbens of rats.
Published in: Neurosci Lett

Ligand: deoxycholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2015)
Median affinity: 4 pEC50
Reference (Journal): Bile acids: natural ligands for an orphan nuclear receptor.
Published in: Science

Ligand: deoxycholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2015)
Median affinity: 4 pEC50
Reference (Journal): Endogenous bile acids are ligands for the nuclear receptor FXR/BAR.
Published in: Mol Cell

Ligand: fexaramine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pEC50
Reference (Journal): A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR.
Published in: Mol Cell

Ligand: guggulsterone (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptor.
Published in: Mol Endocrinol

Ligand: guggulsterone (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): A natural product that lowers cholesterol as an antagonist ligand for FXR.
Published in: Science

Ligand: GW4064 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pEC50
Reference (Journal): Identification of a chemical tool for the orphan nuclear receptor FXR.
Published in: J Med Chem

Ligand: HPG1860 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pEC50
Reference (Journal): Discovery of HPG1860, a Structurally Novel Nonbile Acid FXR Agonist Currently in Clinical Development for the Treatment of Nonalcoholic Steatohepatitis.
Published in: J Med Chem

Ligand: INT-767 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pEC50
Reference (Journal): Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist.
Published in: Mol Pharmacol

Ligand: lithocholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.3 pEC50
Reference (Journal): Bile acids: natural ligands for an orphan nuclear receptor.
Published in: Science

Ligand: lithocholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.3 pEC50
Reference (Journal): Identification of a nuclear receptor for bile acids.
Published in: Science

Ligand: lithocholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.3 pEC50
Reference (Journal): Endogenous bile acids are ligands for the nuclear receptor FXR/BAR.
Published in: Mol Cell

Ligand: nidufexor (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pEC50
Reference (Journal): Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Published in: J Med Chem

Ligand: obeticholic acid (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: EMA & FDA (2016)
Primary target: yes
Median affinity: 7 pEC50
Reference (Journal): 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.
Published in: J Med Chem

Ligand: tropifexor (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pEC50
Reference (Journal): Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
Published in: J Med Chem