Target family: 1I. Vitamin D receptor-like receptors (type: nhr)
Target: Pregnane X receptor

Ligand: 17β-estradiol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1954, prior history unavailable)
Median affinity:  -
Reference (Journal): The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution.
Published in: Mol Endocrinol

Ligand: 3-keto-lithocholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.8 pEC50
Reference (Journal): The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity.
Published in: Proc Natl Acad Sci USA

Ligand: 5β-cholestane-3α,7α,12α-triol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.3 pEC50
Reference (Journal): Identification of bile acid precursors as endogenous ligands for the nuclear xenobiotic pregnane X receptor.
Published in: Proc Natl Acad Sci USA

Ligand: 5β-cholestane-3α,7α,12α-triol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): Identification of an endogenous ligand that activates pregnane X receptor-mediated sterol clearance.
Published in: Proc Natl Acad Sci USA

Ligand: 5β-pregnane-3,20-dione (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.4 pIC50
Reference (Journal): The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution.
Published in: Mol Endocrinol

Ligand: clotrimazole (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1975)
Median affinity:  -
Reference (Journal): Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction.
Published in: Proc Natl Acad Sci USA

Ligand: dexamethasone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1958), EMA (2010)
Median affinity: 6.1 pEC50
Reference (Journal): An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway.
Published in: Cell

Ligand: garcinoic acid (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.480000019073486 pKd
Reference (Journal): Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
Published in: J Med Chem

Ligand: garcinoic acid (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.889999866485596 pEC50
Reference (Journal): Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.
Published in: J Med Chem

Ligand: hyperforin (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pEC50
Reference (Journal): St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor.
Published in: Proc Natl Acad Sci USA

Ligand: hyperforin (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pEC50
Reference (Journal): St John's wort, a herbal antidepressant, activates the steroid X receptor.
Published in: J Endocrinol

Ligand: lithocholic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.05 pEC50
Reference (Journal): The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity.
Published in: Proc Natl Acad Sci USA

Ligand: lovastatin (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1987)
Median affinity:  pEC50
Reference (Journal): The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.
Published in: J Clin Invest

Ligand: mifepristone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2000)
Median affinity: 5 pEC50
Reference (Journal): The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.
Published in: J Clin Invest

Ligand: nifedipine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1981)
Median affinity:  -
Reference (Journal): Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction.
Published in: Proc Natl Acad Sci USA

Ligand: paclitaxel (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1992), EMA (2008)
Median affinity: 5.3 pEC50
Reference (Journal): The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux.
Published in: Nat Med

Ligand: phenobarbital (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (no date available)
Median affinity:  -
Reference (Journal): The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.
Published in: J Clin Invest

Ligand: pregnenolone-16α-carbonitrile (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.5 pEC50
Reference (Journal): An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway.
Published in: Cell

Ligand: rifampicin (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1971)
Primary target: no
Median affinity:  pEC50
Reference (Journal): SXR, a novel steroid and xenobiotic-sensing nuclear receptor.
Published in: Genes Dev

Ligand: rifampicin (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1971)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.
Published in: J Clin Invest

Ligand: (+)-S20 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.4 pEC50
Reference (Journal): A pregnane X receptor agonist with unique species-dependent stereoselectivity and its implications in drug development.
Published in: Mol Pharmacol

Ligand: S20 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.7 pEC50
Reference (Journal): A pregnane X receptor agonist with unique species-dependent stereoselectivity and its implications in drug development.
Published in: Mol Pharmacol

Ligand: schisandrin A (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.7 pEC50
Reference (Journal): Traditional Chinese medicines Wu Wei Zi (Schisandra chinensis Baill) and Gan Cao (Glycyrrhiza uralensis Fisch) activate pregnane X receptor and increase warfarin clearance in rats.
Published in: J Pharmacol Exp Ther