Table 1.

Reported FXR ligands

Year	Function	Compounds	Structure type	Source	Reference
1995	Agonist	Farnesol Farnesol metabolites	Terpenoid	Nature	[2]
1999	Agonist	CDCA DCA LCA TTNPB	Steroid Aromatics	Nature Synthesis	[4] [5]
1999	Agonist	CDCA CA DCA LCA	Steroid	Nature	[3]
2000	Agonist	Forskolin	Steroid	Nature	[7]
2000	Agonist	GW4064 GW9047	Aromatics	Synthesis	[120]
2001	Agonist	1,1-Bisphosphonate esters	Aromatics	Synthesis	[121]
2002	Agonist	6-ECDCA	Steroid	Semi-synthesis	[10]
2003	Agonist	fexaramine	Aromatics	Synthesis	[122]
2003	Antagonist	Guggulsterone	Steroid	Nature	[9]
2003	Agonist	Fexaramate Fexarene Fexaramine Fexarine fexarchloramide	Aromatics	Synthesis	[123]
2003	Agonist Antagonist	AGN29 AGN 31 AGN 34	Aromatics	Synthesis	[124]
2004	Agonist	UDCA	Steroid	Nature	[125]
2004	Agonist	CDCA derivatives	Steroid	Semi-synthesis	[126]
2004	Antagonist	Arachidonic acid Docosahexaenoic acid Linolenic acid	Fatty acid	Nature	[127]
2005	Agonist	Xanthohumol	Aromatics	Nature	[128]
2006	Agonist	22 (R)-hydroxycholesterol	Steroid	Nature	[129]
2006	Agonist Antagonist	Bile alcohols 5β-cyprinol Bile alcohols 5β-bufol Bile alcohols 5α-cyprinol Bile alcohols 5α-bufol	Steroid	Semi-synthesis	[130]
2006	Agonist	Androsterone	Steroid	Nature	[6]
2006	Agonist	Diphenylmethane skeleton	Steroid	Synthesis	[131]
2007	Antagonist	GW4064 derivatives	Aromatics	Semi-synthesis	[132]
2007	Antagonist	Stigmasterol	Steroid	Nature	[8]
2007	Agonist	Cafestol	Terpenoid	Nature	[133]
2008	Agonist	GSK8062	Aromatics	Semi-synthesis	[134]
2008	Agonist	Pyrazolidine-3,5-dione derivatives	Aromatics	Semi-synthesis	[135]
2008	Agonis	Coumestrol	Steroid	Nature	[136]
2008	Agonist	Methyl cholate, Methyl deoxycholate 5β-Cholanic acid, 5β-Cholanic acid-7α,12α-diol NIHS700 marchantinA marchantin E	Steroid Aromatics	Semi-synthesis Nature	[137]
2009	Agonist	Froglitazone Rosiglitazone Pioglitazone	Alkaloid	Synthesis	[138]
2009	Agonist	WAY-362450	Alkaloid	Synthesis	[139]
2009	Agonist	Pyrrole [2,3-d]azepines	Alkaloid	Semi-synthesis	[140]
2009	Agonist	N-oxide pyridine GW4064	Aromatics		[141]
2009	Agonist	Bile alcohols	Steroid	Semi-synthesis	[142]
2010	Antagonist	Oleanolic acid	Terpenoid	Nature	(20)
2011	Agonist	GSK2324	Aromatics	Semi-synthesis	[143]
2011	Antagonist	Sulfated sterols	Steroid	Semi-synthesis	[144]
2011	Agonist	6a-Ethyl-24-norcholanyl-23- amine derivate	Steroid	Semi-synthesis	[145]
2011	Antagonist	Tuberatolides	Terpenoid	Nature	[146]