Target family: Bile acid receptor (type: gpcr)
Target: GPBA receptor

Ligand: XYT528B (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.079999923706055 pEC50
Reference (Journal): Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5<sup>H88Y</sup> Mutant Mice.
Published in: J Med Chem

Ligand: S-EMCA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.090000152587891 pEC50
Reference (Journal): Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.
Published in: J Med Chem

Ligand: oleanolic acid (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.65 pEC50
Reference (Journal): Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea.
Published in: Biochem Biophys Res Commun

Ligand: lithocholic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 pEC50
Reference (Journal): Identification of membrane-type receptor for bile acids (M-BAR).
Published in: Biochem Biophys Res Commun

Ligand: INT-767 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 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: deoxycholic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2015)
Median affinity: 6.2 pEC50
Reference (Journal): Identification of membrane-type receptor for bile acids (M-BAR).
Published in: Biochem Biophys Res Commun

Ligand: compound 77A [PMID: 37639383] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pEC50
Reference (Journal): Discovery, Structure-Activity Relationships, and In Vivo Activity of Dihydropyridone Agonists of the Bile Acid Receptor TGR5.
Published in: J Med Chem

Ligand: compound 77A [PMID: 37639383] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pEC50
Reference (Journal): Discovery, Structure-Activity Relationships, and In Vivo Activity of Dihydropyridone Agonists of the Bile Acid Receptor TGR5.
Published in: J Med Chem

Ligand: compound 15 [PMID: 25411721] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.420000076293945 pEC50
Reference (Journal): G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonists reduce the production of proinflammatory cytokines and stabilize the alternative macrophage phenotype.
Published in: J Med Chem

Ligand: compound 15 [PMID: 25411721] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pEC50
Reference (Journal): G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) agonists reduce the production of proinflammatory cytokines and stabilize the alternative macrophage phenotype.
Published in: J Med Chem

Ligand: compound 11d [PMID: 34406006] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.170000076293945 pEC50
Reference (Journal): Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5<sup>H88Y</sup> Mutant Mice.
Published in: J Med Chem

Ligand: compound 11d [PMID: 34406006] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.039999961853027 pEC50
Reference (Journal): Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5<sup>H88Y</sup> Mutant Mice.
Published in: J Med Chem

Ligand: cholic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2013), FDA (2015)
Median affinity: 5 pEC50
Reference (Journal): Identification of membrane-type receptor for bile acids (M-BAR).
Published in: Biochem Biophys Res Commun

Ligand: chenodeoxycholic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1983), EMA (2017)
Median affinity: 5.4 pEC50
Reference (Journal): Identification of membrane-type receptor for bile acids (M-BAR).
Published in: Biochem Biophys Res Commun

Ligand: betulinic acid (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.980000019073486 pEC50
Reference (Journal): Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes.
Published in: J Med Chem

Ligand: XYT528B (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.579999923706055 pEC50
Reference (Journal): Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5<sup>H88Y</sup> Mutant Mice.
Published in: J Med Chem