Target family: Free fatty acid receptors (type: gpcr)
Target: FFA2 receptor

Ligand: butyric acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids.
Published in: J Biol Chem

Ligand: CATPB (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3.
Published in: J Biol Chem

Ligand: compound 1 [PMID: 23589301] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pEC50
Reference (Journal): Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptor.
Published in: J Biol Chem

Ligand: propanoic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids.
Published in: Biochem Biophys Res Commun

Ligand: propanoic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation.
Published in: J Biol Chem

Ligand: pentanoic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids.
Published in: J Biol Chem

Ligand: trans-2-methylcrotonic acid (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 3.799999952316284 pEC50
Reference (Journal): Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3.
Published in: J Biol Chem

Ligand: isobutyric acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation.
Published in: J Biol Chem

Ligand: GLPG0974 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.
Published in: J Med Chem

Ligand: CPTB (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.150000095367432 pIC50
Reference (Journal): The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators.
Published in: Bioorg Med Chem Lett

Ligand: GLPG0974 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.050000190734863 pIC50
Reference (Journal): Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects.
Published in: Br J Clin Pharmacol

Ligand: butyric acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3.
Published in: J Biol Chem

Ligand: butyric acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation.
Published in: J Biol Chem

Ligand: butyric acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids.
Published in: Biochem Biophys Res Commun

Ligand: AMG7703 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator.
Published in: Mol Pharmacol

Ligand: AMG7703 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification and functional characterization of allosteric agonists for the G protein-coupled receptor FFA2.
Published in: Mol Pharmacol

Ligand: acetic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Functional characterization of human receptors for short chain fatty acids and their role in polymorphonuclear cell activation.
Published in: J Biol Chem

Ligand: acetic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Identification of a free fatty acid receptor, FFA2R, expressed on leukocytes and activated by short-chain fatty acids.
Published in: Biochem Biophys Res Commun

Ligand: acetic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3.
Published in: J Biol Chem

Ligand: acetic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids.
Published in: J Biol Chem

Ligand: 1-methylcyclopropanecarboxylic acid (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 2.5999999046325684 pEC50
Reference (Journal): Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3.
Published in: J Biol Chem