Target family: Free fatty acid receptors (type: gpcr)
Target: FFA1 receptor

Ligand: myristic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.
Published in: Nature

Ligand: myristic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids.
Published in: J Biol Chem

Ligand: myristic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs.
Published in: Biochem Biophys Res Commun

Ligand: medica 16 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pEC50
Reference (Journal): A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs.
Published in: Biochem Biophys Res Commun

Ligand: linoleic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids.
Published in: J Biol Chem

Ligand: linoleic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs.
Published in: Biochem Biophys Res Commun

Ligand: linoleic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.
Published in: Nature

Ligand: HWL-088 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pEC50
Reference (Journal): HWL-088, a new potent free fatty acid receptor 1 (FFAR1) agonist, improves glucolipid metabolism and acts additively with metformin in ob/ob diabetic mice.
Published in: Br J Pharmacol

Ligand: GW9508 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.
Published in: Br J Pharmacol

Ligand: GW1100 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.
Published in: Br J Pharmacol

Ligand: GW1100 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Uncovering the pharmacology of the G protein-coupled receptor GPR40: high apparent constitutive activity in guanosine 5'-O-(3-[35S]thio)triphosphate binding studies reflects binding of an endogenous agonist.
Published in: Mol Pharmacol

Ligand: fasiglifam (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pEC50
Reference (Journal): Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial.
Published in: Diabetes Obes Metab

Ligand: fasiglifam (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pEC50
Reference (Journal): TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats.
Published in: J Pharmacol Exp Ther

Ligand: fasiglifam (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pEC50
Reference (Journal): Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.
Published in: ACS Med Chem Lett

Ligand: fasiglifam (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pEC50
Reference (Journal): High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875.
Published in: Nature

Ligand: docosahexaenoic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.
Published in: Nature

Ligand: docosahexaenoic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids.
Published in: J Biol Chem

Ligand: compound B [PMID:18477808] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pEC50
Reference (Journal): Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice.
Published in: Diabetes

Ligand: compound 4 [PMID: 27074625] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Journal): Development and Characterization of a Potent Free Fatty Acid Receptor 1 (FFA1) Fluorescent Tracer.
Published in: J Med Chem

Ligand: AMG-837 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.5 pEC50
Reference (Journal): Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor.
Published in: Mol Pharmacol

Ligand: α-linolenic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.
Published in: Nature

Ligand: α-linolenic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids.
Published in: J Biol Chem

Ligand: α-linolenic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs.
Published in: Biochem Biophys Res Commun