Target family: GPR18, GPR55 and GPR119 (type: gpcr)
Target: <i>GPR119</i>

Ligand: 1-oleoyl glycerol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): 2-Oleoyl glycerol is a GPR119 agonist and signals GLP-1 release in humans.
Published in: J Clin Endocrinol Metab

Ligand: 1-palmitoyl-lysophosphatidylcholine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.8 pEC50
Reference (Journal): Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor.
Published in: Biochem Biophys Res Commun

Ligand: 1-stearoyl-lysophosphatidylcholine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor.
Published in: Biochem Biophys Res Commun

Ligand: 2-oleoyl glycerol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): 2-Oleoyl glycerol is a GPR119 agonist and signals GLP-1 release in humans.
Published in: J Clin Endocrinol Metab

Ligand: APD668 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pEC50
Reference (Journal): Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Published in: Bioorg Med Chem Lett

Ligand: APD668 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.569999694824219 pEC50
Reference (Journal): Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Published in: Bioorg Med Chem Lett

Ligand: AR231453 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.2 pEC50
Reference (Journal): A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release.
Published in: Endocrinology

Ligand: AS1269574 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pEC50
Reference (Journal): Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion.
Published in: Biochem Biophys Res Commun

Ligand: AS1535907 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The role of small molecule GPR119 agonist, AS1535907, in glucose-stimulated insulin secretion and pancreatic β-cell function.
Published in: Diabetes Obes Metab

Ligand: AS1535907 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Synthesis and structure-activity relationship of 4-amino-2-phenylpyrimidine derivatives as a series of novel GPR119 agonists.
Published in: Bioorg Med Chem

Ligand: AS1535907 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Novel GPR119 agonist AS1535907 contributes to first-phase insulin secretion in rat perfused pancreas and diabetic db/db mice.
Published in: Biochem Biophys Res Commun

Ligand: AS1907417 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6 pEC50
Reference (Journal): AS1907417, a novel GPR119 agonist, as an insulinotropic and β-cell preservative agent for the treatment of type 2 diabetes.
Published in: Biochem Biophys Res Commun

Ligand: compound 1 [PMID: 21273063] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.44 pEC50
Reference (Journal): Design of potent and selective GPR119 agonists for type II diabetes.
Published in: Bioorg Med Chem Lett

Ligand: compound 1 [PMID: 21939274] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.1 pEC50
Reference (Journal): Oxidative metabolism of a quinoxaline derivative by xanthine oxidase in rodent plasma.
Published in: Chem Res Toxicol

Ligand: compound 20f [PMID: 21536438] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.74 pEC50
Reference (Journal): Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes.
Published in: Bioorg Med Chem Lett

Ligand: compound 23 [PMID: 21444206] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.22 pEC50
Reference (Journal): Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Published in: Bioorg Med Chem Lett

Ligand: compound 29a [PMID: 21444206] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.15 pEC50
Reference (Journal): Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Published in: Bioorg Med Chem Lett

Ligand: compound 2 [PMID: 21939274] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.77 pEC50
Reference (Journal): Oxidative metabolism of a quinoxaline derivative by xanthine oxidase in rodent plasma.
Published in: Chem Res Toxicol

Ligand: compound 36j [PMID: 21536438] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.52 pEC50
Reference (Journal): Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes.
Published in: Bioorg Med Chem Lett

Ligand: compound 36 [PMID: 21273063] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.72 pEC50
Reference (Journal): Design of potent and selective GPR119 agonists for type II diabetes.
Published in: Bioorg Med Chem Lett

Ligand: compound 3a [PMID: 21444206] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.96 pEC50
Reference (Journal): Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Published in: Bioorg Med Chem Lett

Ligand: compound 3j [PMID: 21444206] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.05 pEC50
Reference (Journal): Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Published in: Bioorg Med Chem Lett

Ligand: compound 3 [PMID: 21310611] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.1 pEC50
Reference (Journal): Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.
Published in: Bioorg Med Chem Lett

Ligand: compound 42 [PMID: 22545772] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.1 pEC50
Reference (Journal): Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.
Published in: J Med Chem

Ligand: compound 58 [PMID: 21273063] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.4 pEC50
Reference (Journal): Design of potent and selective GPR119 agonists for type II diabetes.
Published in: Bioorg Med Chem Lett

Ligand: compound 8g [PMID: 21444206] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.3 pEC50
Reference (Journal): Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control.
Published in: Bioorg Med Chem Lett

Ligand: DS-8500a (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.289999961853027 pEC50
Reference (Journal): DS-8500a, an Orally Available G Protein-Coupled Receptor 119 Agonist, Upregulates Glucagon-Like Peptide-1 and Enhances Glucose-Dependent Insulin Secretion and Improves Glucose Homeostasis in Type 2 Diabetic Rats.
Published in: J Pharmacol Exp Ther

Ligand: JNJ-38431055 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.3 pEC50
Reference (Journal): Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile.
Published in: Bioorg Med Chem Lett

Ligand: lysophosphatidylethanolamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.2 pEC50
Reference (Journal): Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor.
Published in: Biochem Biophys Res Commun

Ligand: lysophosphatidylinositol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.2 pEC50
Reference (Journal): Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor.
Published in: Biochem Biophys Res Commun

Ligand: MBX-2982 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
Published in: Bioorg Med Chem Lett

Ligand: N-oleoyldopamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.5 pEC50
Reference (Journal): N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.
Published in: Mol Endocrinol

Ligand: N-oleoylethanolamide (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.
Published in: Mol Endocrinol

Ligand: N-oleoylethanolamide (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents.
Published in: Cell Metab

Ligand: N-oleoylethanolamide (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors.
Published in: J Biomol Screen

Ligand: N-palmitoylethanolamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: oleoyl-lysophosphatidylcholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.8 pEC50
Reference (Journal): Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor.
Published in: Biochem Biophys Res Commun

Ligand: olvanil (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.1 pEC50
Reference (Journal): N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.
Published in: Mol Endocrinol

Ligand: PSN375963 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pEC50
Reference (Journal): Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents.
Published in: Cell Metab

Ligand: PSN632408 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents.
Published in: Cell Metab

Ligand: (R)-N-oleoyltyrosinol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.3 pEC50
Reference (Journal): N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.
Published in: Mol Endocrinol

Ligand: SEA (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: (S)-N-oleoyltyrosinol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.2 pEC50
Reference (Journal): N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119.
Published in: Mol Endocrinol

Ligand: YH18968 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.550000190734863 pEC50
Reference (Journal): YH18968, a Novel 1,2,4-Triazolone G-Protein Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes Mellitus.
Published in: Biomol Ther (Seoul)