Target family: Lysophospholipid (LPA) receptors (type: gpcr)
Target: LPA<sub>3</sub> receptor

Ligand: 2-oleoyl-LPA (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8 pEC50
Reference (Journal): Lysophosphatidic acid (LPA) receptors of the EDG family are differentially activated by LPA species. Structure-activity relationship of cloned LPA receptors.
Published in: FEBS Lett

Ligand: alkyl OMPT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.21 pEC50
Reference (Journal): Phosphorothioate analogues of alkyl lysophosphatidic acid as LPA3 receptor-selective agonists.
Published in: ChemMedChem

Ligand: α-fluoromethylenephosphonate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.3 pEC50
Reference (Journal): Structure-activity relationships of fluorinated lysophosphatidic acid analogues.
Published in: J Med Chem

Ligand: AM966 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model.
Published in: Br J Pharmacol

Ligand: AM966 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model.
Published in: Br J Pharmacol

Ligand: compound 12 [PMID: 19800804] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.519999980926514 pIC50
Reference (Journal): Structure-based drug design identifies novel LPA3 antagonists.
Published in: Bioorg Med Chem

Ligand: CpX (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pEC50
Reference (Journal): Lysophosphatidic Acid Receptor Agonism: Discovery of Potent Nonlipid Benzofuran Ethanolamine Structures.
Published in: J Pharmacol Exp Ther

Ligand: CpY (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pEC50
Reference (Journal): Lysophosphatidic Acid Receptor Agonism: Discovery of Potent Nonlipid Benzofuran Ethanolamine Structures.
Published in: J Pharmacol Exp Ther

Ligand: dioctanoylglycerol pyrophosphate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.
Published in: Mol Pharmacol

Ligand: dioctanoylglycerol pyrophosphate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.96999979019165 pIC50
Reference (Journal): Short-chain phosphatidates are subtype-selective antagonists of lysophosphatidic acid receptors.
Published in: Mol Pharmacol

Ligand: dioctanoylglycerol pyrophosphate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Short-chain phosphatidates are subtype-selective antagonists of lysophosphatidic acid receptors.
Published in: Mol Pharmacol

Ligand: dodecylphosphate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.05 pKi
Reference (Journal): Fatty alcohol phosphates are subtype-selective agonists and antagonists of lysophosphatidic acid receptors.
Published in: Mol Pharmacol

Ligand: dodecyl-thiophosphate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pKi
Reference (Journal): Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activators of PPARgamma, and inhibitors of autotaxin.
Published in: J Med Chem

Ligand: farnesyl diphosphate (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.81 pKd
Reference (Journal): Farnesyl phosphates are endogenous ligands of lysophosphatidic acid receptors: inhibition of LPA GPCR and activation of PPARs.
Published in: Biochim Biophys Acta

Ligand: farnesyl diphosphate (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.809999942779541 pIC50
Reference (Journal): Unique ligand selectivity of the GPR92/LPA5 lysophosphatidate receptor indicates role in human platelet activation.
Published in: J Biol Chem

Ligand: farnesyl monophosphate (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): Unique ligand selectivity of the GPR92/LPA5 lysophosphatidate receptor indicates role in human platelet activation.
Published in: J Biol Chem

Ligand: farnesyl monophosphate (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.32 pKd
Reference (Journal): Farnesyl phosphates are endogenous ligands of lysophosphatidic acid receptors: inhibition of LPA GPCR and activation of PPARs.
Published in: Biochim Biophys Acta

Ligand: H2L5186303 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.909999847412109 pIC50
Reference (Journal): Structure-based drug design identifies novel LPA3 antagonists.
Published in: Bioorg Med Chem

Ligand: Ki16425 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.440000057220459 pKi
Reference (Journal): Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.
Published in: Mol Pharmacol

Ligand: LPA (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.69 pKd
Reference (Journal): Molecular cloning and characterization of a novel human G-protein-coupled receptor, EDG7, for lysophosphatidic acid.
Published in: J Biol Chem

Ligand: LPA (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pEC50
Reference (Journal): LPA and its analogs-attractive tools for elucidation of LPA biology and drug development.
Published in: Curr Med Chem

Ligand: NAEPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): LPA and its analogs-attractive tools for elucidation of LPA biology and drug development.
Published in: Curr Med Chem

Ligand: oleoyl-thiophosphate (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6.260000228881836 pEC50
Reference (Journal): Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activators of PPARgamma, and inhibitors of autotaxin.
Published in: J Med Chem

Ligand: OMPT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.17 pEC50
Reference (Journal): Identification of a phosphothionate analogue of lysophosphatidic acid (LPA) as a selective agonist of the LPA3 receptor.
Published in: J Biol Chem

Ligand: T13 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pEC50
Reference (Journal): LPA and its analogs-attractive tools for elucidation of LPA biology and drug development.
Published in: Curr Med Chem

Ligand: VPC12249 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): LPA and its analogs-attractive tools for elucidation of LPA biology and drug development.
Published in: Curr Med Chem

Ligand: VPC12249 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.369999885559082 pKi
Reference (Journal): Activity of 2-substituted lysophosphatidic acid (LPA) analogs at LPA receptors: discovery of a LPA1/LPA3 receptor antagonist.
Published in: Mol Pharmacol

Ligand: VPC12249 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Activity of 2-substituted lysophosphatidic acid (LPA) analogs at LPA receptors: discovery of a LPA1/LPA3 receptor antagonist.
Published in: Mol Pharmacol

Ligand: VPC32179 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist.
Published in: Bioorg Med Chem Lett

Ligand: VPC32183 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.76 pIC50
Reference (Journal): Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist.
Published in: Bioorg Med Chem Lett

Ligand: VPC32183 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.760000228881836 pIC50
Reference (Journal): Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist.
Published in: Bioorg Med Chem Lett