Target family: Lysophospholipid (LPA) receptors (type: gpcr)
Target: LPA<sub>1</sub> receptor

Ligand: 2-oleoyl-LPA (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 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: ACT-1016-0707 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.539999961853027 pIC50
Reference (Journal): Discovery of the Novel, Orally Active, and Selective LPA1 Receptor Antagonist ACT-1016-0707 as a Preclinical Candidate for the Treatment of Fibrotic Diseases.
Published in: J Med Chem

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

Ligand: AM095 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist.
Published in: J Pharmacol Exp Ther

Ligand: AM095 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.110000133514404 pIC50
Reference (Journal): Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist.
Published in: J Pharmacol Exp Ther

Ligand: AM966 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist.
Published in: J Pharmacol Exp Ther

Ligand: AM966 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pEC50
Reference (Journal): A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model.
Published in: Br J Pharmacol

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Primary target: no
Median affinity: 6.21999979019165 pIC50
Reference (Journal): Antidepressants induce profibrotic responses via the lysophosphatidic acid receptor LPA<sub>1</sub>.
Published in: Eur J Pharmacol

Ligand: anti-BrP-LPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.679999828338623 pIC50
Reference (Journal): Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo.
Published in: Cancer Res

Ligand: anti-BrP-LPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.119999885559082 pKi
Reference (Journal): Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo.
Published in: Cancer Res

Ligand: BMS-986020 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.899999618530273 pIC50

Ligand: BMS-986278 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.15999984741211 pKB
Reference (Journal): Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA<sub>1</sub>) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases.
Published in: J Med Chem

Ligand: BrP-LPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.340000152587891 pIC50
Reference (Journal): Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo.
Published in: Cancer Res

Ligand: BrP-LPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.090000152587891 pKi
Reference (Journal): Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo.
Published in: Cancer Res

Ligand: CpX (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pEC50
Reference (Journal): Lysophosphatidic Acid Receptor Agonism: Discovery of Potent Nonlipid Benzofuran Ethanolamine Structures.
Published in: J Pharmacol Exp Ther

Ligand: CpX (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKi
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: 6.300000190734863 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: 8.300000190734863 pKi
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
Primary target: no
Median affinity:  pKi
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
Primary target: no
Median affinity:  pKi
Reference (Journal): LPA and its analogs-attractive tools for elucidation of LPA biology and drug development.
Published in: Curr Med Chem

Ligand: Ki16425 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.
Published in: Mol Pharmacol

Ligand: LPA (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Diversity of lysophosphatidic acid receptor-mediated intracellular calcium signaling in early cortical neurogenesis.
Published in: J Neurosci

Ligand: LPA (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Ventricular zone gene-1 (vzg-1) encodes a lysophosphatidic acid receptor expressed in neurogenic regions of the developing cerebral cortex.
Published in: J Cell Biol

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

Ligand: mianserin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): Antidepressants induce profibrotic responses via the lysophosphatidic acid receptor LPA<sub>1</sub>.
Published in: Eur J Pharmacol

Ligand: NAEPA (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6.710000038146973 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: 6.710000038146973 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: oleoyl-thiophosphate (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6.710000038146973 pEC50
Reference (Journal): Pharmacological tools for lysophospholipid GPCRs: development of agonists and antagonists for LPA and S1P receptors.
Published in: Acta Pharmacol Sin

Ligand: ONO-3080573 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1.
Published in: Cell

Ligand: ONO-7300243 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 6.800000190734863 pIC50
Reference (Journal): Discovery of ONO-7300243 from a Novel Class of Lysophosphatidic Acid Receptor 1 Antagonists: From Hit to Lead.
Published in: ACS Med Chem Lett

Ligand: ONO-9780307 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.570000171661377 pIC50
Reference (Journal): Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1.
Published in: Cell

Ligand: ONO-9910539 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.659999847412109 pIC50
Reference (Journal): Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1.
Published in: Cell

Ligand: SAR100842 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Translational engagement of lysophosphatidic acid receptor 1 in skin fibrosis: from dermal fibroblasts of patients with scleroderma to tight skin 1 mouse.
Published in: Br J Pharmacol

Ligand: syn-BrP-LPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.559999942779541 pKi
Reference (Journal): Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo.
Published in: Cancer Res

Ligand: syn-BrP-LPA (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.190000057220459 pIC50
Reference (Journal): Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo.
Published in: Cancer Res

Ligand: T13 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): LPA and its analogs-attractive tools for elucidation of LPA biology and drug development.
Published in: Curr Med Chem

Ligand: T13 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): Pharmacological tools for lysophospholipid GPCRs: development of agonists and antagonists for LPA and S1P receptors.
Published in: Acta Pharmacol Sin

Ligand: UCM-05194 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.619999885559082 pEC50
Reference (Journal): A Novel Agonist of the Type 1 Lysophosphatidic Acid Receptor (LPA<sub>1</sub>), UCM-05194, Shows Efficacy in Neuropathic Pain Amelioration.
Published in: J Med Chem

Ligand: UCM-05194 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.710000038146973 pKd
Reference (Journal): A Novel Agonist of the Type 1 Lysophosphatidic Acid Receptor (LPA<sub>1</sub>), UCM-05194, Shows Efficacy in Neuropathic Pain Amelioration.
Published in: J Med Chem

Ligand: VPC12249 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  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: 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: 7.75 pKi
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: 6.960000038146973 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