Target family: Prostanoid receptors (type: gpcr)
Target: EP<sub>2</sub> receptor

Ligand: U46619 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.9 pKi
Reference (Journal): The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
Published in: Biochim Biophys Acta

Ligand: U46619 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: treprostinil (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2020)
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Assessing the agonist profiles of the prostacyclin analogues treprostinil and naxaprostene, particularly their DP₁ activity.
Published in: Prostaglandins Leukot Essent Fatty Acids

Ligand: treprostinil (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2020)
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist.
Published in: Biochem Pharmacol

Ligand: TG8-260 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKB
Reference (Journal): Temporal Expression of Neuroinflammatory and Oxidative Stress Markers and Prostaglandin E2 Receptor EP2 Antagonist Effect in a Rat Model of Epileptogenesis.
Published in: ACS Pharmacol Transl Sci

Ligand: TG8-260 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKB
Reference (Journal): Second-Generation Prostaglandin Receptor EP2 Antagonist, TG8-260, with High Potency, Selectivity, Oral Bioavailability, and Anti-Inflammatory Properties.
Published in: ACS Pharmacol Transl Sci

Ligand: TG7-171 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.569999694824219 pKB
Reference (Journal): Development of second generation EP2 antagonists with high selectivity.
Published in: Eur J Med Chem

Ligand: TG6-129 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.0600004196167 pKB
Reference (Journal): Discovery and characterization of carbamothioylacrylamides as EP2 selective antagonists.
Published in: ACS Med Chem Lett

Ligand: TG4-155 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.619999885559082 pKB
Reference (Journal): Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2.
Published in: Proc Natl Acad Sci USA

Ligand: TG11-77 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.010000228881836 pKB
Reference (Journal): Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist for Use in Central Nervous System Disease Models.
Published in: J Med Chem

Ligand: taprenepag (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.
Published in: Exp Eye Res

Ligand: taprenepag (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pIC50
Reference (Journal): Effect of PF-04217329 a prodrug of a selective prostaglandin EP(2) agonist on intraocular pressure in preclinical models of glaucoma.
Published in: Exp Eye Res

Ligand: [3H]PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist.
Published in: Br J Pharmacol

Ligand: [3H]PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pKd
Reference (Journal): A cluster of aromatic amino acids in the i2 loop plays a key role for Gs coupling in prostaglandin EP2 and EP3 receptors.
Published in: J Biol Chem

Ligand: [3H]PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
Published in: Biochim Biophys Acta

Ligand: [3H]PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: [3H]PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Molecular cloning and expression of a rat prostaglandin E2 receptor of the EP2 subtype.
Published in: Prostaglandins

Ligand: rivenprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Stimulation of bone formation and prevention of bone loss by prostaglandin E EP4 receptor activation.
Published in: Proc Natl Acad Sci USA

Ligand: PGN-9856 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): The affinity, intrinsic activity and selectivity of a structurally novel EP<sub>2</sub> receptor agonist at human prostanoid receptors.
Published in: Br J Pharmacol

Ligand: PGF2α (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
Published in: Biochim Biophys Acta

Ligand: PGF2α (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: PGF2α (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Importance of the extracellular domain for prostaglandin EP(2) receptor function.
Published in: Mol Pharmacol

Ligand: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
Published in: Biochim Biophys Acta

Ligand: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity:  pKi
Reference (Journal): Functional domains essential for Gs activity in prostaglandin EP2 and EP3 receptors.
Published in: Life Sci