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

Ligand: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity:  pKi
Reference (Journal): The role of prostaglandin E receptor subtypes (EP1, EP2, EP3, and EP4) in bone resorption: an analysis using specific agonists for the respective EPs.
Published in: Endocrinology

Ligand: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
Median affinity:  pKi
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: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: yes
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)
Median affinity:  pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: yes
Median affinity: 8.039999961853027 pKi
Reference (Journal): Cloning, functional expression, and characterization of the human prostaglandin E2 receptor EP2 subtype.
Published in: J Biol Chem

Ligand: PGD2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Importance of the extracellular domain for prostaglandin EP(2) receptor function.
Published in: Mol Pharmacol

Ligand: PGD2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: PF-04852946 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Characterization of the EP receptor subtype that mediates the inhibitory effects of prostaglandin E2 on IgE-dependent secretion from human lung mast cells.
Published in: Clin Exp Allergy

Ligand: PF-04418948 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKB
Reference (Journal): In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP₂ receptor antagonist.
Published in: Br J Pharmacol

Ligand: PF-04418948 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKB
Reference (Journal): Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor.
Published in: Br J Pharmacol

Ligand: PF-04418948 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.32 pKB
Reference (Journal): Selectivity profiling of the novel EP2 receptor antagonist, PF-04418948, in functional bioassay systems: atypical affinity at the guinea pig EP2 receptor.
Published in: Br J Pharmacol

Ligand: ONO-AE-248 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.4 pKi
Reference (Journal): The role of prostaglandin E receptor subtypes (EP1, EP2, EP3, and EP4) in bone resorption: an analysis using specific agonists for the respective EPs.
Published in: Endocrinology

Ligand: ONO-AE1-329 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.7 pKi
Reference (Journal): The role of prostaglandin E receptor subtypes (EP1, EP2, EP3, and EP4) in bone resorption: an analysis using specific agonists for the respective EPs.
Published in: Endocrinology

Ligand: ONO-AE1-259 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): The role of prostaglandin E receptor subtypes (EP1, EP2, EP3, and EP4) in bone resorption: an analysis using specific agonists for the respective EPs.
Published in: Endocrinology

Ligand: omidenepag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2022)
Primary target: no
Median affinity: 8.4399995803833 pKi
Reference (Journal): Pharmacologic Characterization of Omidenepag Isopropyl, a Novel Selective EP2 Receptor Agonist, as an Ocular Hypotensive Agent.
Published in: Invest Ophthalmol Vis Sci

Ligand: MRE-269 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.239999771118164 pKi
Reference (Journal): 2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug.
Published in: J Pharmacol Exp Ther

Ligand: misoprostol (methyl ester) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity: 5 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: misoprostol (free acid form) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 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: MB-28767 (Synthetic organic)
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: MB-28767 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: MB-28767 (Synthetic organic)
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: isocarbacyclin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2003), FDA (2004)
Median affinity: 5.7 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: iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2003), FDA (2004)
Median affinity: 5.9 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2003), FDA (2004)
Median affinity: 5.8 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: evatanepag (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation.
Published in: Bioorg Med Chem Lett

Ligand: evatanepag (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pEC50
Reference (Journal): Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation.
Published in: Bioorg Med Chem Lett

Ligand: compound 1 [PMID: 20080612] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Neuroprotection by selective allosteric potentiators of the EP2 prostaglandin receptor.
Published in: Proc Natl Acad Sci USA

Ligand: cicaprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: carbacyclin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: carbacyclin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 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: butaprost (free acid form) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Importance of the extracellular domain for prostaglandin EP(2) receptor function.
Published in: Mol Pharmacol

Ligand: butaprost (free acid form) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: butaprost (free acid form) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: 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: AH6809 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: AH6809 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: AH6809 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.9 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: AH13205 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: AH13205 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Importance of the extracellular domain for prostaglandin EP(2) receptor function.
Published in: Mol Pharmacol

Ligand: 19(R)-OH-PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Cloning of a novel human prostaglandin receptor with characteristics of the pharmacologically defined EP2 subtype.
Published in: Mol Pharmacol

Ligand: 19(R)-OH-PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: 17-phenyl-ω-trinor-PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: 16,16-dimethyl-PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: 11-deoxy-PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: 11-deoxy-PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol