Target family: Prostanoid receptors (type: gpcr)
Target: EP<sub>4</sub> receptor

Ligand: KMN-159 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.420000076293945 pKi
Reference (Journal): Difluoromethylene at the &#x3b3;-Lactam &#x3b1;-Position Improves 11-Deoxy-8-aza-PGE<sub>1</sub> Series EP<sub>4</sub> Receptor Binding and Activity: 11-Deoxy-10,10-difluoro-8-aza-PGE<sub>1</sub> Analog (KMN-159) as a Potent EP<sub>4</sub> Agonist.
Published in: J Med Chem

Ligand: KMN-159 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.619999885559082 pKi
Reference (Journal): KMN-159, a novel EP<sub>4</sub> receptor selective agonist, stimulates osteoblastic differentiation in cultured whole rat bone marrow.
Published in: Gene

Ligand: L-161,982 (EP4A) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Prostaglandin receptor EP(4) mediates the bone anabolic effects of PGE(2).
Published in: Mol Pharmacol

Ligand: L-161,982 (EP4A) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Prostaglandin receptor EP(4) mediates the bone anabolic effects of PGE(2).
Published in: Mol Pharmacol

Ligand: L-161,982 (EP4A) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery and Synthesis of a Potent, Selective and Orally Bioavailable EP4 Receptor Agonist.
Published in: Heterocycles

Ligand: L902688 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands.
Published in: J Pharmacol Exp Ther

Ligand: L902688 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.420000076293945 pKi
Reference (Journal): Discovery and Synthesis of a Potent, Selective and Orally Bioavailable EP4 Receptor Agonist.
Published in: Heterocycles

Ligand: L902688 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Vasorelaxation induced by prostaglandin E2 in human pulmonary vein: role of the EP4 receptor subtype.
Published in: Br J Pharmacol

Ligand: MB-28767 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 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: 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: MB-28767 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 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: 7.75 pEC50
Reference (Journal): Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands.
Published in: J Pharmacol Exp Ther

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: MF 498 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.15 pKi
Reference (Journal): MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.
Published in: J Pharmacol Exp Ther

Ligand: misoprostol (free acid form) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 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: misoprostol (methyl ester) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity: 5.3 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: MK-2894 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.25 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: MK-2894 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.25 pKi
Reference (Journal): The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
Published in: J Med Chem

Ligand: MK-2894 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.25 pKi
Reference (Journal): MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.
Published in: J Pharmacol Exp Ther

Ligand: MRE-269 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.309999942779541 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: ONO-AE1-329 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8 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
Primary target: no
Median affinity:  pEC50
Reference (Journal): Differential reactivity of human mammary artery and saphenous vein to prostaglandin E(2) : implication for cardiovascular grafts.
Published in: Br J Pharmacol

Ligand: ONO-AE1-329 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Vasorelaxation induced by prostaglandin E2 in human pulmonary vein: role of the EP4 receptor subtype.
Published in: Br J Pharmacol

Ligand: ONO-AE1-437 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pKi
Reference (Journal): Simultaneous stimulation of EP2 and EP4 is essential to the effect of prostaglandin E2 in chondrocyte differentiation.
Published in: Osteoarthr Cartil

Ligand: ONO-AE2-227 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.57 pKi
Reference (Journal): Involvement of prostaglandin E receptor subtype EP(4) in colon carcinogenesis.
Published in: Cancer Res

Ligand: ONO-AE3-208 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): The prostaglandin receptor EP4 suppresses colitis, mucosal damage and CD4 cell activation in the gut.
Published in: J Clin Invest

Ligand: ONO-AE3-208 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi

Ligand: ONO-AE3-240 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.24 pKi
Reference (Journal): Host prostaglandin E(2)-EP3 signaling regulates tumor-associated angiogenesis and tumor growth.
Published in: J Exp Med

Ligand: PGD2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Published in: Br J Pharmacol

Ligand: PGD2 (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: PGD2 (Metabolite)
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: PGD2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.77 pEC50
Reference (Journal): Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands.
Published in: J Pharmacol Exp Ther

Ligand: PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 9.510000228881836 pEC50
Reference (Journal): Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands.
Published in: J Pharmacol Exp Ther

Ligand: PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Published in: Br J Pharmacol

Ligand: PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Median affinity: 9.2 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)
Median affinity: 8.7 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: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity: 9 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: 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: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity: 8.6 pKd
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: 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: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: no
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: no
Median affinity:  pKi
Reference (Journal): CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties.
Published in: J Pharmacol Exp Ther

Ligand: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity: 6.05 pEC50
Reference (Journal): Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands.
Published in: J Pharmacol Exp Ther

Ligand: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Primary target: 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)
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: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Published in: Br J Pharmacol

Ligand: PGF2α (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Published in: Br J Pharmacol

Ligand: PGF2α (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.05 pEC50
Reference (Journal): Functional selectivity of natural and synthetic prostaglandin EP4 receptor ligands.
Published in: J Pharmacol Exp Ther

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: 6.2 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: PGI2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1995)
Median affinity: 5.1 pKi
Reference (Journal): Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Published in: Br J Pharmacol

Ligand: rivenprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 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: [3H]PGE2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
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: [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: 9 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): 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:  pKd
Reference (Journal): Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
Published in: Br J Pharmacol

Ligand: TCS 2510 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.92 pKi
Reference (Journal): Discovery and Synthesis of a Potent, Selective and Orally Bioavailable EP4 Receptor Agonist.
Published in: Heterocycles

Ligand: TG11-77 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.28000020980835 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: TG6-129 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.409999847412109 pKB
Reference (Journal): Discovery and characterization of carbamothioylacrylamides as EP2 selective antagonists.
Published in: ACS Med Chem Lett

Ligand: THG213.29 (Peptide)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5.52 pIC50
Reference (Journal): Restoration of renal function by a novel prostaglandin EP4 receptor-derived peptide in models of acute renal failure.
Published in: Am J Physiol Regul Integr Comp Physiol

Ligand: treprostinil (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2020)
Median affinity: 6.7 pEC50
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: treprostinil (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2020)
Median affinity: 6.1 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: U46619 (Synthetic organic)
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: U46619 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
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