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

Ligand: 1-OH-PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.7 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: AH23848 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
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: AH23848 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: AH23848 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: AH23848 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: AH23848 (racemic) (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
Published in: Eur J Pharmacol

Ligand: BAY1316957 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Identification of a Benzimidazolecarboxylic Acid Derivative (BAY 1316957) as a Potent and Selective Human Prostaglandin E2 Receptor Subtype 4 (hEP4-R) Antagonist for the Treatment of Endometriosis.
Published in: J Med Chem

Ligand: beraprost (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.139999866485596 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: BGC201531 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): BGC20-1531, a novel, potent and selective prostanoid EP receptor antagonist: a putative new treatment for migraine headache.
Published in: Br J Pharmacol

Ligand: butaprost (free acid form) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.8 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
Median affinity: 4.7 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: carbacyclin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 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: carbacyclin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.6 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: cicaprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 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: CJ-042794 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.51 pKi
Reference (Journal): Effect of prostanoid EP4 receptor antagonist, CJ-042,794, in rat models of pain and inflammation.
Published in: Eur J Pharmacol

Ligand: compound 47 [PMID: 35640059] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Scaffold Hopping Strategy to Identify Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy.
Published in: J Med Chem

Ligand: CP734432 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9 pEC50
Reference (Journal): Ocular pharmacokinetics and hypotensive activity of PF-04475270, an EP4 prostaglandin agonist in preclinical models.
Published in: Exp Eye Res

Ligand: CP734432 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Ocular pharmacokinetics and hypotensive activity of PF-04475270, an EP4 prostaglandin agonist in preclinical models.
Published in: Exp Eye Res

Ligand: CR6086 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.710000038146973 pKd
Reference (Journal): Pharmacological characterisation of CR6086, a potent prostaglandin E<sub>2</sub>receptor 4 antagonist, as a new potential disease-modifying anti-rheumatic drug.
Published in: Arthritis Res Ther

Ligand: CR6086 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.78000020980835 pKi
Reference (Journal): Pharmacological characterisation of CR6086, a potent prostaglandin E<sub>2</sub>receptor 4 antagonist, as a new potential disease-modifying anti-rheumatic drug.
Published in: Arthritis Res Ther

Ligand: CR6086 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.270000457763672 pKd
Reference (Journal): Pharmacological characterisation of CR6086, a potent prostaglandin E<sub>2</sub>receptor 4 antagonist, as a new potential disease-modifying anti-rheumatic drug.
Published in: Arthritis Res Ther

Ligand: CR6086 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.670000076293945 pKd
Reference (Journal): Pharmacological characterisation of CR6086, a potent prostaglandin E<sub>2</sub>receptor 4 antagonist, as a new potential disease-modifying anti-rheumatic drug.
Published in: Arthritis Res Ther

Ligand: enprostil (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 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: ER819762 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 pIC50
Reference (Journal): A novel antagonist of the prostaglandin E(2) EP(4) receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models.
Published in: Br J Pharmacol

Ligand: ER819762 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: 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: evatanepag (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): In vitro pharmacological characterization of CJ-042794, a novel, potent, and selective prostaglandin EP(4) receptor antagonist.
Published in: Life Sci

Ligand: grapiprant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 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: GW 627368 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Piglet saphenous vein contains multiple relaxatory prostanoid receptors: evidence for EP4, EP2, DP and IP receptor subtypes.
Published in: Br J Pharmacol

Ligand: GW 627368 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
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: iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2003), FDA (2004)
Median affinity:  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: iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2003), FDA (2004)
Median affinity: 6.4 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: iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2003), FDA (2004)
Median affinity: 5.6 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:  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:  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