Target family: Prostanoid receptors (type: gpcr)
Target: IP receptor

Ligand: AFP-07 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): 7,7-Difluoroprostacyclin derivative, AFP-07, a highly selective and potent agonist for the prostacyclin receptor.
Published in: Prostaglandins

Ligand: BAY-73-1449 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10 pIC50
Reference (Journal): Vascular actions of the prostacyclin receptor antagonist BAY 73-1449 in the portal hypertensive rat.
Published in: Eur J Pharmacol

Ligand: beraprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 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: beraprost (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.409999847412109 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: beraprost (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 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: BMY 45778 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Relaxant actions of nonprostanoid prostacyclin mimetics on human pulmonary artery.
Published in: J Cardiovasc Pharmacol

Ligand: butaprost (free acid form) (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.3 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: carbacyclin (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: carbacyclin (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 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: CAY10441 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pA2
Reference (Journal): Glial cells isolated from dorsal root ganglia express prostaglandin E(2) (EP(4)) and prostacyclin (IP) receptors.
Published in: Eur J Pharmacol

Ligand: CAY10441 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pA2
Reference (Journal): RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists.
Published in: Br J Pharmacol

Ligand: CAY10441 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists.
Published in: Br J Pharmacol

Ligand: cicaprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: 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: cicaprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 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: EP 157 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Prostaglandin endoperoxide analogues which are both thromboxane receptor antagonists and prostacyclin mimetics.
Published in: Br J Pharmacol

Ligand: esuberaprost (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 pKd
Reference (Journal): Specific binding of the new stable epoprostenol analogue beraprost sodium to prostacyclin receptors on human and rat platelets.
Published in: Arzneimittelforschung

Ligand: FK-788 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.05 pKi
Reference (Journal): Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.
Published in: Bioorg Med Chem Lett

Ligand: FR181157 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.27 pKi
Reference (Journal): Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
Published in: Bioorg Med Chem Lett

Ligand: iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2003), FDA (2004)
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: iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2003), FDA (2004)
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: iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2003), FDA (2004)
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: isocarbacyclin (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: MRE-269 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pKi
Reference (Journal): A comparative study of PGI2 mimetics used clinically on the vasorelaxation of human pulmonary arteries and veins, role of the DP-receptor.
Published in: Prostaglandins Other Lipid Mediat

Ligand: MRE-269 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 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: MRE-269 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.659999847412109 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-1301 (Synthetic organic)
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

Ligand: PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Median affinity: 7.5 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: PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity:  pKi
Reference (Journal): Design and synthesis of a highly selective EP4-receptor agonist. Part 1: 3,7-dithiaPG derivatives with high selectivity.
Published in: Bioorg Med Chem Lett

Ligand: PGE1 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity:  pKi
Reference (Journal): New insights into human prostacyclin receptor structure and function through natural and synthetic mutations of transmembrane charged residues.
Published in: Br J Pharmacol

Ligand: PGI2 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: no
Median affinity: 7.800000190734863 pKi
Reference (Journal): Selective binding site for [3H]prostacyclin on platelets.
Published in: J Clin Invest

Ligand: RO3244794 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKB
Reference (Journal): Evidence for a second receptor for prostacyclin on human airway epithelial cells that mediates inhibition of CXCL9 and CXCL10 release.
Published in: Mol Pharmacol

Ligand: RO3244794 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKB
Reference (Journal): Selective prostacyclin receptor agonism augments glucocorticoid-induced gene expression in human bronchial epithelial cells.
Published in: J Immunol

Ligand: RO3244794 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists.
Published in: Br J Pharmacol

Ligand: RO3244794 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pA2
Reference (Journal): RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists.
Published in: Br J Pharmacol

Ligand: selexipag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: no
Median affinity: 6.590000152587891 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: selexipag (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: no
Median affinity: 5.679999828338623 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: [3H]iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 pKd
Reference (Journal): cDNA cloning of a mouse prostacyclin receptor. Multiple signaling pathways and expression in thymic medulla.
Published in: J Biol Chem

Ligand: [3H]iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: 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]iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: 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]iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pKd
Reference (Journal): Cloning and expression of a cDNA for rat prostacyclin receptor.
Published in: Biochim Biophys Acta

Ligand: [3H]iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: 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]iloprost (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Cloning and expression of a cDNA for the human prostanoid IP receptor.
Published in: J Biol Chem

Ligand: taprostene (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.11 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: taprostene (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): Relaxant actions of nonprostanoid prostacyclin mimetics on human pulmonary artery.
Published in: J Cardiovasc Pharmacol

Ligand: TEI-9063 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Relaxant actions of nonprostanoid prostacyclin mimetics on human pulmonary artery.
Published in: J Cardiovasc Pharmacol

Ligand: TG6-129 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pKB
Reference (Journal): Discovery and characterization of carbamothioylacrylamides as EP2 selective antagonists.
Published in: ACS Med Chem Lett

Ligand: treprostinil (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2020)
Primary target: yes
Median affinity: 8.720000267028809 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: Full agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2020)
Primary target: yes
Median affinity: 8.720000267028809 pEC50
Reference (Journal): Inhaled Treprostinil in Pulmonary Hypertension Due to Interstitial Lung Disease.
Published in: N Engl J Med

Ligand: treprostinil (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (2002), EMA (2020)
Primary target: yes
Median affinity: 7.489999771118164 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: 4.2 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