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

Ligand: PGD2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pIC50
Reference (Journal): Chemoattractant receptor-homologous molecule expressed on Th2 cells activation in vivo increases blood leukocyte counts and its blockade abrogates 13,14-dihydro-15-keto-prostaglandin D2-induced eosinophilia in rats.
Published in: J Pharmacol Exp Ther

Ligand: PGD2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2.
Published in: J Biol Chem

Ligand: PGD3 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Expression and molecular pharmacology of the mouse CRTH2 receptor.
Published in: J Pharmacol Exp Ther

Ligand: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity: 5.5 pKi
Reference (Journal): Expression and molecular pharmacology of the mouse CRTH2 receptor.
Published in: J Pharmacol Exp Ther

Ligand: PGE2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity: 5.3 pKi
Reference (Journal): Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2.
Published in: Br J Pharmacol

Ligand: PGF2α (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2.
Published in: Br J Pharmacol

Ligand: PGF2α (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Expression and molecular pharmacology of the mouse CRTH2 receptor.
Published in: J Pharmacol Exp Ther

Ligand: PGJ2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Expression and molecular pharmacology of the mouse CRTH2 receptor.
Published in: J Pharmacol Exp Ther

Ligand: PGJ2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2.
Published in: Br J Pharmacol

Ligand: QAV680 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.820000171661377 pKd
Reference (Journal): QAW039, a slowly dissociating CRTh2 antagonist with potential for improved clinical efficacy.
Published in: Eur Respir J

Ligand: ramatroban (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pKi
Reference (Journal): CRTH2-specific binding characteristics of [3H]ramatroban and its effects on PGD2-, 15-deoxy-Delta12, 14-PGJ2- and indomethacin-induced agonist responses.
Published in: Eur J Pharmacol

Ligand: ramatroban (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pIC50
Reference (Journal): Chemoattractant receptor-homologous molecule expressed on Th2 cells activation in vivo increases blood leukocyte counts and its blockade abrogates 13,14-dihydro-15-keto-prostaglandin D2-induced eosinophilia in rats.
Published in: J Pharmacol Exp Ther

Ligand: ramatroban (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2.
Published in: J Biol Chem

Ligand: setipiprant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist.
Published in: J Med Chem

Ligand: [3H]PGD2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2.
Published in: Mol Pharmacol

Ligand: [3H]PGD2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKd
Reference (Journal): Chemoattractant receptor-homologous molecule expressed on Th2 cells activation in vivo increases blood leukocyte counts and its blockade abrogates 13,14-dihydro-15-keto-prostaglandin D2-induced eosinophilia in rats.
Published in: J Pharmacol Exp Ther

Ligand: [3H]PGD2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Chemoattractant receptor-homologous molecule expressed on Th2 cells activation in vivo increases blood leukocyte counts and its blockade abrogates 13,14-dihydro-15-keto-prostaglandin D2-induced eosinophilia in rats.
Published in: J Pharmacol Exp Ther

Ligand: [3H]ramatroban (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKd
Reference (Journal): CRTH2-specific binding characteristics of [3H]ramatroban and its effects on PGD2-, 15-deoxy-Delta12, 14-PGJ2- and indomethacin-induced agonist responses.
Published in: Eur J Pharmacol

Ligand: timapiprant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 7.889999866485596 pKi
Reference (Journal): Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils.
Published in: J Pharmacol Exp Ther

Ligand: timapiprant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pKi
Reference (Journal): Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils.
Published in: J Pharmacol Exp Ther

Ligand: TM30089 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.920000076293945 pIC50
Reference (Journal): Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
Published in: J Med Chem

Ligand: TM30089 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.220000267028809 pKi
Reference (Journal): Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
Published in: J Med Chem

Ligand: TM30089 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.920000076293945 pIC50
Reference (Journal): A novel antagonist of CRTH2 blocks eosinophil release from bone marrow, chemotaxis and respiratory burst.
Published in: Allergy

Ligand: U46619 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.5 pKi
Reference (Journal): Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2.
Published in: Br J Pharmacol

Ligand: vidupiprant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
Published in: ACS Med Chem Lett