Target family: P2Y receptors (type: gpcr)
Target: P2Y<sub>12</sub> receptor

Ligand: 2MeSADP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKi
Reference (Journal): Identification of the platelet ADP receptor targeted by antithrombotic drugs.
Published in: Nature

Ligand: 2MeSAMP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor.
Published in: Mol Pharmacol

Ligand: ADP (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pKi
Reference (Journal): Identification of the platelet ADP receptor targeted by antithrombotic drugs.
Published in: Nature

Ligand: ADPβS (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor.
Published in: Mol Pharmacol

Ligand: Ap4A (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Pharmacological characterization of the human P2Y13 receptor.
Published in: Mol Pharmacol

Ligand: AR-C67085 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKd
Reference (Journal): P2X and P2Y nucleotide receptors as targets in cardiovascular disease.
Published in: Future Med Chem

Ligand: ARL66096 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.949999809265137 pIC50
Reference (Journal): Pharmacological profile of the novel P2T-purinoceptor antagonist, FPL 67085 in vitro and in the anaesthetized rat in vivo.
Published in: Br J Pharmacol

Ligand: ARL66096 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.949999809265137 pIC50
Reference (Journal): FPL 66096: a novel, highly potent and selective antagonist at human platelet P2T-purinoceptors.
Published in: Br J Pharmacol

Ligand: AZD1283 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Structure of the human P2Y12 receptor in complex with an antithrombotic drug.
Published in: Nature

Ligand: AZD1283 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): 5-alkyl-1,3-oxazole derivatives of 6-amino-nicotinic acids as alkyl ester bioisosteres are antagonists of the P2Y12 receptor.
Published in: Future Med Chem

Ligand: BX 048 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Novel P2Y12 adenosine diphosphate receptor antagonists for inhibition of platelet aggregation (II): pharmacodynamic and pharmacokinetic characterization.
Published in: Thromb Res

Ligand: BX 667 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Novel P2Y12 adenosine diphosphate receptor antagonists for inhibition of platelet aggregation (II): pharmacodynamic and pharmacokinetic characterization.
Published in: Thromb Res

Ligand: cangrelor (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA & EMA (2015)
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor.
Published in: Mol Pharmacol

Ligand: cangrelor (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA & EMA (2015)
Primary target: yes
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Purine and pyrimidine (P2) receptors as drug targets.
Published in: J Med Chem

Ligand: clopidogrel (active metabolite) (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): P2Y12, a new platelet ADP receptor, target of clopidogrel.
Published in: Semin Vasc Med

Ligand: compound 20o [PMID: 22984835] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.
Published in: J Med Chem

Ligand: compound 4 [PMID: 22984835] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.
Published in: J Med Chem

Ligand: compound 4 [PMID: 23083103] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): Modified diadenosine tetraphosphates with dual specificity for P2Y1 and P2Y12 are potent antagonists of ADP-induced platelet activation.
Published in: J Thromb Haemost

Ligand: compound 58l [PMID: 30843696] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.53000020980835 pIC50
Reference (Journal): Optimization of P2Y<sub>12</sub> Antagonist Ethyl 6-(4-((Benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties.
Published in: J Med Chem

Ligand: INS49266 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.28 pIC50
Reference (Journal): Lipophilic modifications to dinucleoside polyphosphates and nucleotides that confer antagonist properties at the platelet P2Y12 receptor.
Published in: J Med Chem

Ligand: pCMBS (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): P2Y12, a new platelet ADP receptor, target of clopidogrel.
Published in: Semin Vasc Med

Ligand: PSB-0739 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKi
Reference (Journal): High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors.
Published in: J Med Chem

Ligand: PSB-0739 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.8 pA2
Reference (Journal): Interaction of new, very potent non-nucleotide antagonists with Arg256 of the human platelet P2Y12 receptor.
Published in: J Pharmacol Exp Ther

Ligand: R-138727 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Stereoselective inhibition of human platelet aggregation by R-138727, the active metabolite of CS-747 (prasugrel, LY640315), a novel P2Y12 receptor inhibitor.
Published in: Thromb Haemost

Ligand: regrelor (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.95 pIC50
Reference (Journal): Lipophilic modifications to dinucleoside polyphosphates and nucleotides that confer antagonist properties at the platelet P2Y12 receptor.
Published in: J Med Chem

Ligand: [3H]2MeSADP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor.
Published in: Mol Pharmacol

Ligand: [3H]PSB-0413 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Synthesis and preliminary evaluation of [3H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptors.
Published in: Bioorg Med Chem Lett

Ligand: [3H]PSB-0413 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): The platelet P2Y(12) receptor under normal and pathological conditions. Assessment with the radiolabeled selective antagonist [(3)H]PSB-0413.
Published in: Purinergic Signal

Ligand: ticagrelor (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2010), FDA (2011)
Primary target: yes
Median affinity: 8.699999809265137 pKi
Reference (Journal): From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.
Published in: Bioorg Med Chem Lett

Ligand: ticagrelor (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2010), FDA (2011)
Primary target: yes
Median affinity: 8.59000015258789 pKB
Reference (Journal): Competitive mode and site of interaction of ticagrelor at the human platelet P2Y12 -receptor.
Published in: J Thromb Haemost

Ligand: ticagrelor (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2010), FDA (2011)
Primary target: yes
Median affinity: 7.849999904632568 pKi
Reference (Journal): Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone.
Published in: J Med Chem