Target family: P2Y receptors (type: gpcr)
Target: P2Y<sub>1</sub> receptor

Ligand: 2,2'-pyridylisatogen tosylate (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): 2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding.
Published in: Biochem Pharmacol

Ligand: 2',3'-ddATP (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor.
Published in: Br J Pharmacol

Ligand: 2-chloroadenosine-5-triphosphate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): ATP derivatives are antagonists of the P2Y1 receptor: similarities to the platelet ADP receptor.
Published in: Mol Pharmacol

Ligand: 2-Cl-ADP(α-BH3) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pEC50
Reference (Journal): Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists.
Published in: J Med Chem

Ligand: 2MeSADP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor.
Published in: Br J Pharmacol

Ligand: 2MeSADP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.
Published in: Mol Pharmacol

Ligand: 2MeSATP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor.
Published in: Br J Pharmacol

Ligand: 2MeSATP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.
Published in: Mol Pharmacol

Ligand: 2MeSATP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pKi
Reference (Journal): ATP derivatives are antagonists of the P2Y1 receptor: similarities to the platelet ADP receptor.
Published in: Mol Pharmacol

Ligand: A2P5P (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pEC50
Reference (Journal): Identification of competitive antagonists of the P2Y1 receptor.
Published in: Mol Pharmacol

Ligand: adenosine-3'-5'-bisphosphate (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pEC50
Reference (Journal): Identification of competitive antagonists of the P2Y1 receptor.
Published in: Mol Pharmacol

Ligand: ADP (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor.
Published in: Br J Pharmacol

Ligand: ADP (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.
Published in: Mol Pharmacol

Ligand: ADPβS (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
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: Ap3a (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.21999979019165 pEC50
Reference (Journal): Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors.
Published in: J Med Chem

Ligand: Ap5a (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors.
Published in: J Med Chem

Ligand: ATP (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor.
Published in: Br J Pharmacol

Ligand: ATP (Metabolite)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.
Published in: Mol Pharmacol

Ligand: ATP (Metabolite)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.8 pKi
Reference (Journal): ATP derivatives are antagonists of the P2Y1 receptor: similarities to the platelet ADP receptor.
Published in: Mol Pharmacol

Ligand: ATPγS (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor.
Published in: Br J Pharmacol

Ligand: BMS compound 16 [PMID:23368907] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pKi
Reference (Journal): Two disparate ligand-binding sites in the human P2Y1 receptor.
Published in: Nature

Ligand: BMS compound 4c (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): New azole antagonists with high affinity for the P2Y1 receptor.
Published in: Bioorg Med Chem Lett

Ligand: compound 3a [PMID: 22873688] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pEC50
Reference (Journal): Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.
Published in: J Med Chem

Ligand: dATPαS (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): An examination of deoxyadenosine 5'(alpha-thio)triphosphate as a ligand to define P2Y receptors and its selectivity as a low potency partial agonist of the P2Y1 receptor.
Published in: Br J Pharmacol

Ligand: GlaxoSmithKline compound 5h [PMID:20542694] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.85 pKi
Reference (Journal): Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: GlaxoSmithKline compound 6i [PMID:18926700] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: MRS2179 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.
Published in: Mol Pharmacol

Ligand: MRS2179 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of competitive antagonists of the P2Y1 receptor.
Published in: Mol Pharmacol

Ligand: MRS2279 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.
Published in: Mol Pharmacol

Ligand: MRS2298 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor.
Published in: Biochem Pharmacol

Ligand: MRS2365 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pEC50
Reference (Journal): Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog.
Published in: J Pharmacol Exp Ther

Ligand: MRS2496 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor.
Published in: Biochem Pharmacol

Ligand: MRS2500 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor.
Published in: Biochem Pharmacol

Ligand: MRS2500 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): 2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.
Published in: J Med Chem

Ligand: MRS2950 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): Virtual screening leads to the discovery of novel non-nucleotide P2Y₁ receptor antagonists.
Published in: Bioorg Med Chem

Ligand: Pfizer compound 11 [PMID:18445527] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): P2Y1 receptor antagonists as novel antithrombotic agents.
Published in: Bioorg Med Chem Lett

Ligand: Pfizer compound 67 [PMID:18445527] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): P2Y1 receptor antagonists as novel antithrombotic agents.
Published in: Bioorg Med Chem Lett

Ligand: PPADS (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pKi
Reference (Journal): Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist.
Published in: Mol Pharmacol