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

Ligand: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor.
Published in: J Biol Chem

Ligand: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of the adenine binding site of the human A1 adenosine receptor.
Published in: J Biol Chem

Ligand: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.17 pKi
Reference (Journal): Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors.
Published in: Pharmacology

Ligand: 2-hexynyl-NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pKi
Reference (Journal): N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands.
Published in: J Med Chem

Ligand: 5-Cl-5-deoxy-(±)-ENBA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.29 pKi
Reference (Journal): N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
Published in: J Med Chem

Ligand: 8-cyclopentyltheophylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors.
Published in: Biochem Pharmacol

Ligand: adenosine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 7.14 pKi
Reference (Journal): Adenosine receptor agonists: from basic medicinal chemistry to clinical development.
Published in: Expert Opin Emerg Drugs

Ligand: adenosine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity: 7 pKi
Reference (Journal): Adenosine receptor agonists: from basic medicinal chemistry to clinical development.
Published in: Expert Opin Emerg Drugs

Ligand: apadenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.11 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: AS100 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS70 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS99 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: ATL802 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.43 pKi
Reference (Journal): Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
Published in: J Med Chem

Ligand: ATL802 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.02 pKi
Reference (Journal): Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
Published in: J Med Chem

Ligand: BAY 60-6583 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion.
Published in: J Mol Cell Cardiol

Ligand: binodenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.32 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: caffeine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no history prior to 1999), EMA (2009)
Median affinity:  pKi
Reference (Journal): Synthesis and structure-activity relationships of deazaxanthines: analogs of potent A1- and A2-adenosine receptor antagonists.
Published in: J Med Chem

Ligand: caffeine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no history prior to 1999), EMA (2009)
Primary target: yes
Median affinity:  pKi
Reference (Journal): 1,3-Dialkylxanthine derivatives having high potency as antagonists at human A2B adenosine receptors.
Published in: Drug Dev Res

Ligand: caffeine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no history prior to 1999), EMA (2009)
Median affinity:  pKi
Reference (Journal): Caffeine analogs: structure-activity relationships at adenosine receptors.
Published in: Pharmacology

Ligand: caffeine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no history prior to 1999), EMA (2009)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Adenosine A1 receptors in human hippocampus: inhibition of [3H]8-cyclopentyl-1,3-dipropylxanthine binding by antagonist drugs.
Published in: Neurosci Lett

Ligand: caffeine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (no history prior to 1999), EMA (2009)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Antinociceptive effects of novel A2B adenosine receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: capadenoson (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 10 pEC50
Reference (Journal): Partial adenosine A1 receptor agonists for cardiovascular therapies.
Published in: Purinergic Signal

Ligand: CCPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A novel A1 adenosine receptor antagonist, L-97-1 [3-[2-(4-aminophenyl)-ethyl]-8-benzyl-7-{2-ethyl-(2-hydroxy-ethyl)-amino]-ethyl}-1-propyl-3,7-dihydro-purine-2,6-dione], reduces allergic responses to house dust mite in an allergic rabbit model of asthma.
Published in: J Pharmacol Exp Ther

Ligand: CCPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: CCPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.89 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.460000038146973 pKi
Reference (Journal): Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.19 pKi
Reference (Journal): A<SUB>2A</SUB> Adenosine receptor antagonists—future drugs for Parkinson’s disease?
Published in: Drugs Future

Ligand: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors.
Published in: Biochem Pharmacol

Ligand: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.74 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: Cl-IB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.66 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: Cl-IB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.46 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: Cl-IB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.55 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: compound 10 [PMID: 31306001] (Synthetic organic)
Interaction type: Agonist
Action: Inverse agonist
Ligand approved: no
Primary target: no
Median affinity: 8.140000343322754 pKi
Reference (Journal): Modifications on the Amino-3,5-dicyanopyridine Core To Obtain Multifaceted Adenosine Receptor Ligands with Antineuropathic Activity.
Published in: J Med Chem

Ligand: CP608,039 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.14 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: CPFPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKi
Reference (Journal): Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging.
Published in: J Med Chem

Ligand: CPFPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging.
Published in: J Med Chem

Ligand: CSC (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.55 pKi
Reference (Journal): Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists.
Published in: J Med Chem

Ligand: CVT-6883 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.71 pKi
Reference (Journal): Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases.
Published in: J Med Chem

Ligand: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor.
Published in: J Biol Chem

Ligand: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist.
Published in: Br J Pharmacol

Ligand: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): 2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors.
Published in: Biochem Pharmacol

Ligand: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors.
Published in: Biochem Pharmacol

Ligand: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A &quot;locked-on,&quot; constitutively active mutant of the adenosine A1 receptor.
Published in: Eur J Pharmacol

Ligand: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of the adenine binding site of the human A1 adenosine receptor.
Published in: J Biol Chem

Ligand: derenofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure.
Published in: Br J Pharmacol

Ligand: derenofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure.
Published in: Br J Pharmacol

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Comparison of A1 adenosine receptors in brain from different species by radioligand binding and photoaffinity labelling.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A &quot;locked-on,&quot; constitutively active mutant of the adenosine A1 receptor.
Published in: Eur J Pharmacol

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of the adenine binding site of the human A1 adenosine receptor.
Published in: J Biol Chem

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
Published in: J Med Chem

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Coupling of a transfected human brain A1 adenosine receptor in CHO-K1 cells to calcium mobilisation via a pertussis toxin-sensitive mechanism.
Published in: Br J Pharmacol

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Improving potency, selectivity, and water solubility of adenosine A1 receptor antagonists: xanthines modified at position 3 and related pyrimido[1,2,3-cd]purinediones.
Published in: ChemMedChem

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A novel A1 adenosine receptor antagonist, L-97-1 [3-[2-(4-aminophenyl)-ethyl]-8-benzyl-7-{2-ethyl-(2-hydroxy-ethyl)-amino]-ethyl}-1-propyl-3,7-dihydro-purine-2,6-dione], reduces allergic responses to house dust mite in an allergic rabbit model of asthma.
Published in: J Pharmacol Exp Ther

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Improving potency, selectivity, and water solubility of adenosine A1 receptor antagonists: xanthines modified at position 3 and related pyrimido[1,2,3-cd]purinediones.
Published in: ChemMedChem

Ligand: DU172 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pKi
Reference (Journal): Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity.
Published in: Cell

Ligand: FK-453 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.74 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: flavanone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.5 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: flavone (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.5 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: FR194921 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors.
Published in: J Pharmacol Sci

Ligand: galangin (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: GR79236 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: GS9667 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.26 pKi
Reference (Journal): A1 adenosine receptor agonists and their potential therapeutic applications.
Published in: Expert Opin Investig Drugs

Ligand: HEMADO (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.48 pKi
Reference (Journal): [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor.
Published in: Eur J Pharmacol

Ligand: HEMADO (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.48 pKi
Reference (Journal): N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands.
Published in: J Med Chem

Ligand: imaradenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pKi
Reference (Journal): Small molecule AZD4635 inhibitor of A 2A R signaling rescues immune cell function including CD103 + dendritic cells enhancing anti-tumor immunity
Published in: J Immunother Cancer

Ligand: (R,S)-PHPNECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands.
Published in: J Med Chem

Ligand: isobutylmethylxanthine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor.
Published in: J Biol Chem

Ligand: istradefylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: Japan (2013), FDA (2019)
Median affinity: 6.08 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.
Published in: Pharmacol Rev

Ligand: istradefylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: Japan (2013), FDA (2019)
Median affinity: 6.64 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.
Published in: Pharmacol Rev

Ligand: KF26777 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.74 pKi
Reference (Journal): KF26777 (2-(4-bromophenyl)-7,8-dihydro-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one dihydrochloride), a new potent and selective adenosine A3 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: L-97-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): A novel A1 adenosine receptor antagonist, L-97-1 [3-[2-(4-aminophenyl)-ethyl]-8-benzyl-7-{2-ethyl-(2-hydroxy-ethyl)-amino]-ethyl}-1-propyl-3,7-dihydro-purine-2,6-dione], reduces allergic responses to house dust mite in an allergic rabbit model of asthma.
Published in: J Pharmacol Exp Ther

Ligand: LAS38096 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.55 pKi
Reference (Journal): Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.
Published in: J Med Chem

Ligand: LAS38096 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.55 pKi
Reference (Journal): Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists.
Published in: Bioorg Med Chem Lett

Ligand: LUF5831 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist.
Published in: Br J Pharmacol

Ligand: LUF5962 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.130000114440918 pIC50
Reference (Journal): A two-state model for the kinetics of competitive radioligand binding.
Published in: Br J Pharmacol

Ligand: LUF5981 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.05 pKi
Reference (Journal): 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Published in: J Med Chem

Ligand: LUF7602 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pKi
Reference (Journal): Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A<sub>3</sub> Receptor.
Published in: J Med Chem

Ligand: mefloquine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1989), UK (1989)
Primary target: no
Median affinity: 6.170000076293945 pKi
Reference (Journal): Discovery of nonxanthine adenosine A2A receptor antagonists for the treatment of Parkinson's disease.
Published in: Neurology

Ligand: morin (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.9 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRE 2029F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: MRE 2029F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRE 3008F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [(3)H]MRE 3008F20: a novel antagonist radioligand for the pharmacological and biochemical characterization of human A(3) adenosine receptors.
Published in: Mol Pharmacol

Ligand: MRE 3008F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: MRE 3008F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: MRS1041 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1042 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1062 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.3 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1065 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.5 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1066 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.4 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1084 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.4 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1086 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.5 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1093 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.7 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1132 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1191 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.4 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: MRS1191 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: MRS1523 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: MRS1523 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.81 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: MRS1754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.77 pKi
Reference (Journal): Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
Published in: J Med Chem

Ligand: MRS1754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.39 pKi
Reference (Journal): Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
Published in: J Med Chem

Ligand: MRS3558 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: MRS3558 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.980000019073486 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: MRS3558 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.59 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: MRS5151 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.83 pKi
Reference (Journal): Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
Published in: Bioorg Med Chem Lett

Ligand: MRS5151 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.98 pKi
Reference (Journal): Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
Published in: Bioorg Med Chem Lett

Ligand: MRS7469 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Design and in Vivo Characterization of A<sub>1</sub> Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series.
Published in: J Med Chem

Ligand: MRS923 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.6 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS928 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MSX-2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Water-soluble phosphate prodrugs of 1-propargyl-8-styrylxanthine derivatives, A(2A)-selective adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MSX-2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.05 pKi
Reference (Journal): Water-soluble phosphate prodrugs of 1-propargyl-8-styrylxanthine derivatives, A(2A)-selective adenosine receptor antagonists.
Published in: J Med Chem

Ligand: N(6)-cyclohexyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.07 pKi
Reference (Journal): Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors.
Published in: Pharmacology

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of the adenine binding site of the human A1 adenosine receptor.
Published in: J Biol Chem

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor.
Published in: J Biol Chem

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Adenosine receptor agonists: from basic medicinal chemistry to clinical development.
Published in: Expert Opin Emerg Drugs

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding.
Published in: J Biol Chem

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.29 pKi
Reference (Journal): Adenosine receptor antagonists: structures and potential therapeutic applications.
Published in: Curr Pharm Des

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): 2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors.
Published in: Biochem Pharmacol

Ligand: neladenoson (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 10 pEC50
Reference (Journal): Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A<sub>1</sub> Receptor Agonist for the Chronic Treatment of Heart Diseases.
Published in: ChemMedChem

Ligand: PD81723 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes.
Published in: Mol Pharmacol

Ligand: PENECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands.
Published in: J Med Chem

Ligand: piclidenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.29 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: preladenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Blocking striatal adenosine A2A receptors: a new strategy for basal ganglia disorders.
Published in: Recent Pat CNS Drug Discov

Ligand: PSB-10 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.77 pKi
Reference (Journal): 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors.
Published in: Bioorg Med Chem

Ligand: PSB-10 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.09 pKi
Reference (Journal): Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
Published in: J Med Chem

Ligand: PSB-11 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.79 pKi
Reference (Journal): 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors.
Published in: Bioorg Med Chem

Ligand: PSB-11 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.36 pKi
Reference (Journal): 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors.
Published in: Bioorg Med Chem

Ligand: PSB1115 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.66 pKi
Reference (Journal): Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors.
Published in: J Med Chem

Ligand: PSB1115 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): 1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.
Published in: J Med Chem

Ligand: PSB36 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.9 pKi
Reference (Journal): Antinociceptive effects of novel A2B adenosine receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: PSB603 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Published in: J Med Chem

Ligand: PSB603 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Published in: J Med Chem

Ligand: regadenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2008), EMA (2010)
Median affinity: 5 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: rolofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
Published in: J Med Chem

Ligand: rolofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
Published in: J Med Chem

Ligand: rolofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Published in: J Med Chem

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding.
Published in: J Biol Chem

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors.
Published in: Biochem Pharmacol

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor.
Published in: J Biol Chem

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.92 pKi
Reference (Journal): Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors.
Published in: Pharmacology

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of the adenine binding site of the human A1 adenosine receptor.
Published in: J Biol Chem

Ligand: sakuranetin (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: SCH442416 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.95 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: SCH 58261 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding.
Published in: J Biol Chem

Ligand: SCH 58261 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: SCH 58261 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: (S)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor.
Published in: J Biol Chem

Ligand: (S)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding.
Published in: J Biol Chem

Ligand: ST-1535 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.14 pKi
Reference (Journal): 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Published in: J Med Chem

Ligand: [3H]CCPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [3H]CCPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Identification of the adenine binding site of the human A1 adenosine receptor.
Published in: J Biol Chem

Ligand: [3H]DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Identification of the adenine binding site of the human A1 adenosine receptor.
Published in: J Biol Chem

Ligand: [3H]DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors.
Published in: Biochem Pharmacol

Ligand: [3H]DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding.
Published in: J Biol Chem

Ligand: [3H]DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [3H]DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Inhibition of human mast cell activation with the novel selective adenosine A(2B) receptor antagonist 3-isobutyl-8-pyrrolidinoxanthine (IPDX)(2).
Published in: Biochem Pharmacol

Ligand: [3H]DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: TCPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.550000190734863 pKi
Reference (Journal): N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.
Published in: J Med Chem

Ligand: tecadenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.1899995803833 pKi
Reference (Journal): Recent developments in adenosine receptor ligands and their potential as novel drugs.
Published in: Biochim Biophys Acta

Ligand: tecadenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.1899995803833 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Median affinity:  pKi
Reference (Journal): Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors.
Published in: J Med Chem

Ligand: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Median affinity:  pKi
Reference (Journal): 1,3-Dialkylxanthine derivatives having high potency as antagonists at human A2B adenosine receptors.
Published in: Drug Dev Res

Ligand: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Median affinity:  pKi
Reference (Journal): Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor.
Published in: J Biol Chem

Ligand: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Median affinity:  pKi
Reference (Journal): Inhibition of human mast cell activation with the novel selective adenosine A(2B) receptor antagonist 3-isobutyl-8-pyrrolidinoxanthine (IPDX)(2).
Published in: Biochem Pharmacol

Ligand: tonapofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.89 pKi
Reference (Journal): Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Published in: J Med Chem

Ligand: tonapofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.13 pKi
Reference (Journal): Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Published in: J Med Chem

Ligand: vipadenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.17 pKi
Reference (Journal): Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
Published in: J Med Chem

Ligand: VPC171 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): A Positive Allosteric Modulator of the Adenosine A1 Receptor Selectively Inhibits Primary Afferent Synaptic Transmission in a Neuropathic Pain Model.
Published in: Mol Pharmacol

Ligand: VPC171 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes.
Published in: J Med Chem

Ligand: VUF5574 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.
Published in: J Med Chem

Ligand: WRC-0571 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Characterization of 8-(N-methylisopropyl)amino-N6-(5'-endohydroxy- endonorbornyl)-9-methyladenine (WRC-0571), a highly potent and selective, non-xanthine antagonist of A1 adenosine receptors.
Published in: J Pharmacol Exp Ther

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor.
Published in: J Biol Chem

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKd
Reference (Journal): N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
Published in: J Med Chem

Ligand: ZM-241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: ZM-241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol