Target family: Adenosine receptors (type: gpcr)
Target: A<sub>2A</sub> receptor

Ligand: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor.
Published in: J Biol Chem

Ligand: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.12 pKi
Reference (Journal): Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors.
Published in: Pharmacology

Ligand: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: 2-hexynyl-NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  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: 2-hexynyl-NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: 2-hexynyl-NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: AB928 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): AZOLOPYRIMIDINE FOR THE TREATMENT OF CANCER-RELATED DISORDERS

Ligand: AB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.4 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: adenosine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity: 6.510000228881836 pKi
Reference (Journal): Actions of adenosine at its receptors in the CNS: insights from knockouts and drugs.
Published in: Annu Rev Pharmacol Toxicol

Ligand: adenosine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: yes
Median affinity: 6.510000228881836 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)
Median affinity: 6.82 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: 6.510000228881836 pKi
Reference (Journal): Astra Award Lecture. Adenosine, adenosine receptors and the actions of caffeine.
Published in: Pharmacol Toxicol

Ligand: apadenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): Selective A(2A) adenosine receptor activation reduces skin pressure ulcer formation and inflammation.
Published in: Am J Physiol Heart Circ Physiol

Ligand: APNEA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: ATL802 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.18 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: 5.08 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: 6.57 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)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

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: 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): Binding of [3H]MSX-2 (3-(3-hydroxypropyl)-7-methyl-8-(m-methoxystyryl)-1-propargylxanthine) to rat striatal membranes--a new, selective antagonist radioligand for A(2A) adenosine receptors.
Published in: Eur J Pharm Sci

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): 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: CCPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.6 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: CCPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.02 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: CCPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: 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: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor.
Published in: J Biol Chem

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: 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: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor.
Published in: J Biol Chem

Ligand: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.
Published in: J Med Chem

Ligand: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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: CGS 21680 (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: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.72 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: 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: CGS 21680 (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: CGS 24012 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor.
Published in: J Biol Chem

Ligand: ciforadenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): A2AR Antagonism with CPI-444 Induces Antitumor Responses and Augments Efficacy to Anti-PD-(L)1 and Anti-CTLA-4 in Preclinical Models.
Published in: Cancer Immunol Res

Ligand: Cl-IB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.33 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: 5.27 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: 5 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: compound 10 [PMID: 31306001] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.170000076293945 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: compound 4g [PMID: 22220592] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.109999656677246 pKi
Reference (Journal): Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design.
Published in: J Med Chem

Ligand: CPFPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.09 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: 6.03 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: CPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor.
Published in: J Biol Chem

Ligand: CSC (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.27 pKi
Reference (Journal): Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists.
Published in: J Med Chem

Ligand: CV-1674 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: CV-1808 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: CVT-6883 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.48 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
Median affinity: 6.1 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
Median affinity: 6.1 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: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.02 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

Ligand: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: derenofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 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): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: 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: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Binding of [3H]MSX-2 (3-(3-hydroxypropyl)-7-methyl-8-(m-methoxystyryl)-1-propargylxanthine) to rat striatal membranes--a new, selective antagonist radioligand for A(2A) adenosine receptors.
Published in: Eur J Pharm Sci

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
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: FK-453 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.89 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

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: galangin (Natural product)
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: GR79236 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.89 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: 5 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: 5.92 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: HEMADO (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.92 pKi
Reference (Journal): [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor.
Published in: Eur J Pharmacol

Ligand: imaradenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 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: 8.5 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: istradefylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: Japan (2013), FDA (2019)
Median affinity:  pKi
Reference (Journal): Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues.
Published in: Bioorg Med Chem

Ligand: istradefylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: Japan (2013), FDA (2019)
Median affinity:  pKi
Reference (Journal): Adenosine A2A antagonists with potent anti-cataleptic activity.
Published in: Bioorg Med Chem Lett

Ligand: istradefylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: Japan (2013), FDA (2019)
Median affinity:  pKi
Reference (Journal): 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Published in: J Med Chem

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

Ligand: KF 17837S (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: KF26777 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.33 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: LAS38096 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 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: 6 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: LJ-4517 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 pKi
Reference (Journal): GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A<sub>2A</sub> Adenosine Receptor.
Published in: J Med Chem

Ligand: LUF5981 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.71 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: 5.900000095367432 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: 6.980000019073486 pKi
Reference (Journal): Discovery of nonxanthine adenosine A2A receptor antagonists for the treatment of Parkinson's disease.
Published in: Neurology

Ligand: metrifudil (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.5 pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: morin (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.8 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 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: 6.8 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: MRE 3008F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 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: 6.8 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: MRS1041 (Synthetic organic)
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: MRS1042 (Synthetic organic)
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: MRS1065 (Synthetic organic)
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: MRS1066 (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: MRS1084 (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: MRS1086 (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: tonapofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.61 pKi
Reference (Journal): Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Published in: J Med Chem

Ligand: MRS1088 (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: MRS1093 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 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: 4.6 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: 5 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: 5.44 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: 5.69 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: 6.3 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: 6.21 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: 5.63 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: MRS3558 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.97 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: 4.98 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

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

Ligand: MRS923 (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: MRS928 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.2 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: 8.09 pKi
Reference (Journal): Binding of [3H]MSX-2 (3-(3-hydroxypropyl)-7-methyl-8-(m-methoxystyryl)-1-propargylxanthine) to rat striatal membranes--a new, selective antagonist radioligand for A(2A) adenosine receptors.
Published in: Eur J Pharm Sci

Ligand: MSX-2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  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: 8.09 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: 6.34 pKi
Reference (Journal): Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors.
Published in: Pharmacology

Ligand: N(6)-cyclohexyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: N(6)-cyclohexyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a 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): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.
Published in: J Med Chem

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.010000228881836 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: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: PBF-509 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pKi
Reference (Patent): 4-aminopyrimidine derivatives and their as as adenosine A<sub>2A </sub>receptor antagonists

Ligand: PBF-509 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pKi
Reference (Journal): A Novel Antagonist of the Immune Checkpoint Protein Adenosine A2a Receptor Restores Tumor-Infiltrating Lymphocyte Activity in the Context of the Tumor Microenvironment.
Published in: Neoplasia

Ligand: PBF-509 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKi
Reference (Patent): 4-aminopyrimidine derivatives and their as as adenosine A<sub>2A </sub>receptor antagonists

Ligand: PBF-509 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKi
Reference (Journal): A Novel Antagonist of the Immune Checkpoint Protein Adenosine A2a Receptor Restores Tumor-Infiltrating Lymphocyte Activity in the Context of the Tumor Microenvironment.
Published in: Neoplasia

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: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: piclidenoson (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: piclidenoson (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor.
Published in: J Biol Chem

Ligand: preladenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.05 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: 5.57 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: 5.22 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: 5.89 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: 5.68 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: 4.62 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: PSB36 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.01 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: PSB36 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.26 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: 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)
Primary target: yes
Median affinity: 6.539999961853027 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): Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists.
Published in: Bioorg 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): Heterodimerization of substance P and mu-opioid receptors regulates receptor trafficking and resensitization.
Published in: J Biol 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): 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): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor.
Published in: J Biol Chem

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.66 pKi
Reference (Journal): Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors.
Published in: Pharmacology

Ligand: sakuranetin (Natural product)
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: SCH442416 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography.
Published in: J Med Chem

Ligand: SCH442416 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.
Published in: Bioorg Med Chem Lett

Ligand: SCH 58261 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: 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: SCH 58261 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: SCH 58261 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: (S)-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: (S)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: ST-1535 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.18 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: [125I]ZM-241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): 125I-4-(2-[7-amino-2-[2-furyl][1,2,4]triazolo[2,3-a][1,3,5] triazin-5-yl-amino]ethyl)phenol, a high affinity antagonist radioligand selective for the A2a adenosine receptor.
Published in: Mol Pharmacol

Ligand: [3H]CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [3H]CGS 21680, a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain.
Published in: J Pharmacol Exp Ther

Ligand: [3H]CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Binding of the adenosine A2 receptor ligand [3H]CGS 21680 to human and rat brain: evidence for multiple affinity sites.
Published in: J Neurochem

Ligand: [3H]NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 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]SCH 58261 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Differences in the order of potency for agonists but not antagonists at human and rat adenosine A2A receptors.
Published in: Biochem Pharmacol

Ligand: [3H]SCH 58261 (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: [3H]XAC (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKd
Reference (Journal): Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor.
Published in: J Biol Chem

Ligand: [3H]ZM 241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Site-directed mutagenesis studies of human A(2A) adenosine receptors: involvement of glu(13) and his(278) in ligand binding and sodium modulation.
Published in: Biochem Pharmacol

Ligand: [3H]ZM 241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [(3)H]ZM241385--an antagonist radioligand for adenosine A(2A) receptors in rat brain.
Published in: Eur J Pharmacol

Ligand: TCPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.68 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: no
Median affinity: 5.639999866485596 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: tecadenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.639999866485596 pKi
Reference (Journal): Recent developments in adenosine receptor ligands and their potential as novel drugs.
Published in: Biochim Biophys Acta

Ligand: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
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)
Primary target: yes
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)
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: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

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): 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: tonapofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.19 pKi
Reference (Journal): Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Published in: J Med Chem