Target family: Adenosine receptors (type: gpcr)
Target: A<sub>3</sub> receptor

Ligand: ZM-241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.13 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: 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: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and characterization of the human A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors.
Published in: J Biol Chem

Ligand: xanthine amine congener (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: VUF8507 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds.
Published in: J Med Chem

Ligand: VUF8504 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds.
Published in: J Med Chem

Ligand: VUF5574 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.39 pKi
Reference (Journal): Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.
Published in: J Med Chem

Ligand: visnagin (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.2 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: vipadenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 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: tonapofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
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): &quot;Cleavable trifunctional&quot; approach to receptor affinity labeling: chemical regeneration of binding to A1-adenosine receptors.
Published in: Bioconjug Chem

Ligand: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Median affinity:  pKi
Reference (Journal): A binding site model and structure-activity relationships for the rat A3 adenosine receptor.
Published in: Mol 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): Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: TCPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.22 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: [3H]PSB-11 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKd
Reference (Journal): [(3)H]8-Ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one ([(3)H]PSB-11), a novel high-affinity antagonist radioligand for human A(3) adenosine receptors.
Published in: Bioorg Med Chem Lett

Ligand: [3H]NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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]NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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]MRE 3008F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKd
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: [3H]MRE 3008F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.1 pKd
Reference (Journal): Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.
Published in: Bioorg Med Chem Lett

Ligand: [3H]HEMADO (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor.
Published in: Eur J Pharmacol

Ligand: [125I]APNEA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKd
Reference (Journal): Molecular cloning and characterization of an adenosine receptor: the A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

Ligand: [125I]AB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
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: [125I]AB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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: [125I]AB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.9 pKd
Reference (Journal): Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors.
Published in: J Biol Chem

Ligand: ST-1535 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 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: (S)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and characterization of the human A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

Ligand: (S)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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: (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: SCH 58261 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.92 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: SCH442416 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: sakuranetin (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: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.
Published in: Neuropharmacology

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  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): 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): Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors.
Published in: J Biol 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): [(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: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and characterization of the human A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

Ligand: rolofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.36 pKi
Reference (Journal): Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
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: 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: PSB36 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.64 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: 5.19 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: 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: PSB-11 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.63 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: 8.31 pKd
Reference (Journal): [(3)H]8-Ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one ([(3)H]PSB-11), a novel high-affinity antagonist radioligand for human A(3) adenosine receptors.
Published in: Bioorg Med Chem Lett

Ligand: PSB-10 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.36 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: 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: piclidenoson (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
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: piclidenoson (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.
Published in: J Med Chem

Ligand: piclidenoson (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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: 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: PENECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 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: nicardipine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity: 5.5 pKi
Reference (Journal): Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
Published in: J Med 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): Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.
Published in: Neuropharmacology

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors.
Published in: J Biol Chem

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  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): Molecular cloning and characterization of the human A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: 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: 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: N(6)-cyclohexyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.75 pKi
Reference (Journal): A binding site model and structure-activity relationships for the rat A3 adenosine receptor.
Published in: Mol Pharmacol

Ligand: N(6)-cyclohexyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.99 pKi
Reference (Journal): Inhibition of TNF-alpha expression by adenosine: role of A3 adenosine receptors.
Published in: J Immunol

Ligand: MSX-2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 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: MRS928 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS8054 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Structure-Activity Studies of 1<i>H</i>-Imidazo[4,5-<i>c</i>]quinolin-4-amine Derivatives as A<sub>3</sub> Adenosine Receptor Positive Allosteric Modulators.
Published in: J Med Chem

Ligand: MRS5698 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.
Published in: J Med Chem

Ligand: MRS5151 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.62 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: 7.61 pKi
Reference (Journal): Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
Published in: Bioorg Med Chem Lett

Ligand: MRS3558 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.83 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: 9 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: 9.54 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: MRS1754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.24 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: MRS1523 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.14 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: 6.95 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
Primary target: no
Median affinity: 7.699999809265137 pKi
Reference (Journal): Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1505 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1486 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1476 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1220 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
Published in: J Med Chem

Ligand: MRS1220 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Radioligand binding and functional responses of ligands for human recombinant adenosine A(3) receptors.
Published in: Auton Autacoid Pharmacol

Ligand: MRS1220 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.
Published in: Neuropharmacology

Ligand: MRS1220 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Cyclic AMP-dependent inhibition of human neutrophil oxidative activity by substituted 2-propynylcyclohexyl adenosine A(2A) receptor agonists.
Published in: Br J Pharmacol

Ligand: MRS1191 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): 6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1191 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1191 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 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: 7.5 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: 7.5 pKi
Reference (Journal): Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.
Published in: Neuropharmacology

Ligand: MRS1186 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
Published in: J Med Chem

Ligand: MRS1177 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
Published in: J Med Chem

Ligand: MRS1097 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.
Published in: Neuropharmacology

Ligand: MRS1097 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
Published in: J Med Chem

Ligand: MRS1093 (Synthetic organic)
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: MRS1088 (Synthetic organic)
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: MRS1067 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.
Published in: Neuropharmacology

Ligand: MRS1067 (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: 6.5 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRS1041 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: MRE 3010F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 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: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 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: 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: 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 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: MPC-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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: LUF7602 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8 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: LUF6096 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
Published in: J Med Chem

Ligand: LUF6000 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
Published in: J Med Chem

Ligand: LUF5981 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Published in: J Med Chem

Ligand: LJ-4517 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.809999942779541 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: LAS38096 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.98 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: 5.98 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: KF26777 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 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: istradefylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: Japan (2013), FDA (2019)
Median affinity: 5.35 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.
Published in: Pharmacol Rev

Ligand: (R,S)-PHPNECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 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: I-ABOPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Molecular cloning and characterization of the human A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

Ligand: I-ABA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Molecular cloning and characterization of the human A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

Ligand: HEMADO (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.96 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: 8.96 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: GS9667 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): A1 adenosine receptor agonists and their potential therapeutic applications.
Published in: Expert Opin Investig Drugs

Ligand: galangin (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: flavone (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: flavanone (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: FK-453 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and characterization of the human A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

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

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Canine mast cell adenosine receptors: cloning and expression of the A3 receptor and evidence that degranulation is mediated by the A2B receptor.
Published in: Mol Pharmacol

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Canine mast cell adenosine receptors: cloning and expression of the A3 receptor and evidence that degranulation is mediated by the A2B receptor.
Published in: Mol Pharmacol

Ligand: DPCPX (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: 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): Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors.
Published in: J Biol Chem

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): 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: dexniguldipine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.7 pKi
Reference (Journal): Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
Published in: J Med Chem

Ligand: derenofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 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: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning and characterization of the human A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

Ligand: cyclopentyladenosine (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: cyclopentyladenosine (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: cyclopentyladenosine (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: CVT-6883 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.97 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: CSC (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): A binding site model and structure-activity relationships for the rat A3 adenosine receptor.
Published in: Mol Pharmacol

Ligand: CP608,039 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.24 pKi
Reference (Journal): Novel N6-substituted adenosine 5'-N-methyluronamides with high selectivity for human adenosine A3 receptors reduce ischemic myocardial injury.
Published in: Am J Physiol Heart Circ Physiol

Ligand: compound 6c [PMID: 34435786] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.619999885559082 pKi
Reference (Journal): Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A<sub>3</sub> Adenosine Receptor Homology Models and Structural Network Analysis Can Predict This Boundary.
Published in: J Med Chem

Ligand: Cl-IB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of novel A3 adenosine receptor-selective antagonists.
Published in: Neuropharmacology

Ligand: Cl-IB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Activation of the A3 adenosine receptor affects cell cycle progression and cell growth.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: Cl-IB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): 2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors.
Published in: J Med Chem

Ligand: Cl-IB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.74 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: 9.48 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
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): 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: Agonist
Ligand approved: no
Median affinity: 6.23 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
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: Full agonist
Ligand approved: 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
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: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
Published in: J Med Chem

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: 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: 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 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: CCPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.63 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: 7.4 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: CCPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 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: 4 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: 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: 4.880000114440918 pKi
Reference (Journal): 1,3-Dialkylxanthine derivatives having high potency as antagonists at human A2B adenosine receptors.
Published in: Drug Dev Res

Ligand: BW-A1433 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Molecular cloning and characterization of the human A3 adenosine receptor.
Published in: Proc Natl Acad Sci USA

Ligand: BW-A1433 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors.
Published in: J Biol Chem

Ligand: binodenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.04 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

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: ATL802 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 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 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: apadenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.35 pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: adenosine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity: 6.539999961853027 pKi
Reference (Journal): Astra Award Lecture. Adenosine, adenosine receptors and the actions of caffeine.
Published in: Pharmacol Toxicol

Ligand: adenosine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity: 6.539999961853027 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: 5.19 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: no
Median affinity: 6.539999961853027 pKi
Reference (Journal): Actions of adenosine at its receptors in the CNS: insights from knockouts and drugs.
Published in: Annu Rev Pharmacol Toxicol

Ligand: AB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 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: AB-MECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 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: 2-phenylethylyl-adenosine derivative (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.36 pKi
Reference (Journal): Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor.
Published in: J Med Chem

Ligand: 2'-Me-CCPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): 2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.
Published in: J Med Chem

Ligand: 2-hexynyl-NECA (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: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.72 pKi
Reference (Journal): A binding site model and structure-activity relationships for the rat A3 adenosine receptor.
Published in: Mol Pharmacol