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

Ligand: ZM-241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors.
Published in: Biochem Pharmacol

Ligand: ZM-241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.
Published in: Mol Pharmacol

Ligand: ZM-241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: ZM-241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Published in: Biochem Pharmacol

Ligand: XCC (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Published in: Biochem Pharmacol

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pA2
Reference (Journal): Characterization of the human brain putative A2B adenosine receptor expressed in Chinese hamster ovary (CHO.A2B4) cells.
Published in: Br J Pharmacol

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: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Use of the triazolotriazine [3H]ZM 241385 as a radioligand at recombinant human A2B adenosine receptors.
Published in: Drug Des Discov

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors.
Published in: Biochem Pharmacol

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.
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): [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Published in: Biochem Pharmacol

Ligand: vipadenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 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: 7.05 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)
Primary target: yes
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: 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 and rodent native and recombinant adenosine A(2B) receptors by radioligand binding studies.
Published in: Purinergic Signal

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)
Median affinity: 5.25 pKi
Reference (Journal): Characterization of the A2B adenosine receptor from mouse, rabbit, and dog.
Published in: J Pharmacol Exp Ther

Ligand: theophylline (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1976)
Primary target: yes
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: TCPA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells.
Published in: Br J Pharmacol

Ligand: [3H]ZM 241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Use of the triazolotriazine [3H]ZM 241385 as a radioligand at recombinant human A2B adenosine receptors.
Published in: Drug Des Discov

Ligand: [3H]ZM 241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors.
Published in: Biochem Pharmacol

Ligand: [3H]ZM 241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Inhibition of human mast cell activation with the novel selective adenosine A(2B) receptor antagonist 3-isobutyl-8-pyrrolidinoxanthine (IPDX)(2).
Published in: Biochem Pharmacol

Ligand: [3H]PSB603 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.4 pKd
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: [3H]PSB603 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKd
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: [3H]OSIP339391 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.8 pKd
Reference (Journal): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors.
Published in: Biochem Pharmacol

Ligand: [3H]MRS1754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.8 pKd
Reference (Journal): [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Published in: Biochem Pharmacol

Ligand: [3H]DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pKd
Reference (Journal): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors.
Published in: Biochem Pharmacol

Ligand: [125I]ABOPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pKd
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: ST-1535 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.45 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): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: (S)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
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: SCH 58261 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.
Published in: Mol Pharmacol

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

Ligand: 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: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Adenosine receptor activation in human fibroblasts: nucleoside agonists and antagonists.
Published in: Can J Physiol Pharmacol

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.72 pKi
Reference (Journal): Functional characterization of the A2b adenosine receptor in NIH 3T3 fibroblasts.
Published in: Biochem Pharmacol

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]MRS 1754, a selective antagonist radioligand for A(2B) 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): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: (R)-PIA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.
Published in: Mol Pharmacol

Ligand: rolofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.53 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: 9.39 pKd
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: 9.45 pKd
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: 9.26 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: 6.73 pKi
Reference (Journal): Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists.
Published in: Bioorg Med Chem

Ligand: PSB1115 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.27 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: 5.68 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-10 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.68 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-0788 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.4 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: 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): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

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: pentoxifylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1984)
Primary target: no
Median affinity: 5.289999961853027 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: OSIP339391 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B 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): 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: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B 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): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B 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): Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.
Published in: Mol Pharmacol

Ligand: NECA (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5.72 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): [3H]MRS 1754, a selective antagonist radioligand for A(2B) 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): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
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): Adenosine receptor agonists: from basic medicinal chemistry to clinical development.
Published in: Expert Opin Emerg Drugs

Ligand: N(6)-cyclohexyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 3.8 pKi
Reference (Journal): Adenosine receptor activation in human fibroblasts: nucleoside agonists and antagonists.
Published in: Can J Physiol Pharmacol

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:  pKi
Reference (Journal): Involvement of adenosine A1 receptors in the discriminative-stimulus effects of caffeine in rats.
Published in: Psychopharmacology (Berl.)

Ligand: MRS3558 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5 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
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Published in: Biochem Pharmacol

Ligand: MRS1754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.47 pKi
Reference (Journal): Characterization of the A2B adenosine receptor from mouse, rabbit, and dog.
Published in: J Pharmacol Exp Ther

Ligand: MRS1754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 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:  pKi
Reference (Journal): Antagonist pharmacology of adenosine A2B receptors from rat, guinea pig and dog.
Published in: Eur J Pharmacol

Ligand: MRS1754 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  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: MRS1706 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.86 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: 5 pKi
Reference (Book): 
Published in: A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics

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

Ligand: MRS1220 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors.
Published in: Biochem Pharmacol

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

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

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

Ligand: MRE 2029F20 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  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: LUF5981 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.52 pKi
Reference (Journal): Progress in pursuit of therapeutic A2A antagonists: the adenosine A2A receptor selective antagonist KW6002: research and development toward a novel nondopaminergic therapy for Parkinson's disease.
Published in: Neurology

Ligand: LAS38096 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.77 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: LAS38096 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.77 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: KF26777 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.21 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 pKi
Reference (Journal): International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update.
Published in: Pharmacol Rev

Ligand: ISAM-140 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.460000038146973 pKi
Reference (Journal): Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.
Published in: J Med Chem

Ligand: imaradenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.190000057220459 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: I-ABOPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: HEMADO (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.52 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: 4.52 pKi
Reference (Journal): [3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor.
Published in: Eur J Pharmacol

Ligand: GS9667 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.3 pKi
Reference (Journal): A1 adenosine receptor agonists and their potential therapeutic applications.
Published in: Expert Opin Investig Drugs

Ligand: FK-453 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.01 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: 7.06 pKi
Reference (Journal): Characterization of the A2B adenosine receptor from mouse, rabbit, and dog.
Published in: J Pharmacol Exp Ther

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Antagonist pharmacology of adenosine A2B receptors from rat, guinea pig and dog.
Published in: Eur J Pharmacol

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

Ligand: DPCPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors.
Published in: Biochem 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): 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): 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: derenofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pKi
Reference (Journal): The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure.
Published in: Br J Pharmacol

Ligand: derenofylline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.4 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: DEPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: DAX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Published in: Biochem 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: cyclopentyladenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: CVT-6883 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.66 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: 5.09 pKi
Reference (Book): Adenosine receptors: selective agonists and antagonists.
Published in: Adenosine and adenine nucleotides: from molecular biology to integrative physiology.

Ligand: CPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Published in: Biochem Pharmacol

Ligand: CPX (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

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: 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: 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): Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.
Published in: Mol Pharmacol

Ligand: CGS 21680 (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: CGS 21680 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.04 pKi
Reference (Journal): Characterization of the A2B adenosine receptor from mouse, rabbit, and dog.
Published in: J Pharmacol Exp Ther

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: 7.800000190734863 pA2
Reference (Journal): Characterization of the human brain putative A2B adenosine receptor expressed in Chinese hamster ovary (CHO.A2B4) cells.
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): Characterization of the A2B adenosine receptor from mouse, rabbit, and dog.
Published in: J Pharmacol Exp Ther

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Published in: Biochem Pharmacol

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Use of the triazolotriazine [3H]ZM 241385 as a radioligand at recombinant human A2B adenosine receptors.
Published in: Drug Des Discov

Ligand: CGS 15943 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors.
Published in: Biochem 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: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Adenosine receptors as therapeutic targets.
Published in: Nat Rev Drug Discov

Ligand: CCPA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol 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): Characterization of human and rodent native and recombinant adenosine A(2B) receptors by radioligand binding studies.
Published in: Purinergic Signal

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-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)
Median affinity: 4.89 pKi
Reference (Journal): Functional characterization of the A2b adenosine receptor in NIH 3T3 fibroblasts.
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)
Median affinity: 4.52 pKi
Reference (Journal): Functional characterization of the A2b adenosine receptor in NIH 3T3 fibroblasts.
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): 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: BW-A1433 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: binodenoson (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 3.37 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: 6.48 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: BAY 60-6583 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Cardioprotection by ecto-5'-nucleotidase (CD73) and A2B adenosine receptors.
Published in: Circulation

Ligand: BAY-545 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 pIC50
Reference (Journal): Novel non-xanthine antagonist of the A<sub>2B</sub> adenosine receptor: From HTS hit to lead structure.
Published in: Eur J Med Chem

Ligand: BAY-545 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Novel non-xanthine antagonist of the A<sub>2B</sub> adenosine receptor: From HTS hit to lead structure.
Published in: Eur J Med Chem

Ligand: BAY-545 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.010000228881836 pKi
Reference (Journal): Novel non-xanthine antagonist of the A<sub>2B</sub> adenosine receptor: From HTS hit to lead structure.
Published in: Eur J Med Chem

Ligand: ATL802 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.63 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: 8.07 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: AS99 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS96 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS95 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS94 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS74 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS70 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS16 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.7 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS101 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: AS100 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: alloxazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Use of the triazolotriazine [3H]ZM 241385 as a radioligand at recombinant human A2B adenosine receptors.
Published in: Drug Des Discov

Ligand: alloxazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Published in: Biochem Pharmacol

Ligand: adenosine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1989)
Primary target: no
Median affinity: 4.820000171661377 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: 4.820000171661377 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)
Median affinity: 5.29 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: 4.820000171661377 pKi
Reference (Journal): Adenosine receptor agonists: from basic medicinal chemistry to clinical development.
Published in: Expert Opin Emerg Drugs

Ligand: AB-NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.7 pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol

Ligand: 3-isobutyl-8-pyrrolidinoxanthine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 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: 2-hexynyl-NECA (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.
Published in: Biochem Pharmacol

Ligand: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine.
Published in: Mol Pharmacol

Ligand: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Adenosine receptor activation in human fibroblasts: nucleoside agonists and antagonists.
Published in: Can J Physiol Pharmacol

Ligand: 2-chloroadenosine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
Published in: Mol Pharmacol