Target Validation Information
Target ID T86679
Target Name Adenosine A2b receptor
Target Type
Successful
Drug Potency against Target ISOGUANOSINE Drug Info Ki = 331 nM
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 680 nM [533429]
CVT-6883 Drug Info Ki = 22 nM [530243]
ST-1535 Drug Info Ki = 352.3 nM [527823]
8-Bromo-9-methyl-9H-adenine Drug Info Ki = 720 nM [530014]
CVT-7124 Drug Info Ki = 6 nM [530966]
1-Propyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 1880 nM [526332]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide Drug Info Ki = 7 nM [530694]
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 10200 nM [526332]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile Drug Info Ki = 170 nM [529602]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info Ki = 50 nM [533542]
9-Cyclobutyl-9H-adenine Drug Info Ki = 17000 nM [530014]
N6-CYCLOPENTYLADENOSINE Drug Info Ki = 2000 nM [533449]
PSB-0788 Drug Info IC50 = 3.64 nM [530243]
PSB-1115 Drug Info Ki = 53.4 nM [530243]
8-(3-Fluoro-phenyl)-9-methyl-9H-purin-6-ylamine Drug Info IC50 = 5300 nM [525962]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate Drug Info Ki = 391 nM [530752]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine Drug Info Ki = 300 nM [528673]
PSB-601 Drug Info Ki = 3.6 nM [530966]
2-chloro-N6-cyclopentyladenosine Drug Info Ki = 42 nM [529098]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info Ki = 740 nM [530590]
METHYLTHIOADENOSINE Drug Info Ki = 8200 nM [527040]
8-Bromo-9-cyclobutyl-9H-adenine Drug Info Ki = 4100 nM [530014]
8-Bromo-9-isopropyl-9H-adenine Drug Info Ki = 1100 nM [530014]
8-Bromo-9-ethyl-9H-adenine Drug Info Ki = 840 nM [530014]
8-Bromo-9-cyclopentyl-9H-adenine Drug Info Ki = 860 nM [530014]
LUF-5981 Drug Info Ki = 300 nM [528673]
GNF-PF-2224 Drug Info IC50 = 1130 nM
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine Drug Info Ki = 4830 nM [530035]
9-(sec-Butyl)-9H-adenine Drug Info Ki = 19000 nM [530014]
(1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl Drug Info Ki = 10500 nM [530590]
LUF-5816 Drug Info Ki = 300 nM [528673]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile Drug Info Ki = 34 nM [529602]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 11.8 nM [526958]
N6-((+/-)-endo-norborn-2-yl)adenosine Drug Info Ki = 4930 nM [530035]
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 5530 nM [526332]
3-noradamantyl-1,3-dipropylxanthine Drug Info Ki = 296 nM [528544]
CVT-6694 Drug Info Ki = 7 nM [530966]
8-PHENYL THEOPHYLLINE Drug Info IC50 = 1100 nM [525962]
Tonapofylline Drug Info Ki = 90 nM [530752]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol Drug Info Ki = 2800 nM [530966]
PSB-09120 Drug Info Ki = 0.157 nM [530243]
GNF-PF-2700 Drug Info Ki = 1780 nM [530966]
8-bromo-9-isobutyl-9H-purin-6-amine Drug Info Ki = 4200 nM [530966]
FK-453 Drug Info IC50 = 8100 nM [525962]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine Drug Info Ki = 5100 nM [530014]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info Ki = 290 nM [530590]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 820 nM [533429]
1-METHYLXANTHINE Drug Info Ki = 6600 nM [533429]
GW-328267 Drug Info Ki = 1300 nM [527144]
8-Bromo-9-(2-butyl)-9H-adenine Drug Info Ki = 5600 nM [530014]
8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine Drug Info Ki = 7100 nM [530014]
9-Allyl-8-bromo-9H-adenine Drug Info Ki = 4600 nM [530014]
8-Bromo-9-(sec-butyl)-9H-adenine Drug Info Ki = 1200 nM [530014]
8-Bromo-9-propyl-9H-adenine Drug Info Ki = 200 nM [530014]
9-Isopropyl-9H-adenine Drug Info Ki = 16000 nM [530014]
8-Bromo-9-(2-hydroxypropyl)-9H-adenine Drug Info Ki = 640 nM [530014]
9-Propyl-9H-adenine Drug Info Ki = 1700 nM [530014]
2-chloro-2'-C-methyl-tecadenoson Drug Info Ki = 4470 nM [529098]
LUF-5978 Drug Info Ki = 300 nM [528673]
BETA-HYDROXYETHYL THEOPHYLLINE Drug Info Ki = 17300 nM [530966]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 1200 nM [533429]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile Drug Info Ki = 220 nM [529602]
LUF-5980 Drug Info Ki = 300 nM [528673]
1H-Imidazo[4,5-c]quinolin-4-ylamine HCl Drug Info Ki = 1400 nM [530590]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 4.7 nM [526958]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 721 nM [529419]
SB-298 Drug Info Ki = 1.2 nM [530243]
OSIP-339391 Drug Info Ki = 0.5 nM [530966]
2'-Me-tecadenoson Drug Info Ki = 4440 nM [529098]
PD-115199 Drug Info Ki = 15.5 nM [527717]
ALLOXAZINE Drug Info Ki = 3.8 nM [527823]
NECA Drug Info Ki = 22 nM [533449]
ZM-241385 Drug Info Ki = 19.3 nM [530768]
KF-17837 Drug Info Ki = 1 nM [533955]
References
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Ref 526332J Med Chem. 2002 May 23;45(11):2131-8.Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
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Ref 533449J Med Chem. 1988 Jun;31(6):1179-83.Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.
Ref 530243J Med Chem. 2009 Jul 9;52(13):3994-4006.1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Ref 530243J Med Chem. 2009 Jul 9;52(13):3994-4006.1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Ref 525962J Med Chem. 2001 Jan 18;44(2):170-9.2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.
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Ref 528673J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Ref 530966Eur J Med Chem. 2010 Aug;45(8):3459-71. Epub 2010 May 7.Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
Ref 529098Bioorg Med Chem. 2008 Jan 1;16(1):336-53. Epub 2007 Sep 22.5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivityfor A1 receptor from different species.
Ref 530590J Med Chem. 1991 Mar;34(3):1202-6.1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
Ref 527040J Med Chem. 2004 Apr 22;47(9):2243-55.Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative.
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Ref 528673J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Ref 530035J Med Chem. 2009 Apr 23;52(8):2393-406.N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
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Ref 530590J Med Chem. 1991 Mar;34(3):1202-6.1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
Ref 528673J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Ref 529602J Med Chem. 2008 Aug 14;51(15):4449-55. Epub 2008 Jul 19.2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
Ref 526958J Med Chem. 2004 Feb 12;47(4):1031-43.Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugswith peroral bioavailability.
Ref 530035J Med Chem. 2009 Apr 23;52(8):2393-406.N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
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Ref 528544J Med Chem. 2006 Nov 30;49(24):7119-31.Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Ref 530966Eur J Med Chem. 2010 Aug;45(8):3459-71. Epub 2010 May 7.Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
Ref 525962J Med Chem. 2001 Jan 18;44(2):170-9.2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.
Ref 530752Bioorg Med Chem. 2010 Mar 15;18(6):2195-203. Epub 2010 Feb 4.2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
Ref 530966Eur J Med Chem. 2010 Aug;45(8):3459-71. Epub 2010 May 7.Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
Ref 530243J Med Chem. 2009 Jul 9;52(13):3994-4006.1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Ref 530966Eur J Med Chem. 2010 Aug;45(8):3459-71. Epub 2010 May 7.Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
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Ref 525962J Med Chem. 2001 Jan 18;44(2):170-9.2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.
Ref 530014Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Ref 530590J Med Chem. 1991 Mar;34(3):1202-6.1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
Ref 533429J Med Chem. 1988 Oct;31(10):2034-9.Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.
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Ref 530014Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Ref 530014Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Ref 530014Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Ref 530014Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Ref 530014Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Ref 530014Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Ref 530014Bioorg Med Chem. 2009 Apr 1;17(7):2812-22. Epub 2009 Feb 23.8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
Ref 529098Bioorg Med Chem. 2008 Jan 1;16(1):336-53. Epub 2007 Sep 22.5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivityfor A1 receptor from different species.
Ref 528673J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Ref 530966Eur J Med Chem. 2010 Aug;45(8):3459-71. Epub 2010 May 7.Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
Ref 533429J Med Chem. 1988 Oct;31(10):2034-9.Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.
Ref 529602J Med Chem. 2008 Aug 14;51(15):4449-55. Epub 2008 Jul 19.2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
Ref 528673J Med Chem. 2007 Feb 22;50(4):828-34.2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Ref 530590J Med Chem. 1991 Mar;34(3):1202-6.1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.
Ref 526958J Med Chem. 2004 Feb 12;47(4):1031-43.Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugswith peroral bioavailability.
Ref 529419Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3. Epub 2008 Mar 30.Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
Ref 530243J Med Chem. 2009 Jul 9;52(13):3994-4006.1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Ref 530966Eur J Med Chem. 2010 Aug;45(8):3459-71. Epub 2010 May 7.Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
Ref 529098Bioorg Med Chem. 2008 Jan 1;16(1):336-53. Epub 2007 Sep 22.5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivityfor A1 receptor from different species.
Ref 527717J Med Chem. 1992 Jun 12;35(12):2342-5.(E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists.
Ref 527823J Med Chem. 2005 Nov 3;48(22):6887-96.2-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.
Ref 533449J Med Chem. 1988 Jun;31(6):1179-83.Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.
Ref 530768Bioorg Med Chem. 2010 Mar 15;18(6):2081-8. Epub 2010 Feb 15.Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors.
Ref 533955J Med Chem. 1993 Nov 12;36(23):3731-3.Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine.

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