Target Validation Information
Target ID T36059
Target Name Adenosine A3 receptor
Target Type
Clinical Trial
Drug Potency against Target 2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine Drug Info Ki = 110 nM [528748]
NIPECOTIC ACID Drug Info IC50 = 10.1 nM [527823]
5,6,7-Trimethyl-2-p-tolyl-chromen-4-one Drug Info Ki = 4480 nM [534098]
1-phenyl-3-(2-(pyridin-2-yl)quinazolin-4-yl)urea Drug Info Ki = 490 nM [528290]
1-phenyl-3-(2-(pyridin-3-yl)quinazolin-4-yl)urea Drug Info Ki = 51 nM [528290]
LUF-5978 Drug Info Ki = 25 nM [528673]
2,6-diphenyl-9H-purine Drug Info Ki = 38 nM [528192]
N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine Drug Info Ki = 1120 nM [527647]
3,5,7-Trimethoxy-2-phenyl-chromen-4-one Drug Info Ki = 1210 nM [534098]
MESULERGINE Drug Info IC50 = 1.9 nM [527823]
BEMESETRON Drug Info IC50 = 9.3 nM [527823]
NSC-407228 Drug Info Ki = 3400 nM [534098]
(+)-BUTACLAMOL Drug Info IC50 = 8.9 nM [527823]
LUF-5417 Drug Info Ki = 82 nM [530752]
DIZOCILPINE Drug Info IC50 = 2 nM [527823]
2-(4-methoxyphenyl)-6-phenyl-9H-purine Drug Info Ki = 4 nM [528192]
LUF-5957 Drug Info Ki = 200 nM [528192]
LUF-5981 Drug Info Ki = 637 nM [528673]
8-Bromo-9-cyclopentyl-9H-adenine Drug Info Ki = 4200 nM [530014]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine Drug Info Ki = 296 nM [528748]
2,6-diphenyl-8-tButyl-1-deazapurine Drug Info Ki = 115 nM [528673]
1-Prop-2-ynyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 3080 nM [526332]
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 4440 nM [526332]
8-Hydroxy-5,7,9-trimethyl-delta-carboline Drug Info Ki = 13300 nM [529305]
8-Bromo-9-isopropyl-9H-adenine Drug Info Ki = 15000 nM [530014]
1-Butyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 4.61 nM [526332]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info Ki = 51 nM [527647]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine Drug Info Ki = 171 nM [528673]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine Drug Info Ki = 2.3 nM [528684]
N-(2,6-diphenylpyrimidin-4-yl)butyramide Drug Info Ki = 167 nM [527331]
2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 140 nM [527933]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 260 nM [528748]
2,6-dphenyl-8-propyl-1-deazapurine Drug Info Ki = 69 nM [528673]
2-(2''-indolylethyloxy)adenosine Drug Info Ki = 513 nM [528748]
2-aminoquinazoline-4-carboxyanilide Drug Info Ki = 350 nM [529186]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine Drug Info Ki = 3 nM [528684]
1-Cyclopentyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 639 nM [526332]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine Drug Info Ki = 6 nM [528684]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine Drug Info Ki = 39 nM [528684]
2-(4-nitro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 879 nM [527933]
Adenosine Drug Info Ki = 290 nM [552330]
1-phenyl-3-(3-(pyridin-2-yl)isoquinolin-1-yl)urea Drug Info Ki = 76 nM [528290]
1-phenyl-3-(quinazolin-4-yl)urea Drug Info Ki = 1200 nM [528290]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine Drug Info Ki = 134 nM [527647]
REVERSINE Drug Info Ki = 660 nM [527647]
N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info Ki = 340 nM [527647]
2-benzoylaminoquinazoline-4-carboxyanilide Drug Info Ki = 182 nM [529186]
N-(4,6-diphenylpyrimidin-2-yl)propionamide Drug Info Ki = 547 nM [527331]
2-(hex-1-ynyl)-N6-methoxyadenosine Drug Info Ki = 2.8 nM [528684]
1-Benzyl-1H-1,3,4b,9-tetraaza-fluorene-2,4-dione Drug Info Ki = 370 nM [526388]
3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one Drug Info Ki = 125 nM [529313]
8-PHENYL THEOPHYLLINE Drug Info Ki = 500 nM [533542]
N-(4,5-diphenylpyrimidin-2-yl)acetamide Drug Info Ki = 237 nM [527331]
Tonapofylline Drug Info Ki = 10000 nM [530752]
9H-purine derivative Drug Info IC50 = 14 nM [527823]
N-(2,6-diphenylpyrimidin-4-yl)acetamide Drug Info Ki = 6.88 nM [527331]
Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide Drug Info Ki = 392 nM [527331]
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol Drug Info Ki = 262 nM [528673]
2,6-bis(4-methoxyphenyl)-9H-purine Drug Info Ki = 165 nM [528192]
NECA Drug Info Ki = 113 nM [525473]
CIRSIMARITIN Drug Info Ki = 1720 nM [534098]
NSC-19028 Drug Info Ki = 16900 nM [534098]
LUF-5433 Drug Info Ki = 670 nM [530752]
8-propyl-2,6-diphenyl-9H-purine Drug Info Ki = 17 nM [528192]
LUF-5956 Drug Info Ki = 9.5 nM [528192]
Cyclohexyl-(2-phenoxy-9H-purin-6-yl)-amine Drug Info Ki = 47 nM [527647]
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 6880 nM [526332]
2-(4-chlorophenyl)-6-phenyl-9H-purine Drug Info Ki = 94 nM [528192]
6-Hydroxy-5,7-dimethyl-beta-carboline Drug Info Ki = 17700 nM [529305]
N-(2,6-diphenylpyrimidin-4-yl)benzamide Drug Info Ki = 1300 nM [527331]
2,6-diphenyl-1-deazapurine Drug Info Ki = 180 nM [528673]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine Drug Info Ki = 4.3 nM [528684]
2-(5-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 632 nM [527933]
6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine Drug Info Ki = 30 nM [528748]
2-(3''-(benzoimidazole-1''-yl)ethyloxy)adenosine Drug Info Ki = 2070 nM [528748]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine Drug Info Ki = 86 nM [526104]
2-phenylpropoxyadenosine Drug Info Ki = 66 nM [528748]
8-Hydroxy-7,9-dimethyl-delta-carboline Drug Info Ki = 4430 nM [529305]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine Drug Info Ki = 417 nM [530035]
2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine Drug Info Ki = 10.8 nM [528559]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine Drug Info Ki = 360 nM [528748]
2-(3''-pyrrolylethyloxy)adenosine Drug Info Ki = 104 nM [528748]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 234 nM [528748]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 142 nM [528748]
2-(3''-(benzotriazole-1''-yl)ethyloxy)adenosine Drug Info Ki = 1920 nM [528748]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine Drug Info Ki = 4.4 nM [528684]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 1813 nM [529419]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
2-aminoquinazoline-4-carboxy-(4-bromophenyl)amide Drug Info Ki = 550 nM [529186]
1,2-dihydro-2-oxoquinazoline-4-carboxyanilide Drug Info IC50 = 238 nM [529186]
1-Propyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 2370 nM [526332]
GNF-PF-2224 Drug Info Ki = 1300 nM [531209]
LUF-5767 Drug Info Ki = 147 nM [527331]
N*2*-Benzyl-N*6*-cyclohexyl-9H-purine-2,6-diamine Drug Info Ki = 920 nM [527647]
GBR-12909 Drug Info IC50 = 5 nM [527823]
GLUTAMATE Drug Info IC50 = 613 nM [527823]
METHOCTRAMINE Drug Info IC50 = 34 nM [527823]
GW-328267 Drug Info Ki = 92 nM [527144]
2,6-bis(4-chlorophenyl)-9H-purine Drug Info Ki = 68 nM [528192]
SB-298 Drug Info Ki = 422 nM [530243]
3,5,7-Triethoxy-2-phenyl-chromen-4-one Drug Info Ki = 18200 nM [534145]
NITD609 Drug Info IC50 = 8300 nM [531146]
L-249313 Drug Info Ki = 13 nM [525676]
2-(1H-imidazo[4,5-c]pyridin-2-yl)quinoxaline Drug Info Ki = 168 nM [527933]
N6-(3-Iodobenzyl)-2'-O-methyladenosine Drug Info IC50 = 1.7 nM [528886]
METRIFUDIL Drug Info Ki = 47 nM [527473]
2-Phenyl-2H-pyrazolo[4,3-c]quinoline Drug Info Ki = 212 nM [527649]
4-Methoxy-2-phenyl-2H-pyrazolo[4,3-c]quinoline Drug Info Ki = 166 nM [527649]
2-benzyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Drug Info Ki = 74.5 nM [528969]
3-noradamantyl-1,3-dipropylxanthine Drug Info Ki = 4390 nM [528544]
8-bromo-9-isobutyl-9H-purin-6-amine Drug Info Ki = 15000 nM [530966]
KAINATE Drug Info IC50 = 77 nM [527823]
2-chloro-N6-cyclopentyladenosine Drug Info Ki = 18800 nM [529098]
9-Cyclopentyl-9H-adenine Drug Info Ki = 13000 nM [530014]
OSIP-339391 Drug Info Ki = 450 nM [530966]
2,6-diphenyl-8-ethyl-1-deazapurine Drug Info Ki = 8.5 nM [528673]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate Drug Info Ki = 206 nM [530752]
3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione Drug Info Ki = 50 nM [533542]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide Drug Info Ki = 333 nM [530694]
1-Allyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 16100 nM [526332]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 26 nM [529313]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine Drug Info Ki = 3200 nM [530014]
8-Bromo-9-cyclobutyl-9H-adenine Drug Info Ki = 6200 nM [530014]
2,6,8-triphenyl-9H-purine Drug Info Ki = 49 nM [528192]
8-Bromo-9-(sec-butyl)-9H-adenine Drug Info Ki = 15000 nM [530014]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine Drug Info Ki = 92.3 nM [528748]
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine Drug Info Ki = 7.9 nM [528684]
8-Bromo-9-cyclohexyl-9H-adenine Drug Info Ki = 11000 nM [530014]
2-tolyl-6-phenyl-9H-purine Drug Info Ki = 9.4 nM [528192]
2,6-diphenyl-8-methyl-1-deazapurine Drug Info Ki = 61 nM [528673]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol Drug Info Ki = 2050 nM [529305]
N-(4,6-diphenylpyrimidin-2-yl)-4-chlorobenzamide Drug Info Ki = 3280 nM [527331]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide Drug Info Ki = 447 nM [527331]
R-N6-(phenylisopropyl)adenosine Drug Info Ki = 8.7 nM [528748]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine Drug Info Ki = 120 nM [528748]
2-ethynyl-N6-methoxyadenosine Drug Info Ki = 23 nM [528684]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 90 nM [528748]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine Drug Info Ki = 4.1 nM [528684]
2-acetylaminoquinazoline-4-carboxyanilide Drug Info IC50 = 140 nM [529186]
6-guanidino-2-(3''-indolylethyloxy)adenosine Drug Info Ki = 90 nM [528748]
N6-methoxy-2-phenylethynyladenosine Drug Info Ki = 3.8 nM [528684]
N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine Drug Info Ki = 5.9 nM [528684]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine Drug Info Ki = 5.4 nM [528684]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 763 nM [529313]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine Drug Info Ki = 490 nM [528748]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine Drug Info Ki = 13 nM [528684]
4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one Drug Info Ki = 12300 nM [534145]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide Drug Info Ki = 354 nM [530752]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide Drug Info Ki = 267 nM [527331]
2,6-bis(4-tolyl)-9H-purine Drug Info Ki = 9.3 nM [528192]
LUF-5962 Drug Info Ki = 35 nM [528192]
LUF-5816 Drug Info Ki = 6.9 nM [528673]
LUF-5980 Drug Info Ki = 7.3 nM [528673]
SEROTONIN Drug Info IC50 = 79 nM [527823]
1-(2-(diethylamino)quinazolin-4-yl)-3-phenylurea Drug Info Ki = 180 nM [528290]
5-Butyl-8-phenyl-3H-[1,2,4]triazolo[5,1-i]purine Drug Info IC50 = 0.25 nM [527055]
CVT-6883 Drug Info Ki = 1070 nM [530243]
VUF-8507 Drug Info Ki = 200 nM [528290]
VUF-8504 Drug Info Ki = 17 nM [528290]
N6-CYCLOPENTYLADENOSINE Drug Info Ki = 97 nM [527930]
N-(2,6-diphenylpyrimidin-4-yl)propionamide Drug Info Ki = 22.4 nM [527331]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline Drug Info Ki = 955 nM [527933]
2-(3''-indolylethyloxy)adenosine Drug Info Ki = 232 nM [528748]
2-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one Drug Info Ki = 725 nM [530372]
2-chloro-2'-C-methyl-tecadenoson Drug Info Ki = 18900 nM [529098]
GALANGIN Drug Info Ki = 3150 nM [534098]
4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide Drug Info Ki = 79 nM [526099]
1-Phenethyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 7510 nM [526332]
METHYLTHIOADENOSINE Drug Info Ki = 680 nM [527040]
N6-((+/-)-endo-norborn-2-yl)adenosine Drug Info Ki = 101 nM [530035]
References
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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 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 527331J Med Chem. 2004 Dec 16;47(26):6529-40.2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
Ref 527331J Med Chem. 2004 Dec 16;47(26):6529-40.2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
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