Target Validation Information
TTD ID T77365
Target Name Adenosine A2a receptor (ADORA2A)
Type of Target
Successful
Drug Potency against Target Caffeine Drug Info IC50 = 17 nM [59]
Apadenoson Drug Info Ki = 0.5 nM [17]
Istradefylline Drug Info Ki = 13 nM [58]
Tonapofylline Drug Info Ki = 29 nM [17]
(1H-Imidazo[4,5-c]quinolin-4-yl)-phenyl-amine HCl Drug Info Ki = 10500 nM [43]
(E,E)-8-(4-Phenylbutadien-1-yl)caffeine Drug Info Ki = 153 nM [37]
(E,E)-8-[4-(3-Bromophenyl)butadien-1-yl]caffeine Drug Info Ki = 59.1 nM [37]
(E,E)-8-[4-(3-Chlorophenyl)butadien-1-yl]caffeine Drug Info Ki = 104 nM [37]
(E,E)-8-[4-(3-Fluorophenyl)butadien-1-yl]caffeine Drug Info Ki = 114 nM [37]
(S)-DHPA Drug Info Ki = 8500 nM [39]
(Z)-8-(3-chlorostyryl)caffeine Drug Info Ki = 30.2 nM [37]
1,3,7-Tripropyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 1400 nM [53]
1,3,8-Trimethyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 14000 nM [50]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 820 nM [51]
1,3-Diallyl-7-methyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 4000 nM [53]
1,3-Dibenzyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 14000 nM [53]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 1200 nM [51]
1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 1700 nM [53]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 680 nM [51]
1-Allyl-3,7-dimethyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 6500 nM [53]
1-Butyl-8-phenyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 642 nM [7]
1-Ethyl-3-methyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 5000 nM [53]
1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 2200 nM [7]
1-METHYLXANTHINE Drug Info Ki = 6600 nM [51]
1-Phenyl-3-(4-pyridin-2-yl-thiazol-2-yl)-urea Drug Info Ki = 920 nM [5]
1H-Imidazo[4,5-c]quinolin-4-ylamine HCl Drug Info Ki = 1400 nM [43]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine Drug Info Ki = 2160 nM [40]
2,6,8-triphenyl-9H-purine Drug Info Ki = 66 nM [18]
2,6-diphenyl-1-deazapurine Drug Info Ki = 39 nM [22]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine Drug Info Ki = 247 nM [22]
2,6-diphenyl-8-ethyl-1-deazapurine Drug Info Ki = 177 nM [22]
2,6-diphenyl-8-methyl-1-deazapurine Drug Info Ki = 375 nM [22]
2,6-diphenyl-8-tButyl-1-deazapurine Drug Info Ki = 1055 nM [22]
2,6-diphenyl-9H-purine Drug Info Ki = 53 nM [18]
2,6-Diphenyl-pyrimidin-4-ylamine Drug Info Ki = 169 nM [30]
2,6-dphenyl-8-propyl-1-deazapurine Drug Info Ki = 114 nM [22]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 561 nM [32]
2-(2''-indolylethyloxy)adenosine Drug Info Ki = 373 nM [24]
2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine Drug Info Ki = 2.9 nM [29]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine Drug Info Ki = 390 nM [24]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 252 nM [24]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 39.7 nM [24]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 502 nM [24]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine Drug Info Ki = 370 nM [24]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine Drug Info Ki = 450 nM [24]
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine Drug Info Ki = 900 nM [24]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine Drug Info Ki = 1400 nM [24]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 150 nM [24]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine Drug Info Ki = 29.3 nM [24]
2-(3''-(benzoimidazole-1''-yl)ethyloxy)adenosine Drug Info Ki = 3870 nM [24]
2-(3''-indolylethyloxy)adenosine Drug Info Ki = 45 nM [24]
2-(3''-pyrrolylethyloxy)adenosine Drug Info Ki = 95 nM [24]
2-(4-chlorophenyl)-6-phenyl-9H-purine Drug Info Ki = 315 nM [18]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline Drug Info Ki = 3440 nM [16]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine Drug Info Ki = 758 nM [23]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 833 nM [32]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine Drug Info Ki = 1820 nM [23]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol Drug Info Ki = 620 nM [48]
2-(hex-1-ynyl)-N6-methoxyadenosine Drug Info Ki = 267 nM [23]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile Drug Info Ki = 1 nM [36]
2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile Drug Info Ki = 32 nM [36]
2-Amino-4,6-diphenyl-nicotinonitrile Drug Info Ki = 130 nM [36]
2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile Drug Info Ki = 22.7 nM [30]
2-Amino-4,6-diphenyl-pyrimidine Drug Info Ki = 405 nM [30]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile Drug Info Ki = 19 nM [36]
2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile Drug Info Ki = 88 nM [36]
2-Amino-6-furan-2-yl-4-phenyl-nicotinonitrile Drug Info Ki = 11 nM [36]
2-amino-6-phenyl-4-p-tolylnicotinonitrile Drug Info Ki = 118 nM [19]
2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile Drug Info Ki = 54 nM [36]
2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide Drug Info Ki = 17 nM [35]
2-chloro-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 20 nM [34]
2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 391 nM [34]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info Ki = 740 nM [43]
2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 30 nM [34]
2-ethyl-4-(furan-3-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 681 nM [34]
2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 13 nM [34]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 1.6 nM [34]
2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 69 nM [34]
2-ethynyl-N6-methoxyadenosine Drug Info Ki = 3140 nM [23]
2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine Drug Info Ki = 228 nM [26]
2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine Drug Info Ki = 329 nM [26]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info Ki = 290 nM [43]
2-phenyl-2H-pyrazolo[3,4-c]quinolin-4-amine Drug Info Ki = 91 nM [26]
2-phenylpropoxyadenosine Drug Info Ki = 500 nM [24]
2-tolyl-6-phenyl-9H-purine Drug Info Ki = 289 nM [18]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine Drug Info Ki = 2680 nM [23]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine Drug Info Ki = 3960 nM [23]
3-Benzyl-7-methyl-[1,8]naphthyridin-4-ol Drug Info Ki = 3330 nM [13]
3-Benzyl-7-methyl-[1,8]naphthyridine-4-thiol Drug Info Ki = 9140 nM [13]
3-Isopropyl-1-methyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 6000 nM [53]
3-noradamantyl-1,3-dipropylxanthine Drug Info Ki = 673 nM [20]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [49]
4-(ethylthio)-6-phenyl-1,3,5-triazin-2-amine Drug Info Ki = 5 nM [19]
4-(furan-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine Drug Info Ki = 242 nM [38]
4-(furan-2-yl)thieno[3,2-d]pyrimidin-2-amine Drug Info Ki = 14 nM [35]
4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine Drug Info Ki = 35 nM [34]
4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile Drug Info Ki = 19 nM [30]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol Drug Info Ki = 4920 nM [31]
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol Drug Info Ki = 192 nM [22]
5-Azido-6-benzyl-2-methyl-[1,8]naphthyridine Drug Info Ki = 5360 nM [13]
5-Butyl-8-phenyl-3H-[1,2,4]triazolo[5,1-i]purine Drug Info IC50 = 71 nM [9]
6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 261 nM [38]
6-Furan-2-yl-9-phenethyl-9H-purin-2-ylamine Drug Info Ki = 270.5 nM [11]
6-Furan-2-yl-9-phenyl-9H-purin-2-ylamine Drug Info Ki = 68.5 nM [11]
6-guanidino-2-(3''-indolylethyloxy)adenosine Drug Info Ki = 277 nM [24]
7-Allyl-1,3-dimethyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 10000 nM [53]
7-Allyl-1,3-dipropyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 700 nM [53]
7-Isopropyl-7H-adenine Drug Info Ki = 12000 nM [39]
7-Propyl-7H-adenine Drug Info Ki = 18000 nM [39]
8-Br-adenine Drug Info Ki = 3200 nM [39]
8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine Drug Info Ki = 4000 nM [39]
8-Bromo-9-(2-butyl)-9H-adenine Drug Info Ki = 730 nM [39]
8-Bromo-9-(2-hydroxypropyl)-9H-adenine Drug Info Ki = 1100 nM [39]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine Drug Info Ki = 85 nM [39]
8-Bromo-9-(but-3-enyl)-9H-adenine Drug Info Ki = 1600 nM [39]
8-Bromo-9-(sec-butyl)-9H-adenine Drug Info Ki = 390 nM [39]
8-Bromo-9-cyclobutyl-9H-adenine Drug Info Ki = 660 nM [39]
8-Bromo-9-cyclohexyl-9H-adenine Drug Info Ki = 15000 nM [39]
8-Bromo-9-cyclopentyl-9H-adenine Drug Info Ki = 1900 nM [39]
8-Bromo-9-ethyl-9H-adenine Drug Info Ki = 52 nM [39]
8-bromo-9-isobutyl-9H-purin-6-amine Drug Info Ki = 6000 nM [48]
8-Bromo-9-isopropyl-9H-adenine Drug Info Ki = 74 nM [39]
8-Bromo-9-methyl-9H-adenine Drug Info Ki = 120 nM [39]
8-Bromo-9-phenylethyl-9H-adenine Drug Info Ki = 4900 nM [39]
8-Bromo-9-propyl-9H-adenine Drug Info Ki = 300 nM [39]
8-PHENYL THEOPHYLLINE Drug Info Ki = 850 nM [43]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 1900 nM [7]
8-propyl-2,6-diphenyl-9H-purine Drug Info Ki = 167 nM [18]
9-(2-Hydroxyethyl)-9H-adenine Drug Info Ki = 11000 nM [39]
9-(2-Hydroxypropyl)-9H-adenine Drug Info Ki = 3100 nM [39]
9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 23 nM [35]
9-(3-Hydroxypropyl)-9H-adenine Drug Info Ki = 3900 nM [39]
9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 85 nM [35]
9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 372 nM [35]
9-(sec-Butyl)-9H-adenine Drug Info Ki = 16000 nM [39]
9-Allyl-8-bromo-9H-adenine Drug Info Ki = 730 nM [39]
9-benzyl-6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 40 nM [35]
9-Benzyl-8-bromo-9H-adenine Drug Info Ki = 6100 nM [39]
9-BENZYL-9H-ADENINE Drug Info Ki = 8500 nM [39]
9-But-3-enyl-9H-adenine Drug Info Ki = 8500 nM [39]
9-Butyl-9H-adenine Drug Info Ki = 7800 nM [39]
9-Cyclobutyl-9H-adenine Drug Info Ki = 4800 nM [39]
9-Cycloheptyl-9H-adenine Drug Info Ki = 11000 nM [39]
9-Cyclopentyl-9H-adenine Drug Info Ki = 1800 nM [39]
9-Cyclopropyl-9H-adenine Drug Info Ki = 2300 nM [39]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine Drug Info Ki = 600 nM [6]
9-Ethyl-9H-adenine Drug Info Ki = 2200 nM [39]
9-Isopropyl-9H-adenine Drug Info Ki = 4100 nM [39]
9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine Drug Info Ki = 46.3 nM [15]
9-Methyl-9H-adenine Drug Info Ki = 6900 nM [39]
9-Phenylethyl-9H-adenine Drug Info Ki = 9600 nM [39]
9-Propyl-9H-adenine Drug Info Ki = 9600 nM [39]
Alloxazine Drug Info Ki = 935 nM [15]
ARISTEROMYCIN Drug Info Ki = 2150 nM [3]
CVT-6883 Drug Info Ki = 3280 nM [41]
Cyclohexyl-(2-phenoxy-9H-purin-6-yl)-amine Drug Info Ki = 16000 nM [12]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine Drug Info Ki = 14000 nM [12]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate Drug Info Ki = 1640 nM [47]
FK-453 Drug Info IC50 = 1180 nM [47]
FK-838 Drug Info Ki = 1202 nM [47]
FR-166124 Drug Info IC50 = 6200 nM [1]
Galangin Drug Info Ki = 18100 nM [55]
GNF-PF-2224 Drug Info Ki = 157 nM [45]
GNF-PF-2700 Drug Info Ki = 624 nM [48]
GW-328267 Drug Info IC50 = 0.4 nM [44]
isobutylmethylxanthine Drug Info Ki = 8000 nM [53]
Isoguanosine Drug Info Ki = 331 nM
Istradefylline Drug Info Ki = 2 nM [29]
KF-17837 Drug Info Ki = 1 nM [54]
Kuanoniamine D Drug Info Ki = 13700 nM [56]
LUF-5417 Drug Info Ki = 2340 nM [47]
LUF-5433 Drug Info Ki = 1900 nM [47]
LUF-5437 Drug Info Ki = 570 nM [5]
LUF-5767 Drug Info Ki = 899 nM [10]
LUF-5956 Drug Info Ki = 148 nM [18]
LUF-5957 Drug Info Ki = 118 nM [18]
LUF-5962 Drug Info Ki = 55 nM [18]
LUF-5978 Drug Info Ki = 189 nM [22]
LUF-5980 Drug Info Ki = 230 nM [22]
LUF-5981 Drug Info Ki = 194 nM [22]
METHYLTHIOADENOSINE Drug Info Ki = 1180 nM [8]
METRIFUDIL Drug Info Ki = 25 nM [2]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info Ki = 1700 nM [12]
N-(2,6-diphenylpyrimidin-4-yl)-2-ethylbutyramide Drug Info Ki = 381 nM [10]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide Drug Info Ki = 157 nM [10]
N-(2,6-diphenylpyrimidin-4-yl)acetamide Drug Info Ki = 489 nM [10]
N-(2,6-diphenylpyrimidin-4-yl)butyramide Drug Info Ki = 124 nM [10]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide Drug Info Ki = 376 nM [10]
N-(2,6-diphenylpyrimidin-4-yl)propionamide Drug Info Ki = 81.9 nM [10]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide Drug Info Ki = 209 nM [46]
N-(3-Phenyl-[1,2,4]thiadiazol-5-yl)-benzamide Drug Info Ki = 4400 nM [5]
N-(4,6-diphenylpyrimidin-2-yl)propionamide Drug Info Ki = 893 nM [10]
N-(4-Pyridin-2-yl-thiazol-2-yl)-benzamide Drug Info Ki = 8700 nM [5]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide Drug Info Ki = 3030 nM [47]
N6-((+/-)-endo-norborn-2-yl)adenosine Drug Info Ki = 1270 nM [40]
N6-(4-hydroxybenzyl)adenine riboside Drug Info Ki = 2620 nM [25]
N6-CYCLOPENTYLADENOSINE Drug Info Ki = 2470 nM [47]
N6-methoxy-2-phenylethynyladenosine Drug Info Ki = 4290 nM [23]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine Drug Info Ki = 2960 nM [23]
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine Drug Info Ki = 12500 nM [23]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine Drug Info Ki = 1780 nM [23]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine Drug Info Ki = 6520 nM [23]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine Drug Info Ki = 6310 nM [23]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine Drug Info Ki = 5740 nM [23]
N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine Drug Info Ki = 4170 nM [28]
N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine Drug Info Ki = 1900 nM [28]
PD-115199 Drug Info Ki = 15.5 nM [14]
Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol Drug Info Ki = 9524 nM [33]
PSB-0788 Drug Info Ki = 1730 nM [41]
PSB-09120 Drug Info Ki = 122 nM [41]
PSB-601 Drug Info Ki = 93.7 nM [41]
R-N6-(phenylisopropyl)adenosine Drug Info Ki = 884 nM [24]
SB-298 Drug Info Ki = 2139 nM [41]
SCH 420814 Drug Info Ki = 0.6 nM [21]
SCH-442416 Drug Info Ki = 0.5 nM [4]
SCH-63390 Drug Info Ki = 2.4 nM [57]
ST-1535 Drug Info Ki = 6.6 nM [36]
Tonapofylline Drug Info Ki = 2440 nM [47]
ZM-241385 Drug Info Ki = 1.2 nM [42]
[3H]CCPA Drug Info Ki = 2300 nM [27]
[3H]NECA Drug Info Ki = 22 nM [52]
[3H]OSIP339391 Drug Info Ki = 328 nM [48]
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