Target Validation Information
TTD ID T92072
Target Name Adenosine A1 receptor (ADORA1)
Type of Target
Successful
Drug Potency against Target Caffeine Drug Info IC50 = 107000 nM [71]
Drug Info IC50 = 9500 nM [70]
CVT-124 Drug Info Ki = 0.45 nM [69]
Tecadenoson Drug Info Ki = 6.5 nM [23]
Drug Info Ki = 8.6 nM [28]
Drug Info IC50 = 1700 nM [28]
Drug Info Ki = 67 nM [33]
Drug Info Ki = 3100 nM [47]
Drug Info Ki = 255 nM [29]
Drug Info Ki = 37.5 nM [17]
Drug Info Ki = 6.35 nM [17]
Drug Info Ki = 94 nM
Drug Info Ki = 651 nM [55]
Drug Info Ki = 0.61 nM [28]
Drug Info Ki = 2765 nM [46]
Drug Info Ki = 86 nM [9]
Drug Info Ki = 7000 nM [44]
Drug Info Ki = 615 nM [40]
Drug Info Ki = 28 nM [42]
Drug Info Ki = 27.1 nM [17]
Drug Info IC50 = 3100 nM [3]
Drug Info Ki = 8.75 nM [17]
Drug Info Ki = 36 nM [9]
Drug Info IC50 = 5300 nM [8]
Drug Info Ki = 35 nM [49]
Drug Info Ki = 4900 nM [47]
Drug Info Ki = 2900 nM [47]
Drug Info Ki = 2100 nM [51]
Drug Info Ki = 3200 nM [66]
Drug Info Ki = 0.29 nM [24]
Drug Info Ki = 10000 nM [40]
Drug Info Ki = 37 nM [51]
Drug Info Ki = 3.7 nM [17]
Drug Info Ki = 180 nM [50]
Drug Info Ki = 50 nM [56]
Drug Info Ki = 40 nM [13]
Drug Info Ki = 4.4 nM [24]
(9-Methyl-9H-purin-6-yl)-phenyl-amine Drug Info Ki = 6900 nM [44]
1,3-Diallyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 10000 nM [60]
1,3-Diethyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 3300 nM [60]
1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 500 nM [60]
1,3-Dipropyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 700 nM [60]
1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 130 nM [59]
1-METHYLXANTHINE Drug Info Ki = 9000 nM [60]
1-Propyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 3310 nM [11]
1H-Imidazo[4,5-c]quinolin-4-ylamine HCl Drug Info Ki = 1600 nM [51]
2'-Me-tecadenoson Drug Info Ki = 150 nM [33]
2,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info Ki = 58 nM [9]
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine Drug Info Ki = 1.56 nM [48]
2,6,8-triphenyl-9H-purine Drug Info Ki = 21 nM [24]
2,6-bis(4-tolyl)-9H-purine Drug Info Ki = 235 nM [24]
2,6-dimethyl-8-ethyl-1-deazapurine Drug Info Ki = 101 nM [28]
2,6-diphenyl-1-deazapurine Drug Info Ki = 1.2 nM [28]
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine Drug Info Ki = 0.87 nM [28]
2,6-diphenyl-8-ethyl-1-deazapurine Drug Info Ki = 2.4 nM [28]
2,6-diphenyl-8-methyl-1-deazapurine Drug Info Ki = 14 nM [28]
2,6-diphenyl-8-tButyl-1-deazapurine Drug Info Ki = 5.5 nM [28]
2,6-diphenyl-9H-purine Drug Info Ki = 4.1 nM [24]
2,6-Diphenyl-pyrimidin-4-ylamine Drug Info Ki = 25.2 nM [36]
2,6-dphenyl-8-propyl-1-deazapurine Drug Info Ki = 2.5 nM [28]
2-(1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 50 nM [38]
2-(2''-indolylethyloxy)adenosine Drug Info Ki = 197 nM [30]
2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine Drug Info Ki = 56 nM [35]
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine Drug Info Ki = 130 nM [30]
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 210 nM [30]
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 443 nM [30]
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 358 nM [30]
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine Drug Info Ki = 150 nM [30]
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine Drug Info Ki = 310 nM [30]
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine Drug Info Ki = 350 nM [30]
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine Drug Info Ki = 1820 nM [30]
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine Drug Info Ki = 253 nM [30]
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine Drug Info Ki = 145 nM [30]
2-(3''-indolylethyloxy)adenosine Drug Info Ki = 148 nM [30]
2-(3''-pyrrolylethyloxy)adenosine Drug Info Ki = 218 nM [30]
2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 350 nM [22]
2-(4-chlorophenyl)-6-phenyl-9H-purine Drug Info Ki = 27 nM [24]
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline Drug Info Ki = 0.5 nM [22]
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine Drug Info Ki = 95 nM [29]
2-(4-methoxyphenyl)-6-phenyl-9H-purine Drug Info Ki = 32 nM [24]
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline Drug Info Ki = 8000 nM [38]
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine Drug Info Ki = 282 nM [29]
2-(6-amino-8-bromo-9H-purin-9-yl)ethanol Drug Info Ki = 1500 nM [57]
2-(6-Cyclopentylamino-purin-9-yl)-ethanol Drug Info Ki = 3300 nM [44]
2-(hex-1-ynyl)-N6-methoxyadenosine Drug Info Ki = 97 nM [29]
2-Amino-4,6-di-furan-2-yl-nicotinonitrile Drug Info Ki = 12 nM [42]
2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile Drug Info Ki = 43 nM [42]
2-Amino-4,6-diphenyl-nicotinonitrile Drug Info Ki = 14 nM [42]
2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile Drug Info Ki = 3.3 nM [36]
2-Amino-4,6-diphenyl-pyrimidine Drug Info Ki = 17.7 nM [36]
2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile Drug Info Ki = 5.8 nM [42]
2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile Drug Info Ki = 12 nM [42]
2-amino-6-phenyl-4-p-tolylnicotinonitrile Drug Info Ki = 274 nM [25]
2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile Drug Info Ki = 22 nM [42]
2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide Drug Info Ki = 60 nM [41]
2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine Drug Info Ki = 230 nM [27]
2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 2041 nM [40]
2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info Ki = 270 nM [51]
2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 3205 nM [40]
2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 917 nM [40]
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 388 nM [40]
2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine Drug Info Ki = 1466 nM [40]
2-ethynyl-N6-methoxyadenosine Drug Info Ki = 25 nM [29]
2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Drug Info Ki = 12 nM [32]
2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine Drug Info Ki = 21 nM [32]
2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Drug Info Ki = 29 nM [32]
2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine Drug Info Ki = 45 nM [32]
2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine Drug Info Ki = 34 nM [51]
2-phenyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one Drug Info Ki = 203 nM [32]
2-phenyl-2H-pyrazolo[3,4-c]quinolin-4-amine Drug Info Ki = 659 nM [32]
2-phenylpropoxyadenosine Drug Info Ki = 960 nM [30]
2-tolyl-6-phenyl-9H-purine Drug Info Ki = 4 nM [24]
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine Drug Info Ki = 1280 nM [29]
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine Drug Info Ki = 2790 nM [29]
3,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info Ki = 59 nM [9]
3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one Drug Info Ki = 3336 nM [38]
3-Benzyl-7-methyl-[1,8]naphthyridin-4-ol Drug Info Ki = 4180 nM [19]
3-Benzyl-7-methyl-[1,8]naphthyridine-4-thiol Drug Info Ki = 8720 nM [19]
3-noradamantyl-1,3-dipropylxanthine Drug Info Ki = 8 nM [26]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [58]
4-(ethylthio)-6-phenyl-1,3,5-triazin-2-amine Drug Info Ki = 67 nM [25]
4-(furan-2-yl)thieno[3,2-d]pyrimidin-2-amine Drug Info Ki = 479 nM [41]
4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine Drug Info Ki = 675 nM [40]
4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile Drug Info Ki = 10.8 nM [36]
4-Bromo-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info Ki = 33 nM [9]
4-Chloro-7-methyl-2-phenyl-[1,8]naphthyridine Drug Info Ki = 1000 nM [6]
4-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info Ki = 18 nM [9]
4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide Drug Info Ki = 3000 nM [9]
4-Nitro-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info Ki = 22 nM [9]
4-tert-Butyl-N-(4-phenyl-thiazol-2-yl)-benzamide Drug Info Ki = 1360 nM [9]
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol Drug Info Ki = 7370 nM [37]
6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 4951 nM [46]
6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine Drug Info Ki = 640 nM [30]
6-guanidino-2-(3''-indolylethyloxy)adenosine Drug Info Ki = 73.6 nM [30]
7-Bromo-2-phenyl-[1,8]naphthyridin-4-ol Drug Info Ki = 1.6 nM [15]
7-Chloro-2-phenyl-[1,8]naphthyridin-4-ol Drug Info Ki = 1.62 nM [15]
7-Dimethylamino-2-phenyl-[1,8]naphthyridin-4-ol Drug Info Ki = 6.02 nM [15]
7-Methyl-2-propyl-[1,8]naphthyridin-4-ol Drug Info Ki = 61.5 nM [15]
8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine Drug Info Ki = 16000 nM [47]
8-Bromo-9-(2-butyl)-9H-adenine Drug Info Ki = 3200 nM [47]
8-Bromo-9-(3-hydroxypropyl)-9H-adenine Drug Info Ki = 1000 nM [47]
8-Bromo-9-cyclobutyl-9H-adenine Drug Info Ki = 2200 nM [47]
8-Bromo-9-cyclohexyl-9H-adenine Drug Info Ki = 4600 nM [47]
8-Bromo-9-cyclopentyl-9H-adenine Drug Info Ki = 1000 nM [47]
8-Bromo-9-ethyl-9H-adenine Drug Info Ki = 280 nM [47]
8-bromo-9-isobutyl-9H-purin-6-amine Drug Info Ki = 4900 nM [57]
8-Bromo-9-isopropyl-9H-adenine Drug Info Ki = 830 nM [47]
8-Bromo-9-methyl-9H-adenine Drug Info Ki = 570 nM [47]
8-Bromo-9-phenylethyl-9H-adenine Drug Info Ki = 12000 nM [47]
8-Bromo-9-propyl-9H-adenine Drug Info Ki = 1100 nM [47]
8-cyclohexyl-6-(4-tolyl)-2-phenyl-9H-purine Drug Info Ki = 36 nM [24]
8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 67 nM [65]
8-Phenyl-3,7-dihydro-purine-2,6-dione Drug Info Ki = 2500 nM [65]
9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 4027 nM [41]
9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 3920 nM [41]
9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 5765 nM [41]
9-Allyl-8-bromo-9H-adenine Drug Info Ki = 8400 nM [47]
9-benzyl-6-(furan-2-yl)-9H-purin-2-amine Drug Info Ki = 3324 nM [41]
9-Benzyl-8-bromo-9H-adenine Drug Info Ki = 6700 nM [47]
9-Cyclobutyl-9H-adenine Drug Info Ki = 8700 nM [47]
9-Cyclopentyl-9H-adenine Drug Info Ki = 1800 nM [44]
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine Drug Info Ki = 1280 nM [10]
9-Ethyl-9H-adenine Drug Info Ki = 7400 nM [47]
9-Isopropyl-9H-adenine Drug Info Ki = 4300 nM [47]
9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine Drug Info Ki = 0.4 nM [21]
9-Methyl-9H-adenine Drug Info IC50 = 14700 nM [14]
9-Phenyl-9H-purin-6-ylamine Drug Info Ki = 19000 nM [44]
9-Propyl-9H-adenine Drug Info Ki = 9400 nM [47]
A-987306 Drug Info IC50 = 6.7 nM [45]
ARISTEROMYCIN Drug Info Ki = 6260 nM [4]
BRL-61063 Drug Info IC50 = 170 nM [64]
CVT-6883 Drug Info Ki = 1940 nM [49]
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine Drug Info Ki = 3000 nM [18]
Cyclohexyl-(9-ethyl-9H-purin-6-yl)-amine Drug Info Ki = 2000 nM [44]
Cyclohexyl-(9-methyl-9H-purin-6-yl)-amine Drug Info Ki = 940 nM [44]
Cyclopentyl-(9-cyclopentyl-9H-purin-6-yl)-amine Drug Info Ki = 1200 nM [44]
Cyclopentyl-(9-ethyl-9H-purin-6-yl)-amine Drug Info Ki = 440 nM [44]
Cyclopentyl-(9-methyl-9H-purin-6-yl)-amine Drug Info Ki = 540 nM [44]
Cyclopentyl-(9-phenyl-9H-purin-6-yl)-amine Drug Info Ki = 8700 nM [44]
DEPX Drug Info IC50 = 48 nM [61]
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate Drug Info Ki = 72.9 nM [54]
FK-453 Drug Info IC50 = 17.2 nM [54]
FK-838 Drug Info Ki = 6.61 nM [54]
FR-166124 Drug Info IC50 = 15 nM [1]
GNF-PF-2224 Drug Info Ki = 0.5 nM [52]
GNF-PF-2700 Drug Info Ki = 1330 nM [57]
GW-328267 Drug Info Ki = 369 nM [16]
Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide Drug Info Ki = 109 nM [17]
isobutylmethylxanthine Drug Info Ki = 50 nM [63]
Istradefylline Drug Info Ki = 230 nM [31]
KF-17837 Drug Info IC50 = 62 nM [8]
Kuanoniamine D Drug Info Ki = 2940 nM [67]
LUF-5417 Drug Info Ki = 32 nM [54]
LUF-5433 Drug Info Ki = 76 nM [54]
LUF-5737 Drug Info Ki = 8.87 nM [17]
LUF-5767 Drug Info Ki = 2.22 nM [17]
LUF-5816 Drug Info Ki = 0.62 nM [28]
LUF-5853 Drug Info Ki = 11 nM [36]
LUF-5956 Drug Info Ki = 0.82 nM [24]
LUF-5957 Drug Info IC50 = 477 nM [24]
LUF-5978 Drug Info Ki = 0.55 nM [28]
METHYLTHIOADENOSINE Drug Info IC50 = 15100 nM [14]
METRIFUDIL Drug Info Ki = 98 nM [2]
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info Ki = 2730 nM [18]
N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine Drug Info Ki = 4470 nM [18]
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide Drug Info Ki = 14.8 nM [17]
N-(2,6-diphenylpyrimidin-4-yl)benzamide Drug Info Ki = 671 nM [17]
N-(2,6-diphenylpyrimidin-4-yl)butyramide Drug Info Ki = 17.6 nM [17]
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide Drug Info Ki = 11.1 nM [17]
N-(2,6-diphenylpyrimidin-4-yl)propionamide Drug Info Ki = 9.5 nM [17]
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide Drug Info Ki = 358 nM [53]
N-(4,5-diphenylpyrimidin-2-yl)acetamide Drug Info Ki = 483 nM [17]
N-(4,6-diphenylpyrimidin-2-yl)-3-chlorobenzamide Drug Info Ki = 368 nM [17]
N-(4,6-diphenylpyrimidin-2-yl)-3-methylbutyramide Drug Info Ki = 25.1 nM [17]
N-(4,6-diphenylpyrimidin-2-yl)benzamide Drug Info Ki = 309 nM [17]
N-(4,6-diphenylpyrimidin-2-yl)propionamide Drug Info Ki = 46.4 nM [17]
N-(4-Phenyl-thiazol-2-yl)-benzamide Drug Info Ki = 39 nM [9]
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide Drug Info Ki = 9.51 nM [54]
N6-((+/-)-endo-norborn-2-yl)adenosine Drug Info Ki = 0.54 nM [48]
N6-CYCLOPENTYLADENOSINE Drug Info Ki = 810 nM [33]
N6-methoxy-2-phenylethynyladenosine Drug Info Ki = 1210 nM [29]
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine Drug Info Ki = 437 nM [29]
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine Drug Info Ki = 1870 nM [29]
N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine Drug Info Ki = 1380 nM [29]
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine Drug Info Ki = 730 nM [29]
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine Drug Info Ki = 1190 nM [29]
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine Drug Info Ki = 22 nM [29]
N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine Drug Info Ki = 294 nM [34]
N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine Drug Info Ki = 571 nM [34]
P-IODOAMPHETAMINE Drug Info Ki = 1.2 nM [12]
PD-115199 Drug Info Ki = 13.9 nM [20]
PD-81723 Drug Info Ki = 11000 nM [43]
Pentanoic acid (4,6-diphenylpyrimidin-2-yl)amide Drug Info Ki = 27.6 nM [17]
Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol Drug Info Ki = 16500 nM [39]
Phenyl-(9-phenyl-9H-purin-6-yl)-amine Drug Info Ki = 6900 nM [44]
PSB-0788 Drug Info Ki = 386 nM [49]
PSB-601 Drug Info Ki = 260 nM [49]
R-N6-(phenylisopropyl)adenosine Drug Info Ki = 2 nM [30]
SCH-442416 Drug Info Ki = 1815 nM [7]
SCH-63390 Drug Info Ki = 504 nM [68]
ST-1535 Drug Info Ki = 71.8 nM [21]
Tonapofylline Drug Info Ki = 1.3 nM [54]
VUF-8507 Drug Info Ki = 3200 nM [5]
[3H]CCPA Drug Info Ki = 650 nM [33]
[3H]NECA Drug Info Ki = 8.2 nM [62]
[3H]OSIP339391 Drug Info Ki = 450 nM [57]
References
REF 1 Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist. Bioorg Med Chem Lett. 1999 Jul 19;9(14):1979-84.
REF 2 N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. J Med Chem. 1999 Sep 9;42(18):3463-77.
REF 3 Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali. J Nat Prod. 2000 Mar;63(3):318-21.
REF 4 Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. J Med Chem. 2000 Jun 1;43(11):2196-203.
REF 5 Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. J Med Chem. 2000 Jun 1;43(11):2227-38.
REF 6 A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives. J Med Chem. 2000 Jul 27;43(15):2814-23.
REF 7 Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using p... J Med Chem. 2000 Nov 16;43(23):4359-62.
REF 8 2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic gluc... J Med Chem. 2001 Jan 18;44(2):170-9.
REF 9 Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor. Bioorg Med Chem Lett. 2001 Aug 6;11(15):2017-9.
REF 10 Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1931-4.
REF 11 Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. J Med Chem. 2002 May 23;45(11):2131-8.
REF 12 Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective a... J Med Chem. 1992 Oct 30;35(22):4143-9.
REF 13 Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic... J Med Chem. 2004 Feb 12;47(4):1031-43.
REF 14 Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique aden... J Med Chem. 2004 Apr 22;47(9):2243-55.
REF 15 Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. J Med Chem. 2004 Jun 3;47(12):3019-31.
REF 16 Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor. J Med Chem. 2004 Jul 29;47(16):4041-53.
REF 17 2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. J Med Chem. 2004 Dec 16;47(26):6529-40.
REF 18 Reversine and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem. 2005 Jul 28;48(15):4910-8.
REF 19 1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4604-10.
REF 20 (E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists. J Med Chem. 1992 Jun 12;35(12):2342-5.
REF 21 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 pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.
REF 22 2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database search... J Med Chem. 2005 Dec 29;48(26):8253-60.
REF 23 Adenosine receptors as therapeutic targets. Nat Rev Drug Discov. 2006 Mar;5(3):247-64.
REF 24 2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. J Med Chem. 2006 May 18;49(10):2861-7.
REF 25 Identification of non-furan containing A2A antagonists using database mining and molecular similarity approaches. Bioorg Med Chem Lett. 2006 Dec 1;16(23):5993-7.
REF 26 Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7119-31.
REF 27 2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. J Med Chem. 2006 Dec 14;49(25):7373-83.
REF 28 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34.
REF 29 N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor. J Med Chem. 2007 Mar 22;50(6):1222-30.
REF 30 Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor. J Med Chem. 2007 Apr 19;50(8):1810-27.
REF 31 N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 an... Bioorg Med Chem. 2007 Jul 15;15(14):5003-17.
REF 32 New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluati... J Med Chem. 2007 Aug 23;50(17):4061-74.
REF 33 5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 ... Bioorg Med Chem. 2008 Jan 1;16(1):336-53.
REF 34 N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A... Eur J Med Chem. 2008 Aug;43(8):1639-47.
REF 35 Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. J Med Chem. 2008 Feb 14;51(3):400-6.
REF 36 A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. Bioorg Med Chem. 2008 Mar 15;16(6):2741-52.
REF 37 Synthesis of eudistomin D analogues and its effects on adenosine receptors. Bioorg Med Chem. 2008 Apr 1;16(7):3825-30.
REF 38 Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists. J Med Chem. 2008 Mar 27;51(6):1764-70.
REF 39 Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2916-9.
REF 40 Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3.
REF 41 Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpu... Bioorg Med Chem Lett. 2008 May 1;18(9):2924-9.
REF 42 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem. 2008 Aug 14;51(15):4449-55.
REF 43 Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of t... J Med Chem. 2008 Sep 25;51(18):5875-9.
REF 44 N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor. J Med Chem. 1991 Sep;34(9):2877-82.
REF 45 cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
REF 46 Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines. J Med Chem. 2009 Jan 8;52(1):33-47.
REF 47 8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands. Bioorg Med Chem. 2009 Apr 1;17(7):2812-22.
REF 48 N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine recept... J Med Chem. 2009 Apr 23;52(8):2393-406.
REF 49 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with... J Med Chem. 2009 Jul 9;52(13):3994-4006.
REF 50 2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a new scaffold to obtain potent and selective human A3 adenosine receptor antagonists: new insights into ... J Med Chem. 2009 Dec 10;52(23):7640-52.
REF 51 1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. J Med Chem. 1991 Mar;34(3):1202-6.
REF 52 Synthesis and theoretical studies on energetics of novel N- and O- perfluoroalkyl triazole tagged thienopyrimidines--their potential as adenosine r... Eur J Med Chem. 2010 May;45(5):1739-45.
REF 53 Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1697-700.
REF 54 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.
REF 55 Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. J Med Chem. 2010 Apr 22;53(8):3028-37.
REF 56 Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists. Bioorg Med Chem. 2010 May 1;18(9):3078-87.
REF 57 Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods. Eur J Med Chem. 2010 Aug;45(8):3459-71.
REF 58 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 59 Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-,... J Med Chem. 1989 Jun;32(6):1231-7.
REF 60 Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. J Med Chem. 1988 Oct;31(10):2034-9.
REF 61 125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors. J Med Chem. 1988 Apr;31(4):745-51.
REF 62 Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. J Med Chem. 1988 Jun;31(6):1179-83.
REF 63 Adenosine receptors: targets for future drugs. J Med Chem. 1982 Mar;25(3):197-207.
REF 64 Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. J Med Chem. 1994 Feb 18;37(4):476-85.
REF 65 Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationshi... J Med Chem. 1993 Oct 29;36(22):3341-9.
REF 66 Adenosine-1 active ligands: cirsimarin, a flavone glycoside from Microtea debilis. J Nat Prod. 1997 Jun;60(6):638-41.
REF 67 Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp. J Nat Prod. 1998 Feb;61(2):301-5.
REF 68 Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A... J Med Chem. 1998 Jun 4;41(12):2126-33.
REF 69 Medicinal chemistry of adenosine A1 receptor ligands. Curr Top Med Chem. 2003;3(4):355-67.
REF 70 Recent advances in the research of HIV-1 RNase H inhibitors. Mini Rev Med Chem. 2008 Oct;8(12):1243-51.
REF 71 Effects of uric acid and caffeine on A1 adenosine receptor binding in developing rat brain. Pharmacol Biochem Behav. 1990 Apr;35(4):791-5.

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