Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T36059 | ||||
Target Name | Adenosine A3 receptor (ADORA3) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | Adenosine | Drug Info | Ki = 290 nM | [44] | |
Drug Info | IC50 = 5 nM | [14] | |||
Drug Info | IC50 = 613 nM | [14] | |||
(+)-BUTACLAMOL | Drug Info | IC50 = 8.9 nM | [14] | ||
1,2-dihydro-2-oxoquinazoline-4-carboxyanilide | Drug Info | IC50 = 238 nM | [27] | ||
1-(2-(diethylamino)quinazolin-4-yl)-3-phenylurea | Drug Info | Ki = 180 nM | [18] | ||
1-Allyl-3,7-dihydro-purine-2,6-dione | Drug Info | Ki = 16100 nM | [5] | ||
1-Benzyl-1H-1,3,4b,9-tetraaza-fluorene-2,4-dione | Drug Info | Ki = 370 nM | [6] | ||
1-Benzyl-3-methyl-3,7-dihydro-purine-2,6-dione | Drug Info | Ki = 4440 nM | [5] | ||
1-Butyl-3,7-dihydro-purine-2,6-dione | Drug Info | Ki = 4.61 nM | [5] | ||
1-Cyclopentyl-3,7-dihydro-purine-2,6-dione | Drug Info | Ki = 639 nM | [5] | ||
1-Phenethyl-3,7-dihydro-purine-2,6-dione | Drug Info | Ki = 7510 nM | [5] | ||
1-phenyl-3-(2-(pyridin-2-yl)quinazolin-4-yl)urea | Drug Info | Ki = 490 nM | [18] | ||
1-phenyl-3-(2-(pyridin-3-yl)quinazolin-4-yl)urea | Drug Info | Ki = 51 nM | [18] | ||
1-phenyl-3-(3-(pyridin-2-yl)isoquinolin-1-yl)urea | Drug Info | Ki = 76 nM | [18] | ||
1-phenyl-3-(quinazolin-4-yl)urea | Drug Info | Ki = 1200 nM | [18] | ||
1-Prop-2-ynyl-3,7-dihydro-purine-2,6-dione | Drug Info | Ki = 3080 nM | [5] | ||
1-Propyl-3,7-dihydro-purine-2,6-dione | Drug Info | Ki = 2370 nM | [5] | ||
2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine | Drug Info | Ki = 417 nM | [32] | ||
2,6,8-triphenyl-9H-purine | Drug Info | Ki = 49 nM | [17] | ||
2,6-bis(4-chlorophenyl)-9H-purine | Drug Info | Ki = 68 nM | [17] | ||
2,6-bis(4-methoxyphenyl)-9H-purine | Drug Info | Ki = 165 nM | [17] | ||
2,6-bis(4-tolyl)-9H-purine | Drug Info | Ki = 9.3 nM | [17] | ||
2,6-diphenyl-1-deazapurine | Drug Info | Ki = 180 nM | [21] | ||
2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine | Drug Info | Ki = 171 nM | [21] | ||
2,6-diphenyl-8-ethyl-1-deazapurine | Drug Info | Ki = 8.5 nM | [21] | ||
2,6-diphenyl-8-methyl-1-deazapurine | Drug Info | Ki = 61 nM | [21] | ||
2,6-diphenyl-8-tButyl-1-deazapurine | Drug Info | Ki = 115 nM | [21] | ||
2,6-diphenyl-9H-purine | Drug Info | Ki = 38 nM | [17] | ||
2,6-dphenyl-8-propyl-1-deazapurine | Drug Info | Ki = 69 nM | [21] | ||
2-(1H-benzo[d]imidazol-2-yl)quinoxaline | Drug Info | Ki = 763 nM | [29] | ||
2-(1H-imidazo[4,5-c]pyridin-2-yl)quinoxaline | Drug Info | Ki = 168 nM | [16] | ||
2-(2''-indolylethyloxy)adenosine | Drug Info | Ki = 513 nM | [23] | ||
2-(3''(5''-chloro-indolyl)ethyloxy)adenosine | Drug Info | Ki = 296 nM | [23] | ||
2-(3''(7''-bromo-indolyl)ethyloxy)adenosine | Drug Info | Ki = 142 nM | [23] | ||
2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine | Drug Info | Ki = 260 nM | [23] | ||
2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine | Drug Info | Ki = 234 nM | [23] | ||
2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine | Drug Info | Ki = 490 nM | [23] | ||
2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine | Drug Info | Ki = 120 nM | [23] | ||
2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine | Drug Info | Ki = 110 nM | [23] | ||
2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine | Drug Info | Ki = 360 nM | [23] | ||
2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine | Drug Info | Ki = 90 nM | [23] | ||
2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine | Drug Info | Ki = 92.3 nM | [23] | ||
2-(3''-(benzoimidazole-1''-yl)ethyloxy)adenosine | Drug Info | Ki = 2070 nM | [23] | ||
2-(3''-(benzotriazole-1''-yl)ethyloxy)adenosine | Drug Info | Ki = 1920 nM | [23] | ||
2-(3''-indolylethyloxy)adenosine | Drug Info | Ki = 232 nM | [23] | ||
2-(3''-pyrrolylethyloxy)adenosine | Drug Info | Ki = 104 nM | [23] | ||
2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline | Drug Info | Ki = 140 nM | [16] | ||
2-(4-chlorophenyl)-6-phenyl-9H-purine | Drug Info | Ki = 94 nM | [17] | ||
2-(4-ethylthiobenzimidazol-2-yl)quinoxaline | Drug Info | Ki = 955 nM | [16] | ||
2-(4-hydroxypent-1-yl)-N6-methoxyadenosine | Drug Info | Ki = 5.4 nM | [22] | ||
2-(4-methoxyphenyl)-6-phenyl-9H-purine | Drug Info | Ki = 4 nM | [17] | ||
2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline | Drug Info | Ki = 26 nM | [29] | ||
2-(4-nitro-1H-benzo[d]imidazol-2-yl)quinoxaline | Drug Info | Ki = 879 nM | [16] | ||
2-(5-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline | Drug Info | Ki = 632 nM | [16] | ||
2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine | Drug Info | Ki = 4.1 nM | [22] | ||
2-(hex-1-ynyl)-N6-methoxyadenosine | Drug Info | Ki = 2.8 nM | [22] | ||
2-acetylaminoquinazoline-4-carboxyanilide | Drug Info | IC50 = 140 nM | [27] | ||
2-aminoquinazoline-4-carboxy-(4-bromophenyl)amide | Drug Info | Ki = 550 nM | [27] | ||
2-aminoquinazoline-4-carboxyanilide | Drug Info | Ki = 350 nM | [27] | ||
2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine | Drug Info | Ki = 10.8 nM | [20] | ||
2-benzoylaminoquinazoline-4-carboxyanilide | Drug Info | Ki = 182 nM | [27] | ||
2-benzyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one | Drug Info | Ki = 74.5 nM | [25] | ||
2-chloro-2'-C-methyl-tecadenoson | Drug Info | Ki = 18900 nM | [26] | ||
2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine | Drug Info | Ki = 1813 nM | [30] | ||
2-ethynyl-N6-methoxyadenosine | Drug Info | Ki = 23 nM | [22] | ||
2-Phenyl-2H-pyrazolo[4,3-c]quinoline | Drug Info | Ki = 212 nM | [13] | ||
2-phenyl-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one | Drug Info | Ki = 725 nM | [34] | ||
2-phenylpropoxyadenosine | Drug Info | Ki = 66 nM | [23] | ||
2-tolyl-6-phenyl-9H-purine | Drug Info | Ki = 9.4 nM | [17] | ||
2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine | Drug Info | Ki = 3 nM | [22] | ||
2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine | Drug Info | Ki = 4.4 nM | [22] | ||
3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one | Drug Info | Ki = 125 nM | [29] | ||
3-Methyl-1-phenethyl-3,7-dihydro-purine-2,6-dione | Drug Info | Ki = 6880 nM | [5] | ||
3-noradamantyl-1,3-dipropylxanthine | Drug Info | Ki = 4390 nM | [19] | ||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | Ki < 1000 nM | [38] | ||
4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one | Drug Info | Ki = 12300 nM | [43] | ||
4-Methoxy-2-phenyl-2H-pyrazolo[4,3-c]quinoline | Drug Info | Ki = 166 nM | [13] | ||
4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide | Drug Info | Ki = 79 nM | [3] | ||
5,6,7-Trimethyl-2-p-tolyl-chromen-4-one | Drug Info | Ki = 4480 nM | [42] | ||
5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol | Drug Info | Ki = 2050 nM | [28] | ||
5,7-diphenyl-3H-imidazo[4,5-b]pyridin-2-ol | Drug Info | Ki = 262 nM | [21] | ||
5-Butyl-8-phenyl-3H-[1,2,4]triazolo[5,1-i]purine | Drug Info | IC50 = 0.25 nM | [8] | ||
6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine | Drug Info | Ki = 30 nM | [23] | ||
6-guanidino-2-(3''-indolylethyloxy)adenosine | Drug Info | Ki = 90 nM | [23] | ||
6-Hydroxy-5,7-dimethyl-beta-carboline | Drug Info | Ki = 17700 nM | [28] | ||
8-Bromo-9-(3-hydroxypropyl)-9H-adenine | Drug Info | Ki = 3200 nM | [31] | ||
8-Bromo-9-(sec-butyl)-9H-adenine | Drug Info | Ki = 15000 nM | [31] | ||
8-Bromo-9-cyclobutyl-9H-adenine | Drug Info | Ki = 6200 nM | [31] | ||
8-Bromo-9-cyclohexyl-9H-adenine | Drug Info | Ki = 11000 nM | [31] | ||
8-Bromo-9-cyclopentyl-9H-adenine | Drug Info | Ki = 4200 nM | [31] | ||
8-bromo-9-isobutyl-9H-purin-6-amine | Drug Info | Ki = 15000 nM | [37] | ||
8-Bromo-9-isopropyl-9H-adenine | Drug Info | Ki = 15000 nM | [31] | ||
8-Hydroxy-5,7,9-trimethyl-delta-carboline | Drug Info | Ki = 13300 nM | [28] | ||
8-Hydroxy-7,9-dimethyl-delta-carboline | Drug Info | Ki = 4430 nM | [28] | ||
8-PHENYL THEOPHYLLINE | Drug Info | Ki = 500 nM | [41] | ||
8-propyl-2,6-diphenyl-9H-purine | Drug Info | Ki = 17 nM | [17] | ||
9-Cyclopentyl-9H-adenine | Drug Info | Ki = 13000 nM | [31] | ||
9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine | Drug Info | Ki = 86 nM | [4] | ||
9H-purine derivative | Drug Info | IC50 = 14 nM | [14] | ||
BEMESETRON | Drug Info | IC50 = 9.3 nM | [14] | ||
CIRSIMARITIN | Drug Info | Ki = 1720 nM | [42] | ||
CVT-6883 | Drug Info | Ki = 1070 nM | [33] | ||
Cyclohexyl-(2-phenoxy-9H-purin-6-yl)-amine | Drug Info | Ki = 47 nM | [12] | ||
Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine | Drug Info | Ki = 134 nM | [12] | ||
DIZOCILPINE | Drug Info | IC50 = 2 nM | [14] | ||
Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate | Drug Info | Ki = 206 nM | [36] | ||
flavone | Drug Info | Ki = 16900 nM | [42] | ||
Galangin | Drug Info | Ki = 3150 nM | [42] | ||
GNF-PF-2224 | Drug Info | Ki = 1300 nM | [40] | ||
GW-328267 | Drug Info | Ki = 92 nM | [9] | ||
Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide | Drug Info | Ki = 392 nM | [10] | ||
isobutylmethylxanthine | Drug Info | Ki = 50 nM | [41] | ||
L-249313 | Drug Info | Ki = 13 nM | [2] | ||
LUF-5417 | Drug Info | Ki = 82 nM | [36] | ||
LUF-5433 | Drug Info | Ki = 670 nM | [36] | ||
LUF-5767 | Drug Info | Ki = 147 nM | [10] | ||
LUF-5816 | Drug Info | Ki = 6.9 nM | [21] | ||
LUF-5956 | Drug Info | Ki = 9.5 nM | [17] | ||
LUF-5957 | Drug Info | Ki = 200 nM | [17] | ||
LUF-5962 | Drug Info | Ki = 35 nM | [17] | ||
LUF-5978 | Drug Info | Ki = 25 nM | [21] | ||
LUF-5980 | Drug Info | Ki = 7.3 nM | [21] | ||
LUF-5981 | Drug Info | Ki = 637 nM | [21] | ||
MESULERGINE | Drug Info | IC50 = 1.9 nM | [14] | ||
METHOCTRAMINE | Drug Info | IC50 = 34 nM | [14] | ||
METHYLTHIOADENOSINE | Drug Info | Ki = 680 nM | [7] | ||
METRIFUDIL | Drug Info | Ki = 47 nM | [11] | ||
MRS1041 | Drug Info | Ki = 18200 nM | [43] | ||
MRS928 | Drug Info | Ki = 1210 nM | [42] | ||
N*2*-Benzyl-N*6*-cyclohexyl-9H-purine-2,6-diamine | Drug Info | Ki = 920 nM | [12] | ||
N*6*-Cyclohexyl-N*2*-ethyl-9H-purine-2,6-diamine | Drug Info | Ki = 1120 nM | [12] | ||
N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine | Drug Info | Ki = 51 nM | [12] | ||
N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine | Drug Info | Ki = 340 nM | [12] | ||
N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide | Drug Info | Ki = 447 nM | [10] | ||
N-(2,6-diphenylpyrimidin-4-yl)acetamide | Drug Info | Ki = 6.88 nM | [10] | ||
N-(2,6-diphenylpyrimidin-4-yl)benzamide | Drug Info | Ki = 1300 nM | [10] | ||
N-(2,6-diphenylpyrimidin-4-yl)butyramide | Drug Info | Ki = 167 nM | [10] | ||
N-(2,6-diphenylpyrimidin-4-yl)isobutyramide | Drug Info | Ki = 267 nM | [10] | ||
N-(2,6-diphenylpyrimidin-4-yl)propionamide | Drug Info | Ki = 22.4 nM | [10] | ||
N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide | Drug Info | Ki = 333 nM | [35] | ||
N-(4,5-diphenylpyrimidin-2-yl)acetamide | Drug Info | Ki = 237 nM | [10] | ||
N-(4,6-diphenylpyrimidin-2-yl)-4-chlorobenzamide | Drug Info | Ki = 3280 nM | [10] | ||
N-(4,6-diphenylpyrimidin-2-yl)propionamide | Drug Info | Ki = 547 nM | [10] | ||
N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide | Drug Info | Ki = 354 nM | [36] | ||
N6-((+/-)-endo-norborn-2-yl)adenosine | Drug Info | Ki = 101 nM | [32] | ||
N6-(3-Iodobenzyl)-2'-O-methyladenosine | Drug Info | IC50 = 1.7 nM | [24] | ||
N6-CYCLOPENTYLADENOSINE | Drug Info | Ki = 97 nM | [15] | ||
N6-methoxy-2-phenylethynyladenosine | Drug Info | Ki = 3.8 nM | [22] | ||
N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine | Drug Info | Ki = 2.3 nM | [22] | ||
N6-methoxy-2-[(3-pyridinyl)ethynyl]-adenosine | Drug Info | Ki = 7.9 nM | [22] | ||
N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine | Drug Info | Ki = 4.3 nM | [22] | ||
N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine | Drug Info | Ki = 5.9 nM | [22] | ||
N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine | Drug Info | Ki = 39 nM | [22] | ||
N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine | Drug Info | Ki = 6 nM | [22] | ||
N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine | Drug Info | Ki = 13 nM | [22] | ||
NIPECOTIC ACID | Drug Info | IC50 = 10.1 nM | [14] | ||
NITD609 | Drug Info | IC50 = 8300 nM | [39] | ||
NSC-407228 | Drug Info | Ki = 3400 nM | [42] | ||
R-N6-(phenylisopropyl)adenosine | Drug Info | Ki = 8.7 nM | [23] | ||
REVERSINE | Drug Info | Ki = 660 nM | [12] | ||
SB-298 | Drug Info | Ki = 422 nM | [33] | ||
SEROTONIN | Drug Info | IC50 = 79 nM | [14] | ||
Tonapofylline | Drug Info | Ki = 10000 nM | [36] | ||
VUF-8504 | Drug Info | Ki = 17 nM | [18] | ||
VUF-8507 | Drug Info | Ki = 200 nM | [18] | ||
[3H]CCPA | Drug Info | Ki = 18800 nM | [26] | ||
[3H]kainate | Drug Info | IC50 = 77 nM | [14] | ||
[3H]NECA | Drug Info | Ki = 113 nM | [1] | ||
[3H]OSIP339391 | Drug Info | Ki = 450 nM | [37] | ||
References | |||||
REF 1 | 5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors. J Med Chem. 1999 Apr 22;42(8):1384-92. | ||||
REF 2 | The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family. Bioorg Med Chem Lett. 2000 Jan 3;10(1):31-4. | ||||
REF 3 | 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 4 | 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 5 | 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 6 | Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists. J Med Chem. 2002 Aug 1;45(16):3337-44. | ||||
REF 7 | 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 8 | Facile synthesis of fused 1,2,4-triazolo[1,5-c]pyrimidine derivatives as human adenosine A3 receptor ligands. Bioorg Med Chem Lett. 2004 May 17;14(10):2443-6. | ||||
REF 9 | 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 10 | 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 11 | (N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists. J Med Chem. 2005 Mar 24;48(6):1745-58. | ||||
REF 12 | 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 13 | New 2-arylpyrazolo[4,3-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. J Med Chem. 2005 Jul 28;48(15):5001-8. | ||||
REF 14 | 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 15 | Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprote... J Med Chem. 2005 Dec 29;48(26):8103-7. | ||||
REF 16 | 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 17 | 2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. J Med Chem. 2006 May 18;49(10):2861-7. | ||||
REF 18 | Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models. J Med Chem. 2006 Jul 13;49(14):4085-97. | ||||
REF 19 | 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 20 | 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 21 | 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34. | ||||
REF 22 | 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 23 | 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 24 | Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands. Bioorg Med Chem. 2007 Aug 15;15(16):5440-7. | ||||
REF 25 | 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 26 | 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 27 | Scouting human A3 adenosine receptor antagonist binding mode using a molecular simplification approach: from triazoloquinoxaline to a pyrimidine sk... J Med Chem. 2007 Dec 27;50(26):6596-606. | ||||
REF 28 | Synthesis of eudistomin D analogues and its effects on adenosine receptors. Bioorg Med Chem. 2008 Apr 1;16(7):3825-30. | ||||
REF 29 | 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 30 | 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 31 | 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 32 | 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 33 | 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 34 | 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 35 | 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 36 | 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 37 | 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 38 | 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 39 | Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80. | ||||
REF 40 | Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands. Bioorg Med Chem. 2010 Nov 15;18(22):7890-9. | ||||
REF 41 | Adenosine receptors: targets for future drugs. J Med Chem. 1982 Mar;25(3):197-207. | ||||
REF 42 | Interactions of flavonoids and other phytochemicals with adenosine receptors. J Med Chem. 1996 Feb 2;39(3):781-8. | ||||
REF 43 | Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301. | ||||
REF 44 | Medicinal chemistry of adenosine A3 receptor ligands. Curr Top Med Chem. 2003;3(4):445-62. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.