Page last updated: 2024-08-07 15:51:42
Adenosine receptor A3
An adenosine receptor A3 that is encoded in the genome of human. [PRO:DAN]
Synonyms
Research
Bioassay Publications (218)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (0.46) | 18.7374 |
| 1990's | 17 (7.80) | 18.2507 |
| 2000's | 99 (45.41) | 29.6817 |
| 2010's | 75 (34.40) | 24.3611 |
| 2020's | 26 (11.93) | 2.80 |
Compounds (180)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 9-ethyladenine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| taxifolin | Homo sapiens (human) | Ki | 34.1000 | 1 | 1 |
| 1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | Ki | 2.0839 | 36 | 38 |
| 1,3-dipropyl-8-(4-sulfophenyl)xanthine | Homo sapiens (human) | Ki | 0.1830 | 2 | 2 |
| 3-methylcholanthrene | Homo sapiens (human) | IC50 | 5.5440 | 1 | 0 |
| 3-methylcholanthrene | Homo sapiens (human) | Ki | 3.1340 | 1 | 0 |
| enprofylline | Homo sapiens (human) | Ki | 125.3000 | 2 | 2 |
| 4-nonylphenol | Homo sapiens (human) | IC50 | 1.9150 | 1 | 0 |
| 4-nonylphenol | Homo sapiens (human) | Ki | 1.0820 | 1 | 0 |
| 8-(4-sulfophenyl)theophylline | Homo sapiens (human) | Ki | 8.4450 | 2 | 2 |
| 8-cyclopentyl-1,3-dimethylxanthine | Homo sapiens (human) | Ki | 1.3000 | 1 | 1 |
| 8-phenyltheophylline | Homo sapiens (human) | IC50 | 1.2500 | 1 | 1 |
| theophylline | Homo sapiens (human) | Ki | 54.8657 | 20 | 20 |
| amiodarone | Homo sapiens (human) | IC50 | 17.5470 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 9.9180 | 1 | 0 |
| astemizole | Homo sapiens (human) | IC50 | 29.1200 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 16.4610 | 1 | 0 |
| benzbromarone | Homo sapiens (human) | IC50 | 5.2220 | 1 | 0 |
| benzbromarone | Homo sapiens (human) | Ki | 2.9520 | 1 | 0 |
| bithionol | Homo sapiens (human) | IC50 | 0.8290 | 1 | 0 |
| bithionol | Homo sapiens (human) | Ki | 0.4680 | 1 | 0 |
| caffeine | Homo sapiens (human) | Ki | 34.9750 | 12 | 12 |
| candesartan | Homo sapiens (human) | IC50 | 1.2199 | 1 | 0 |
| candesartan | Homo sapiens (human) | Ki | 0.6895 | 1 | 0 |
| celecoxib | Homo sapiens (human) | IC50 | 24.6220 | 1 | 0 |
| celecoxib | Homo sapiens (human) | Ki | 13.9170 | 1 | 0 |
| cgs 15943 | Homo sapiens (human) | IC50 | 0.4060 | 1 | 1 |
| cgs 15943 | Homo sapiens (human) | Ki | 4.9631 | 18 | 18 |
| ciglitazone | Homo sapiens (human) | IC50 | 3.0470 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | Ki | 1.7220 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 4.7520 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 2.6860 | 1 | 0 |
| disulfiram | Homo sapiens (human) | IC50 | 0.3560 | 1 | 0 |
| disulfiram | Homo sapiens (human) | Ki | 0.2010 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 3.1953 | 1 | 0 |
| ebastine | Homo sapiens (human) | Ki | 1.8061 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 3.2490 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 1.8360 | 1 | 0 |
| felodipine | Homo sapiens (human) | IC50 | 1.0570 | 1 | 0 |
| felodipine | Homo sapiens (human) | Ki | 0.5970 | 1 | 0 |
| fenofibrate | Homo sapiens (human) | IC50 | 5.7010 | 1 | 0 |
| fenofibrate | Homo sapiens (human) | Ki | 3.2220 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 11.9350 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 6.7460 | 1 | 0 |
| 1-(5-isoquinolinesulfonyl)piperazine | Homo sapiens (human) | Ki | 25.0000 | 1 | 1 |
| haloprogin | Homo sapiens (human) | IC50 | 0.2230 | 1 | 0 |
| haloprogin | Homo sapiens (human) | Ki | 0.1260 | 1 | 0 |
| hexachlorophene | Homo sapiens (human) | IC50 | 0.6389 | 1 | 0 |
| hexachlorophene | Homo sapiens (human) | Ki | 0.3611 | 1 | 0 |
| iodoquinol | Homo sapiens (human) | IC50 | 0.9330 | 1 | 0 |
| iodoquinol | Homo sapiens (human) | Ki | 0.5270 | 1 | 0 |
| miconazole | Homo sapiens (human) | IC50 | 2.8110 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 1.5890 | 1 | 0 |
| mitotane | Homo sapiens (human) | IC50 | 7.4450 | 1 | 0 |
| mitotane | Homo sapiens (human) | Ki | 4.2080 | 1 | 0 |
| nicardipine | Homo sapiens (human) | Ki | 3.2500 | 1 | 1 |
| nifedipine | Homo sapiens (human) | IC50 | 7.2140 | 1 | 0 |
| nifedipine | Homo sapiens (human) | Ki | 7.6645 | 3 | 3 |
| nimodipine | Homo sapiens (human) | Ki | 8.4700 | 1 | 1 |
| nisoldipine | Homo sapiens (human) | IC50 | 7.1200 | 1 | 0 |
| nisoldipine | Homo sapiens (human) | Ki | 4.0240 | 1 | 0 |
| nitrendipine | Homo sapiens (human) | Ki | 8.3000 | 1 | 1 |
| propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
| rabeprazole | Homo sapiens (human) | IC50 | 3.2190 | 1 | 0 |
| rabeprazole | Homo sapiens (human) | Ki | 1.8200 | 1 | 0 |
| sulconazole | Homo sapiens (human) | IC50 | 2.6280 | 1 | 0 |
| sulconazole | Homo sapiens (human) | Ki | 1.4850 | 1 | 0 |
| troglitazone | Homo sapiens (human) | IC50 | 5.2080 | 1 | 0 |
| troglitazone | Homo sapiens (human) | Ki | 2.9430 | 1 | 0 |
| 8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 13.7741 | 10 | 10 |
| ici 204,219 | Homo sapiens (human) | IC50 | 1.3630 | 1 | 0 |
| ici 204,219 | Homo sapiens (human) | Ki | 0.7700 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | IC50 | 32.9250 | 1 | 0 |
| ethinyl estradiol | Homo sapiens (human) | Ki | 18.6100 | 1 | 0 |
| 17-alpha-hydroxyprogesterone | Homo sapiens (human) | IC50 | 4.7300 | 1 | 0 |
| 17-alpha-hydroxyprogesterone | Homo sapiens (human) | Ki | 2.6740 | 1 | 0 |
| visnagin | Homo sapiens (human) | Ki | 60.0000 | 1 | 1 |
| phenothiazine | Homo sapiens (human) | IC50 | 25.6400 | 1 | 0 |
| phenothiazine | Homo sapiens (human) | Ki | 14.4920 | 1 | 0 |
| dibenzothiazyl disulfide | Homo sapiens (human) | IC50 | 0.3470 | 1 | 0 |
| dibenzothiazyl disulfide | Homo sapiens (human) | Ki | 0.1960 | 1 | 0 |
| sterogenol | Homo sapiens (human) | IC50 | 4.7580 | 1 | 0 |
| sterogenol | Homo sapiens (human) | Ki | 2.6890 | 1 | 0 |
| 2-chloroadenosine | Homo sapiens (human) | Ki | 3.0890 | 4 | 4 |
| 2-fluoroadenosine | Homo sapiens (human) | Ki | 0.0990 | 1 | 1 |
| azacitidine | Homo sapiens (human) | Ki | 2.8450 | 1 | 2 |
| flavanone | Homo sapiens (human) | Ki | 50.1000 | 1 | 1 |
| flavone | Homo sapiens (human) | Ki | 16.9000 | 2 | 2 |
| gentian violet | Homo sapiens (human) | IC50 | 4.1660 | 1 | 0 |
| gentian violet | Homo sapiens (human) | Ki | 2.3550 | 1 | 0 |
| 1-naphthylisothiocyanate | Homo sapiens (human) | IC50 | 6.1000 | 1 | 0 |
| 1-naphthylisothiocyanate | Homo sapiens (human) | Ki | 3.4480 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 6.0140 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | Ki | 3.3990 | 1 | 0 |
| 9-benzyladenine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| hyaluronoglucosaminidase | Homo sapiens (human) | Ki | 0.0220 | 1 | 1 |
| 3-deazaadenosine | Homo sapiens (human) | Ki | 0.4610 | 1 | 1 |
| stanozolol | Homo sapiens (human) | IC50 | 8.3250 | 1 | 0 |
| stanozolol | Homo sapiens (human) | Ki | 4.7050 | 1 | 0 |
| danazol | Homo sapiens (human) | IC50 | 11.1600 | 1 | 0 |
| danazol | Homo sapiens (human) | Ki | 6.3090 | 1 | 0 |
| ribavirin | Homo sapiens (human) | Ki | 7.4100 | 1 | 1 |
| closantel | Homo sapiens (human) | IC50 | 0.0960 | 1 | 0 |
| closantel | Homo sapiens (human) | Ki | 0.0540 | 1 | 0 |
| niguldipine | Homo sapiens (human) | Ki | 2.8000 | 3 | 3 |
| adenosine | Homo sapiens (human) | IC50 | 0.0011 | 1 | 1 |
| adenosine | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| nelfinavir | Homo sapiens (human) | IC50 | 14.7960 | 1 | 0 |
| nelfinavir | Homo sapiens (human) | Ki | 8.3630 | 1 | 0 |
| rolofylline | Homo sapiens (human) | Ki | 4.3900 | 2 | 2 |
| 3'-amino-3'-deoxyadenosine | Homo sapiens (human) | Ki | 0.2585 | 2 | 2 |
| metrifudil | Homo sapiens (human) | Ki | 0.2244 | 2 | 4 |
| 9-methyladenine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| 7-methyladenine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| 9-(2,3-dihydroxypropyl)adenine, (s)-isomer | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| 8-bromoadenine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n(6)-benzyladenosine | Homo sapiens (human) | Ki | 0.2957 | 2 | 2 |
| 5-methylcytidine | Homo sapiens (human) | Ki | 8.0200 | 1 | 1 |
| phenylisopropyladenosine | Homo sapiens (human) | Ki | 0.0111 | 3 | 3 |
| 5'-n-methylcarboxamideadenosine | Homo sapiens (human) | Ki | 0.0154 | 2 | 2 |
| 3,7-dimethyl-1-propargylxanthine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n-methyladenosine | Homo sapiens (human) | Ki | 0.0093 | 1 | 1 |
| 2'-o-methyladenosine | Homo sapiens (human) | IC50 | 0.0150 | 1 | 1 |
| n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Homo sapiens (human) | IC50 | 0.0017 | 19 | 19 |
| n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Homo sapiens (human) | Ki | 0.0506 | 37 | 37 |
| 2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | IC50 | 0.0112 | 1 | 1 |
| 2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | Ki | 1.4705 | 14 | 14 |
| adenosine amine congener | Homo sapiens (human) | Ki | 0.0124 | 1 | 1 |
| 8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 3.9455 | 2 | 2 |
| 7-bromoeudistomine d | Homo sapiens (human) | Ki | 2.0500 | 2 | 2 |
| 1-propylxanthine | Homo sapiens (human) | Ki | 2.3700 | 1 | 1 |
| tecadenoson | Homo sapiens (human) | Ki | 25.8000 | 1 | 1 |
| 1-deazaadenosine | Homo sapiens (human) | Ki | 0.4373 | 1 | 3 |
| 4'-hydroxyflavanone | Homo sapiens (human) | Ki | 42.8000 | 1 | 1 |
| zm 241385 | Homo sapiens (human) | Ki | 1.5980 | 11 | 11 |
| sch 58261 | Homo sapiens (human) | Ki | 7.4571 | 7 | 7 |
| 2'-hydroxyflavanone | Homo sapiens (human) | Ki | 6.0700 | 1 | 1 |
| cirsimaritin | Homo sapiens (human) | Ki | 1.7200 | 1 | 1 |
| 2-(4-morpholinoanilino)-6-cyclohexylaminopurine | Homo sapiens (human) | Ki | 0.6600 | 1 | 1 |
| regadenoson | Homo sapiens (human) | Ki | 6.6700 | 3 | 3 |
| estradiol 3-benzoate | Homo sapiens (human) | IC50 | 21.7800 | 1 | 0 |
| estradiol 3-benzoate | Homo sapiens (human) | Ki | 12.3120 | 1 | 0 |
| 6-chloroflavone | Homo sapiens (human) | Ki | 32.0000 | 1 | 1 |
| mrs 1067 | Homo sapiens (human) | Ki | 0.4204 | 4 | 4 |
| diethyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate | Homo sapiens (human) | Ki | 2.5100 | 1 | 1 |
| sakuranetin | Homo sapiens (human) | Ki | 3.4000 | 2 | 2 |
| mrs 1191 | Homo sapiens (human) | Ki | 0.0213 | 4 | 4 |
| mrs 1220 | Homo sapiens (human) | IC50 | 0.0036 | 2 | 2 |
| mrs 1220 | Homo sapiens (human) | Ki | 0.1451 | 22 | 22 |
| 5'-methylthioadenosine | Homo sapiens (human) | IC50 | 71.0000 | 1 | 1 |
| 5'-methylthioadenosine | Homo sapiens (human) | Ki | 0.6800 | 1 | 1 |
| tretinoin | Homo sapiens (human) | IC50 | 5.2750 | 1 | 0 |
| tretinoin | Homo sapiens (human) | Ki | 2.9820 | 1 | 0 |
| 2'-amino-2'-deoxyadenosine | Homo sapiens (human) | Ki | 500.1505 | 2 | 2 |
| adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | IC50 | 4.3824 | 15 | 15 |
| adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | Ki | 0.4634 | 45 | 49 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 2.2080 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 1.2480 | 1 | 0 |
| wr-142,490 | Homo sapiens (human) | Ki | 6.9410 | 1 | 1 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 3.7058 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 2.0946 | 1 | 0 |
| n(6)-cyclopentyladenosine | Homo sapiens (human) | Ki | 1.4554 | 18 | 18 |
| flunarizine | Homo sapiens (human) | IC50 | 5.1980 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 2.9380 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | IC50 | 5.3500 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | Ki | 3.0240 | 1 | 0 |
| N-[4-(2-pyridinyl)-2-thiazolyl]cyclopentanecarboxamide | Homo sapiens (human) | Ki | 2.1000 | 1 | 1 |
| thioguanine anhydrous | Homo sapiens (human) | IC50 | 21.6870 | 1 | 0 |
| thioguanine anhydrous | Homo sapiens (human) | Ki | 12.2580 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 3.7010 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 2.0920 | 1 | 0 |
| 5-(6-aminopurin-9-yl)-N-ethyl-3,4-dihydroxy-2-oxolanecarboxamide | Homo sapiens (human) | Ki | 0.0730 | 1 | 1 |
| 2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Homo sapiens (human) | IC50 | 0.0017 | 2 | 2 |
| 2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Homo sapiens (human) | Ki | 0.0644 | 44 | 46 |
| vx-745 | Homo sapiens (human) | IC50 | 8.5470 | 1 | 0 |
| vx-745 | Homo sapiens (human) | Ki | 4.8310 | 1 | 0 |
| adenosine-5'-(N-propyl)carboxamide | Homo sapiens (human) | Ki | 0.0470 | 2 | 2 |
| 2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Homo sapiens (human) | Ki | 0.2605 | 10 | 10 |
| mrs 1523 | Homo sapiens (human) | Ki | 0.4148 | 6 | 6 |
| quercetin | Homo sapiens (human) | Ki | 30.0000 | 1 | 1 |
| montelukast | Homo sapiens (human) | IC50 | 0.4340 | 1 | 0 |
| montelukast | Homo sapiens (human) | Ki | 0.2450 | 1 | 0 |
| galangin | Homo sapiens (human) | Ki | 3.1500 | 2 | 2 |
| morin | Homo sapiens (human) | Ki | 34.0000 | 1 | 1 |
| isotretinoin | Homo sapiens (human) | IC50 | 4.1690 | 1 | 0 |
| isotretinoin | Homo sapiens (human) | Ki | 2.3570 | 1 | 0 |
| mre 3008-f20 | Homo sapiens (human) | IC50 | 0.0048 | 2 | 2 |
| mre 3008-f20 | Homo sapiens (human) | Ki | 0.1243 | 13 | 14 |
| istradefylline | Homo sapiens (human) | Ki | 3.9188 | 8 | 8 |
| osip 339391 | Homo sapiens (human) | Ki | 0.4500 | 3 | 3 |
| lacidipine | Homo sapiens (human) | IC50 | 4.0360 | 1 | 0 |
| lacidipine | Homo sapiens (human) | Ki | 2.2810 | 1 | 0 |
| psb 1115 | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| n-(1-methyl-2-phenylethyl)adenosine, (s)-isomer | Homo sapiens (human) | Ki | 0.0680 | 1 | 1 |
| sulindac sulfide | Homo sapiens (human) | IC50 | 7.2310 | 1 | 0 |
| sulindac sulfide | Homo sapiens (human) | Ki | 4.0870 | 1 | 0 |
| 8-(3-chlorostyryl)caffeine | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| oxiconazole | Homo sapiens (human) | IC50 | 0.6345 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | Ki | 0.3586 | 1 | 0 |
| artocarpin lectin | Homo sapiens (human) | Ki | 4.5900 | 1 | 1 |
| ciproxifan | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| bafilomycin a1 | Homo sapiens (human) | Ki | 1.0800 | 1 | 1 |
| bw a1433 | Homo sapiens (human) | Ki | 0.0300 | 2 | 2 |
| fk 453 | Homo sapiens (human) | Ki | 2.8000 | 1 | 1 |
| kf 17837 | Homo sapiens (human) | Ki | 2.5000 | 1 | 1 |
| gw 1929 | Homo sapiens (human) | IC50 | 14.3180 | 1 | 0 |
| gw 1929 | Homo sapiens (human) | Ki | 8.0930 | 1 | 0 |
| bay-k-8644, (-)-isomer | Homo sapiens (human) | Ki | 23.5000 | 2 | 2 |
| mrs 1754 | Homo sapiens (human) | Ki | 0.5395 | 9 | 9 |
| bay-k-8644 | Homo sapiens (human) | Ki | 2.7700 | 2 | 2 |
| dexniguldipine | Homo sapiens (human) | Ki | 1.9000 | 2 | 2 |
| binodenoson | Homo sapiens (human) | Ki | 0.6195 | 3 | 3 |
| atl 146e | Homo sapiens (human) | Ki | 0.0450 | 1 | 1 |
| 5'-amino-5'-deoxyadenosine | Homo sapiens (human) | Ki | 500.2125 | 2 | 2 |
| st 1535 | Homo sapiens (human) | Ki | 5.5000 | 2 | 2 |
| mk 936 | Homo sapiens (human) | IC50 | 0.8700 | 1 | 0 |
| mk 936 | Homo sapiens (human) | Ki | 0.4920 | 1 | 0 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| mrs 1097 | Homo sapiens (human) | Ki | 0.1085 | 4 | 4 |
| 3-iodo-4-aminobenzyl-5'-N-methylcarboxamidoadenosine | Homo sapiens (human) | Ki | 0.2512 | 4 | 4 |
| 2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7h-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidine-5-amine | Homo sapiens (human) | Ki | 1.0000 | 4 | 4 |
| vuf 8504 | Homo sapiens (human) | Ki | 3.1338 | 6 | 6 |
| n(6)-(2,2-diphenylethyl)adenosine | Homo sapiens (human) | Ki | 0.0039 | 2 | 2 |
| n-cyclopropyl adenosine-5'-carboxamide | Homo sapiens (human) | Ki | 0.1560 | 3 | 3 |
| sch 442416 | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| mrs 3558 | Homo sapiens (human) | Ki | 0.0003 | 5 | 5 |
| cvt-6883 | Homo sapiens (human) | Ki | 4.0467 | 3 | 3 |
| tozadenant | Homo sapiens (human) | Ki | 3.2850 | 2 | 2 |
| psb 36 | Homo sapiens (human) | Ki | 2.3000 | 1 | 1 |
| luf 6000 | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| lj 529 | Homo sapiens (human) | IC50 | 0.0006 | 1 | 1 |
| lj 529 | Homo sapiens (human) | Ki | 0.0004 | 11 | 11 |
| a 803467 | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| archazolid a | Homo sapiens (human) | Ki | 0.9670 | 1 | 1 |
| archazolid b | Homo sapiens (human) | Ki | 1.1800 | 1 | 1 |
| v 2006 | Homo sapiens (human) | Ki | 1.0050 | 2 | 2 |
| defactinib | Homo sapiens (human) | Ki | 0.0270 | 2 | 0 |
| psb603 | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| nitd 609 | Homo sapiens (human) | IC50 | 8.3000 | 1 | 1 |
| MS-417 | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
| psb 11 | Homo sapiens (human) | Ki | 0.5869 | 6 | 6 |
| n-benzo(1,3)dioxol-5-yl-2-(5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1h-purin-8-yl)-1-methyl-1h-pyrazol-3-yloxy)-acetamide | Homo sapiens (human) | Ki | 1.0000 | 6 | 6 |
| luf 5834 | Homo sapiens (human) | Ki | 0.5380 | 1 | 1 |
| cgs 15696 | Homo sapiens (human) | Ki | 0.2600 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective AJournal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
3,4-Dihydropyrimidin-2(1Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent AJournal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
[no title available]Journal of medicinal chemistry, , 08-08, Volume: 62, Issue:15, 2019
Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human AMedChemComm, , Jan-01, Volume: 9, Issue:1, 2018
Enantiospecific Recognition at the AJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
4-amino-6-alkyloxy-2-alkylthiopyrimidine derivatives as novel non-nucleoside agonists for the adenosine AChemical biology & drug design, , Volume: 88, Issue:5, 2016
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.European journal of medicinal chemistry, , Volume: 69, 2013
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.Bioorganic & medicinal chemistry, , Apr-01, Volume: 17, Issue:7, 2009
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Jun-01, Volume: 16, Issue:11, 2008
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Development of spin-labeled probes for adenosine receptors.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.Journal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Structure-Based Optimization of Coumarin hAJournal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Jun-01, Volume: 16, Issue:11, 2008
New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Aug-23, Volume: 50, Issue:17, 2007
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.Journal of medicinal chemistry, , Dec-15, Volume: 48, Issue:25, 2005
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Fluorescent-Labeled Selective Adenosine AJournal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
[no title available]Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Synthesis of eudistomin D analogues and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-01, Volume: 45, Issue:16, 2002
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo-pyrimidines as potent human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
QSAR of adenosine receptor antagonists: Exploring physicochemical requirements for binding of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives with human adenosine A(3) receptor subtype.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 21, Issue:2, 2011
Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Combined target-based and ligand-based drug design approach as a tool to define a novel 3D-pharmacophore model of human A3 adenosine receptor antagonists: pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as a key study.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists: influence of the chain at the N(8) pyrazole nitrogen.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
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 adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 1996
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
[no title available],
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective AJournal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Exploring Non-orthosteric Interactions with a Series of Potent and Selective AACS medicinal chemistry letters, , Feb-10, Volume: 13, Issue:2, 2022
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Interactions of flavonoids and other phytochemicals with adenosine receptors.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 1996
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
Discovery and Structure-Activity Relationship Studies of Novel Adenosine AJournal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.ACS medicinal chemistry letters, , Jul-14, Volume: 13, Issue:7, 2022
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Discovery of benzothiazole-based adenosine A2B receptor antagonists with improved A2A selectivity.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 20, Issue:14, 2010
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.Journal of medicinal chemistry, , May-04, Volume: 49, Issue:9, 2006
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.Chemistry & biology, , Volume: 12, Issue:2, 2005
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Ribose-modified purine nucleosides as ribonucleotide reductase inhibitors. Synthesis, antitumor activity, and molecular modeling of N6-substituted 3'-C-methyladenosine derivatives.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.Journal of medicinal chemistry, , Apr-19, Volume: 50, Issue:8, 2007
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.ACS medicinal chemistry letters, , Jul-09, Volume: 6, Issue:7, 2015
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Selective AACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
[no title available]ACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
Structural Characterization of Agonist Binding to an AJournal of medicinal chemistry, , 10-10, Volume: 62, Issue:19, 2019
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards AEuropean journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
[no title available]Journal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
1'-Homonucleosides and their structural analogues: A review.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.Bioorganic & medicinal chemistry, , Dec-01, Volume: 17, Issue:23, 2009
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
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 responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.Journal of medicinal chemistry, , Jan-11, Volume: 50, Issue:1, 2007
The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
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.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.Journal of medicinal chemistry, , Sep-09, Volume: 47, Issue:19, 2004
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor.Journal of medicinal chemistry, , Jan-30, Volume: 46, Issue:3, 2003
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
Discovery of first-in-class multi-target adenosine AEuropean journal of medicinal chemistry, , Sep-01, Volume: 201, 2020
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
2-(N-acyl) and 2-N-acyl-N(6)-substituted analogues of adenosine and their affinity at the human adenosine receptors.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 14, Issue:6, 2004
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Synthesis of eudistomin D analogues and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Synthesis of hybrid molecules of caffeine and eudistomin D and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 15, Issue:9, 2007
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective AJournal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
3,4-Dihydropyrimidin-2(1Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent AJournal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Trifluorinated Pyrimidine-Based AJournal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
Structure-activity relationship studies and pharmacological characterization of NEuropean journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Enantiospecific Recognition at the AJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Design, Synthesis, and Pharmacological Characterization of 2-(2-Furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine Derivatives: New Highly Potent AJournal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
[no title available]Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.Journal of medicinal chemistry, , Mar-27, Volume: 46, Issue:7, 2003
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
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 adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.Journal of medicinal chemistry, , Sep-09, Volume: 47, Issue:19, 2004
Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Interactions of flavonoids and other phytochemicals with adenosine receptors.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 1996
[no title available]ACS medicinal chemistry letters, , Jun-09, Volume: 13, Issue:6, 2022
Exploring Non-orthosteric Interactions with a Series of Potent and Selective AACS medicinal chemistry letters, , Feb-10, Volume: 13, Issue:2, 2022
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Selective AACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
Development of Covalent, Clickable Probes for Adenosine AJournal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
1,2,4-triazolo[1,5-a]quinoxaline derivatives and their simplified analogues as adenosine A₃ receptor antagonists. Synthesis, structure-affinity relationships and molecular modeling studies.Bioorganic & medicinal chemistry, , Jan-01, Volume: 23, Issue:1, 2015
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo-pyrimidines as potent human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 10, Issue:1, 2000
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-04, Volume: 42, Issue:22, 1999
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.Journal of medicinal chemistry, , Jul-16, Volume: 41, Issue:15, 1998
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
[no title available]ACS medicinal chemistry letters, , Jun-09, Volume: 13, Issue:6, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
Discovery and Structure-Activity Relationship Studies of Novel Adenosine AJournal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
Examining the Role of the Linker in Bitopic Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Selective AACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
Discovery of first-in-class multi-target adenosine AEuropean journal of medicinal chemistry, , Sep-01, Volume: 201, 2020
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Structural Characterization of Agonist Binding to an AJournal of medicinal chemistry, , 10-10, Volume: 62, Issue:19, 2019
A Structure-Activity Relationship Study of Bitopic NJournal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human AMedChemComm, , Jan-01, Volume: 9, Issue:1, 2018
The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the AJournal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
[no title available]Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.European journal of medicinal chemistry, , Volume: 69, 2013
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists.ACS medicinal chemistry letters, , Dec-08, Volume: 2, Issue:12, 2011
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Synthesis of hybrid analogues of caffeine and eudistomin D and its affinity for adenosine receptors.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Synthesis of eudistomin D analogues and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.Journal of medicinal chemistry, , Apr-19, Volume: 50, Issue:8, 2007
Synthesis of hybrid molecules of caffeine and eudistomin D and its effects on adenosine receptors.Bioorganic & medicinal chemistry, , May-01, Volume: 15, Issue:9, 2007
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5'-N-ethylcarboxamido-adenosines: the first example of adenosine-related structures with potent agonist activity at the human A(2B) adenosine receptor.Bioorganic & medicinal chemistry, , Apr-01, Volume: 15, Issue:7, 2007
Synthesis and biological evaluation of novel 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]- 9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamide derivatives as useful templates for the development of A2B adenosine receptor agonists.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.Journal of medicinal chemistry, , May-04, Volume: 49, Issue:9, 2006
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.Chemistry & biology, , Volume: 12, Issue:2, 2005
2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.Journal of medicinal chemistry, , Jul-15, Volume: 47, Issue:15, 2004
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors.Bioorganic & medicinal chemistry letters, , Dec-03, Volume: 11, Issue:23, 2001
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.Bioorganic & medicinal chemistry letters, , May-21, Volume: 11, Issue:10, 2001
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Structure activity relationship of 2-arylalkynyl-adenine derivatives as human AMedChemComm, , Nov-01, Volume: 9, Issue:11, 2018
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors.Journal of medicinal chemistry, , Aug-30, Volume: 44, Issue:18, 2001
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes.Bioorganic & medicinal chemistry letters, , Sep-18, Volume: 10, Issue:18, 2000
N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Interaction of AEuropean journal of medicinal chemistry, , Mar-05, Volume: 231, 2022
Selective AACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New AJournal of medicinal chemistry, , 09-09, Volume: 64, Issue:17, 2021
[no title available]Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
[no title available]ACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human AMedChemComm, , Jan-01, Volume: 9, Issue:1, 2018
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards AEuropean journal of medicinal chemistry, , Sep-05, Volume: 157, 2018
[no title available]Journal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.European journal of medicinal chemistry, , Volume: 69, 2013
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry, , May-15, Volume: 17, Issue:10, 2009
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.Bioorganic & medicinal chemistry, , Dec-01, Volume: 17, Issue:23, 2009
Topological descriptors in modeling the agonistic activity of human A3 adenosine receptor ligands: the derivatives of 2-chloro-N(6)-substituted-4'-thioadenosine-5'-uronamide.European journal of medicinal chemistry, , Volume: 44, Issue:4, 2009
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-15, Volume: 50, Issue:23, 2007
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.Journal of medicinal chemistry, , Sep-09, Volume: 47, Issue:19, 2004
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor.Journal of medicinal chemistry, , Jan-30, Volume: 46, Issue:3, 2003
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles.Bioorganic & medicinal chemistry letters, , Jul-07, Volume: 8, Issue:13, 1998
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.Journal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.Journal of medicinal chemistry, , Apr-09, Volume: 58, Issue:7, 2015
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.ACS medicinal chemistry letters, , Sep-11, Volume: 5, Issue:9, 2014
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands.Bioorganic & medicinal chemistry, , Jan-15, Volume: 21, Issue:2, 2013
Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound A₂A adenosine receptor.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists.ACS medicinal chemistry letters, , Dec-08, Volume: 2, Issue:12, 2011
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Selective AACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.Journal of medicinal chemistry, , Sep-26, Volume: 45, Issue:20, 2002
Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
Interactions of flavonoids and other phytochemicals with adenosine receptors.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-07, Volume: 39, Issue:12, 1996
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Selective AACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A₃ adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
QSAR of adenosine receptor antagonists: Exploring physicochemical requirements for binding of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives with human adenosine A(3) receptor subtype.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 21, Issue:2, 2011
Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites.Bioorganic & medicinal chemistry, , Jul-15, Volume: 17, Issue:14, 2009
Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Combined target-based and ligand-based drug design approach as a tool to define a novel 3D-pharmacophore model of human A3 adenosine receptor antagonists: pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as a key study.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Synthesis, biological activity, and molecular modeling investigation of new pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as human A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands.Journal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
Fluorosulfonyl- and bis-(beta-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists: influence of the chain at the N(8) pyrazole nitrogen.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.Bioorganic & medicinal chemistry letters, , Feb-07, Volume: 10, Issue:3, 2000
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-04, Volume: 42, Issue:22, 1999
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
AJournal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
AJournal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
Nanomolar anti-sickling compounds identified by ligand-based pharmacophore approach.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.Journal of medicinal chemistry, , Jun-15, Volume: 49, Issue:12, 2006
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-28, Volume: 45, Issue:7, 2002
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands.Bioorganic & medicinal chemistry, , Jan-15, Volume: 21, Issue:2, 2013
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
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.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-12, Volume: 42, Issue:16, 1999
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 1996
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
Selective AACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-13, Volume: 41, Issue:17, 1998
[no title available]Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-01, Volume: 44, Issue:5, 2001
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Design and in Vivo Characterization of AJournal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.Journal of medicinal chemistry, , May-10, Volume: 55, Issue:9, 2012
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
Scaffold decoration at positions 5 and 8 of 1,2,4-triazolo[1,5-c]pyrimidines to explore the antagonist profiling on adenosine receptors: a preliminary structure-activity relationship study.Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14, 2014
Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility.Journal of medicinal chemistry, , Feb-10, Volume: 54, Issue:3, 2011
Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 2012
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.Bioorganic & medicinal chemistry, , Sep-15, Volume: 16, Issue:18, 2008
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine AJournal of medicinal chemistry, , 01-26, Volume: 60, Issue:2, 2017
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Polypharmacology of NJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A₂A and A₃ adenosine receptor ligands.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 18, Issue:19, 2010
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry, , May-15, Volume: 17, Issue:10, 2009
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.Bioorganic & medicinal chemistry, , Dec-01, Volume: 17, Issue:23, 2009
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.Journal of medicinal chemistry, , Aug-28, Volume: 46, Issue:18, 2003
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Fluorescent-Labeled Selective Adenosine AJournal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Selective AACS medicinal chemistry letters, , Apr-14, Volume: 13, Issue:4, 2022
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
New 2-heterocyclyl-imidazo[2,1-i]purin-5-one derivatives as potent and selective human A3 adenosine receptor antagonists.Journal of medicinal chemistry, , Jul-28, Volume: 54, Issue:14, 2011
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-01, Volume: 45, Issue:16, 2002
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.European journal of medicinal chemistry, , Volume: 45, Issue:8, 2010
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.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Enables
This protein enables 1 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled adenosine receptor activity | molecular function | Combining with adenosine and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, GOC:mah, PMID:9755289] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
| Schaffer collateral - CA1 synapse | cellular component | A synapse between the Schaffer collateral axon of a CA3 pyramidal cell and a CA1 pyramidal cell. [PMID:16399689] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
Involved In
This protein is involved in 11 target(s):
| Target | Category | Definition |
|---|
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| activation of adenylate cyclase activity | biological process | Any process that initiates the activity of the inactive enzyme adenylate cyclase. [GOC:ai] |
| regulation of heart contraction | biological process | Any process that modulates the frequency, rate or extent of heart contraction. Heart contraction is the process in which the heart decreases in volume in a characteristic way to propel blood through the body. [GOC:dph, GOC:go_curators, GOC:tb] |
| negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
| response to wounding | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating damage to the organism. [GOC:go_curators] |
| regulation of norepinephrine secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of norepinephrine. [GOC:ef] |
| negative regulation of cell migration | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell migration. [GOC:go_curators] |
| negative regulation of NF-kappaB transcription factor activity | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the activity of the transcription factor NF-kappaB. [GOC:dph, GOC:rl, GOC:tb] |
| presynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
| G protein-coupled adenosine receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a receptor binding to extracellular adenosine and transmitting the signal to a heterotrimeric G-protein complex to initiate a change in cell activity. [GOC:dph] |