Page last updated: 2024-08-07 16:22:21
Adenosine receptor A2a
An adenosine receptor A2a that is encoded in the genome of human. [PRO:WCB, UniProtKB:P29274]
Synonyms
Research
Bioassay Publications (233)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 9 (3.86) | 18.7374 |
1990's | 20 (8.58) | 18.2507 |
2000's | 94 (40.34) | 29.6817 |
2010's | 88 (37.77) | 24.3611 |
2020's | 22 (9.44) | 2.80 |
Compounds (155)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
9-ethyladenine | Homo sapiens (human) | Ki | 2.2000 | 1 | 1 |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | IC50 | 0.2033 | 3 | 3 |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | Ki | 15,444.2009 | 46 | 48 |
1,3-dipropyl-8-(4-sulfophenyl)xanthine | Homo sapiens (human) | Ki | 6.4500 | 2 | 2 |
enprofylline | Homo sapiens (human) | Ki | 67.7260 | 5 | 5 |
5-(n,n-hexamethylene)amiloride | Homo sapiens (human) | IC50 | 2.6850 | 2 | 2 |
8-(4-sulfophenyl)theophylline | Homo sapiens (human) | Ki | 5.2500 | 2 | 2 |
8-cyclopentyl-1,3-dimethylxanthine | Homo sapiens (human) | Ki | 0.1400 | 1 | 1 |
8-phenyltheophylline | Homo sapiens (human) | IC50 | 0.4540 | 1 | 1 |
8-phenyltheophylline | Homo sapiens (human) | Ki | 1.7500 | 2 | 2 |
theophylline | Homo sapiens (human) | IC50 | 12.0070 | 1 | 0 |
theophylline | Homo sapiens (human) | Ki | 8.5486 | 27 | 26 |
bithionol | Homo sapiens (human) | IC50 | 1.1670 | 1 | 0 |
bithionol | Homo sapiens (human) | Ki | 0.6550 | 1 | 0 |
caffeine | Homo sapiens (human) | IC50 | 20.4720 | 1 | 0 |
caffeine | Homo sapiens (human) | Ki | 20.5069 | 21 | 20 |
cgs 15943 | Homo sapiens (human) | IC50 | 0.0120 | 1 | 1 |
cgs 15943 | Homo sapiens (human) | Ki | 0.0007 | 15 | 18 |
clotrimazole | Homo sapiens (human) | IC50 | 12.7110 | 1 | 0 |
clotrimazole | Homo sapiens (human) | Ki | 7.1360 | 1 | 0 |
denbufylline | Homo sapiens (human) | Ki | 31.5000 | 1 | 1 |
econazole | Homo sapiens (human) | IC50 | 14.6160 | 1 | 0 |
econazole | Homo sapiens (human) | Ki | 8.2060 | 1 | 0 |
hexachlorophene | Homo sapiens (human) | IC50 | 1.6138 | 1 | 0 |
hexachlorophene | Homo sapiens (human) | Ki | 0.9060 | 1 | 0 |
nocodazole | Homo sapiens (human) | IC50 | 7.5090 | 1 | 0 |
nocodazole | Homo sapiens (human) | Ki | 4.2190 | 1 | 0 |
miconazole | Homo sapiens (human) | IC50 | 14.2530 | 1 | 0 |
miconazole | Homo sapiens (human) | Ki | 8.0020 | 1 | 0 |
nifedipine | Homo sapiens (human) | Ki | 96.1333 | 3 | 3 |
nisoldipine | Homo sapiens (human) | IC50 | 4.0580 | 1 | 0 |
nisoldipine | Homo sapiens (human) | Ki | 2.2780 | 1 | 0 |
propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
raloxifene | Homo sapiens (human) | IC50 | 2.1110 | 1 | 0 |
raloxifene | Homo sapiens (human) | Ki | 1.1850 | 1 | 0 |
trioxsalen | Homo sapiens (human) | IC50 | 1.3120 | 1 | 0 |
trioxsalen | Homo sapiens (human) | Ki | 0.7370 | 1 | 0 |
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 0.1019 | 12 | 12 |
ethinyl estradiol | Homo sapiens (human) | IC50 | 20.9310 | 1 | 0 |
ethinyl estradiol | Homo sapiens (human) | Ki | 11.7510 | 1 | 0 |
1-aminoanthraquinone | Homo sapiens (human) | Ki | 3.2000 | 1 | 1 |
2-chloroadenosine | Homo sapiens (human) | Ki | 0.1500 | 2 | 2 |
azacitidine | Homo sapiens (human) | Ki | 2.8450 | 1 | 2 |
gentian violet | Homo sapiens (human) | IC50 | 3.3650 | 1 | 0 |
gentian violet | Homo sapiens (human) | Ki | 1.8890 | 1 | 0 |
4-octylphenol | Homo sapiens (human) | IC50 | 22.4320 | 1 | 0 |
4-octylphenol | Homo sapiens (human) | Ki | 12.5930 | 1 | 0 |
amiloride | Homo sapiens (human) | Ki | 8.9600 | 3 | 3 |
9-benzyladenine | Homo sapiens (human) | Ki | 8.5000 | 1 | 1 |
3-deazaadenosine | Homo sapiens (human) | Ki | 0.4610 | 1 | 1 |
1,4-diaminoanthraquinone | Homo sapiens (human) | Ki | 0.3200 | 1 | 1 |
ribavirin | Homo sapiens (human) | Ki | 7.4100 | 1 | 1 |
mefloquine | Homo sapiens (human) | Ki | 6.5530 | 1 | 1 |
oxfendazole | Homo sapiens (human) | IC50 | 1.5040 | 1 | 0 |
oxfendazole | Homo sapiens (human) | Ki | 0.8440 | 1 | 0 |
imiquimod | Homo sapiens (human) | IC50 | 5.3200 | 1 | 0 |
imiquimod | Homo sapiens (human) | Ki | 2.9870 | 1 | 0 |
adenosine | Homo sapiens (human) | Ki | 0.2900 | 3 | 3 |
rolofylline | Homo sapiens (human) | Ki | 0.1968 | 5 | 5 |
metrifudil | Homo sapiens (human) | Ki | 0.4026 | 2 | 4 |
9-methyladenine | Homo sapiens (human) | Ki | 6.9000 | 1 | 1 |
3-methylxanthine | Homo sapiens (human) | Ki | 240.0000 | 1 | 1 |
7-methyladenine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
9-(2,3-dihydroxypropyl)adenine, (s)-isomer | Homo sapiens (human) | Ki | 8.5000 | 1 | 1 |
1-methylxanthine | Homo sapiens (human) | Ki | 1.9000 | 1 | 1 |
8-bromoadenine | Homo sapiens (human) | Ki | 3.2000 | 1 | 1 |
5-methylcytidine | Homo sapiens (human) | Ki | 8.0200 | 1 | 1 |
phenylisopropyladenosine | Homo sapiens (human) | Ki | 1.1113 | 3 | 3 |
5'-n-methylcarboxamideadenosine | Homo sapiens (human) | Ki | 0.4660 | 1 | 1 |
bw a1433u | Homo sapiens (human) | Ki | 0.3200 | 2 | 2 |
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine | Homo sapiens (human) | Ki | 1.6926 | 18 | 18 |
2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | Ki | 1.6296 | 9 | 9 |
adenosine amine congener | Homo sapiens (human) | Ki | 0.3700 | 1 | 1 |
8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 0.5700 | 4 | 4 |
7-bromoeudistomine d | Homo sapiens (human) | Ki | 4.9200 | 2 | 2 |
1,3-dipropyl-8-phenylxanthine | Homo sapiens (human) | Ki | 1.6275 | 4 | 4 |
8-(dicyclopropylmethyl)-1,3-dipropylxanthine | Homo sapiens (human) | Ki | 0.4300 | 1 | 1 |
kfm 19 | Homo sapiens (human) | Ki | 1.9080 | 2 | 3 |
2-(1-octynyl)adenosine | Homo sapiens (human) | Ki | 0.0358 | 2 | 2 |
1-isoamyl-3-isobutylxanthine | Homo sapiens (human) | Ki | 6.5000 | 1 | 1 |
tecadenoson | Homo sapiens (human) | Ki | 36.2350 | 3 | 3 |
1-deazaadenosine | Homo sapiens (human) | Ki | 0.4373 | 1 | 3 |
1,3-dipropyl-7-methylxanthine | Homo sapiens (human) | Ki | 4.0500 | 2 | 2 |
bw a522 | Homo sapiens (human) | Ki | 0.7000 | 1 | 1 |
2-hexynyladenosine-5'-n-ethylcarboxamide | Homo sapiens (human) | Ki | 0.0057 | 1 | 1 |
1,3-dipropylxanthine | Homo sapiens (human) | Ki | 5.0600 | 5 | 5 |
sb 203580 | Homo sapiens (human) | IC50 | 6.0680 | 1 | 0 |
sb 203580 | Homo sapiens (human) | Ki | 3.4070 | 1 | 0 |
zm 241385 | Homo sapiens (human) | IC50 | 0.0216 | 9 | 11 |
zm 241385 | Homo sapiens (human) | Ki | 30,963.5033 | 32 | 32 |
sch 58261 | Homo sapiens (human) | IC50 | 0.0260 | 2 | 1 |
sch 58261 | Homo sapiens (human) | Ki | 0.0016 | 17 | 17 |
l 734005 | Homo sapiens (human) | IC50 | 1.0400 | 1 | 1 |
2-(4-morpholinoanilino)-6-cyclohexylaminopurine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
regadenoson | Homo sapiens (human) | Ki | 181.7937 | 7 | 7 |
8-cyclohexylcaffeine | Homo sapiens (human) | Ki | 1.4301 | 3 | 3 |
mrs 1220 | Homo sapiens (human) | Ki | 0.0250 | 1 | 1 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | IC50 | 0.0336 | 8 | 8 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | Ki | 0.2134 | 52 | 59 |
diethylstilbestrol | Homo sapiens (human) | IC50 | 9.0130 | 1 | 0 |
diethylstilbestrol | Homo sapiens (human) | Ki | 5.0600 | 1 | 0 |
roflumilast | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
wr-142,490 | Homo sapiens (human) | Ki | 0.0610 | 3 | 3 |
2'-c-methyladenosine | Homo sapiens (human) | Ki | 4.6100 | 2 | 2 |
n(6)-cyclopentyladenosine | Homo sapiens (human) | Ki | 1.0144 | 12 | 12 |
tamoxifen | Homo sapiens (human) | IC50 | 7.0990 | 1 | 0 |
tamoxifen | Homo sapiens (human) | Ki | 3.9850 | 1 | 0 |
5-(6-aminopurin-9-yl)-N-ethyl-3,4-dihydroxy-2-oxolanecarboxamide | Homo sapiens (human) | Ki | 0.0160 | 1 | 1 |
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide | Homo sapiens (human) | Ki | 3.5921 | 24 | 26 |
adenosine-5'-(N-propyl)carboxamide | Homo sapiens (human) | Ki | 0.2100 | 1 | 1 |
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Homo sapiens (human) | IC50 | 0.0190 | 1 | 1 |
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Homo sapiens (human) | Ki | 0.0685 | 15 | 15 |
mrs 1523 | Homo sapiens (human) | Ki | 3.6600 | 1 | 1 |
tolcapone | Homo sapiens (human) | IC50 | 0.9300 | 1 | 1 |
genistein | Homo sapiens (human) | IC50 | 17.4420 | 1 | 0 |
genistein | Homo sapiens (human) | Ki | 9.7920 | 1 | 0 |
entacapone | Homo sapiens (human) | IC50 | 2.3200 | 1 | 1 |
galangin | Homo sapiens (human) | Ki | 22.6000 | 3 | 3 |
mre 3008-f20 | Homo sapiens (human) | Ki | 0.1404 | 9 | 10 |
istradefylline | Homo sapiens (human) | IC50 | 5.2490 | 1 | 2 |
istradefylline | Homo sapiens (human) | Ki | 0.0468 | 20 | 20 |
osip 339391 | Homo sapiens (human) | Ki | 0.3280 | 3 | 3 |
psb 1115 | Homo sapiens (human) | Ki | 3.7900 | 1 | 1 |
n-(1-methyl-2-phenylethyl)adenosine, (s)-isomer | Homo sapiens (human) | Ki | 1.8000 | 1 | 1 |
8-(3-chlorostyryl)caffeine | Homo sapiens (human) | Ki | 0.0928 | 3 | 3 |
isoalloxazine | Homo sapiens (human) | Ki | 0.9350 | 1 | 1 |
ciproxifan | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
bw a1433 | Homo sapiens (human) | Ki | 0.1900 | 1 | 1 |
fk 453 | Homo sapiens (human) | IC50 | 11.3000 | 1 | 1 |
fk 453 | Homo sapiens (human) | Ki | 1.3000 | 1 | 1 |
kf 17837 | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
kf 17837 | Homo sapiens (human) | Ki | 0.0710 | 1 | 1 |
gw 1929 | Homo sapiens (human) | IC50 | 37.2540 | 1 | 0 |
gw 1929 | Homo sapiens (human) | Ki | 20.9150 | 1 | 0 |
mrs 1754 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 0 |
mrs 1754 | Homo sapiens (human) | Ki | 0.4293 | 10 | 10 |
sb 334867-a | Homo sapiens (human) | Ki | 0.6700 | 1 | 1 |
cv 1808 | Homo sapiens (human) | Ki | 0.0760 | 1 | 1 |
1-(3,4-dichlorophenyl)-3-(4-((1-ethyl-3-piperidyl)amino)-6-methyl-2-pyrimidinyl)guanidine | Homo sapiens (human) | IC50 | 0.5457 | 1 | 1 |
binodenoson | Homo sapiens (human) | Ki | 0.2322 | 5 | 5 |
atl 146e | Homo sapiens (human) | Ki | 0.0005 | 4 | 4 |
5'-amino-5'-deoxyadenosine | Homo sapiens (human) | Ki | 0.4178 | 5 | 5 |
rwj 68354 | Homo sapiens (human) | IC50 | 1.0320 | 1 | 0 |
rwj 68354 | Homo sapiens (human) | Ki | 0.5800 | 1 | 0 |
uk-432097 | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
uk-432097 | Homo sapiens (human) | Ki | 0.0040 | 2 | 2 |
nebicapone | Homo sapiens (human) | IC50 | 0.6900 | 1 | 1 |
st 1535 | Homo sapiens (human) | IC50 | 0.4300 | 1 | 1 |
st 1535 | Homo sapiens (human) | Ki | 0.0074 | 5 | 5 |
n-((1s,trans)-2-hydroxycyclopentyl)adenosine | Homo sapiens (human) | Ki | 1.3300 | 1 | 1 |
2-(2-(4-chlorophenyl)ethoxy)adenosine | Homo sapiens (human) | Ki | 0.3462 | 3 | 3 |
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
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 | 0.0015 | 13 | 14 |
n(6)-(2,2-diphenylethyl)adenosine | Homo sapiens (human) | Ki | 0.3950 | 4 | 4 |
cgs 24012 | Homo sapiens (human) | Ki | 0.0310 | 3 | 3 |
n-cyclopropyl adenosine-5'-carboxamide | Homo sapiens (human) | Ki | 0.0500 | 2 | 2 |
sch 442416 | Homo sapiens (human) | Ki | 0.0030 | 8 | 8 |
mrs 3558 | Homo sapiens (human) | Ki | 2.3000 | 5 | 5 |
cvt-6883 | Homo sapiens (human) | Ki | 5.5200 | 3 | 3 |
tozadenant | Homo sapiens (human) | Ki | 0.0059 | 9 | 9 |
psb 36 | Homo sapiens (human) | Ki | 0.9800 | 1 | 1 |
lj 529 | Homo sapiens (human) | Ki | 0.2230 | 8 | 8 |
a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
v 2006 | Homo sapiens (human) | Ki | 0.0012 | 4 | 4 |
defactinib | Homo sapiens (human) | Ki | 0.3700 | 1 | 0 |
psb603 | Homo sapiens (human) | Ki | 5.0003 | 2 | 2 |
nitd 609 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
bix 02565 | Homo sapiens (human) | IC50 | 1.4200 | 1 | 0 |
sildenafil | Homo sapiens (human) | IC50 | 0.2530 | 1 | 0 |
sildenafil | Homo sapiens (human) | Ki | 0.1708 | 2 | 1 |
psb 11 | Homo sapiens (human) | Ki | 0.6940 | 2 | 2 |
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 | 0.8579 | 7 | 7 |
luf 5834 | Homo sapiens (human) | Ki | 0.0280 | 1 | 1 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
xanthine | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | Kd | 0.0709 | 3 | 1 |
enprofylline | Homo sapiens (human) | EC50 | 7.2000 | 1 | 1 |
theophylline | Homo sapiens (human) | EC50 | 28.2000 | 1 | 1 |
theophylline | Homo sapiens (human) | Kd | 2.8115 | 3 | 2 |
caffeine | Homo sapiens (human) | Kd | 15.3144 | 2 | 2 |
cgs 15943 | Homo sapiens (human) | Kd | 0.0032 | 1 | 0 |
propranolol | Homo sapiens (human) | EC50 | 5.0119 | 1 | 1 |
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine | Homo sapiens (human) | Kd | 0.0382 | 3 | 1 |
6-phenyl-1,3,5-triazine-2,4-diamine | Homo sapiens (human) | Kd | 1.5000 | 1 | 1 |
2-chloroadenosine | Homo sapiens (human) | EC50 | 0.0251 | 1 | 1 |
quinpirole | Homo sapiens (human) | EC50 | 0.0490 | 1 | 1 |
adenosine | Homo sapiens (human) | EC50 | 5.4125 | 9 | 9 |
adenosine | Homo sapiens (human) | Kd | 0.0173 | 1 | 1 |
rolofylline | Homo sapiens (human) | Kd | 0.0830 | 2 | 0 |
isoguanosine | Homo sapiens (human) | EC50 | 0.0794 | 1 | 1 |
3-methylxanthine | Homo sapiens (human) | EC50 | 100.0000 | 1 | 1 |
1-methylxanthine | Homo sapiens (human) | EC50 | 75.9000 | 1 | 1 |
phenylisopropyladenosine | Homo sapiens (human) | EC50 | 0.9500 | 1 | 1 |
5'-n-methylcarboxamideadenosine | Homo sapiens (human) | EC50 | 1.7000 | 1 | 1 |
2-chloro-n(6)cyclopentyladenosine | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
1-propylxanthine | Homo sapiens (human) | EC50 | 62.0000 | 1 | 1 |
salvinorin a | Homo sapiens (human) | EC50 | 0.0038 | 1 | 2 |
2-(1-octynyl)adenosine | Homo sapiens (human) | EC50 | 0.6810 | 1 | 1 |
1-deazaadenosine | Homo sapiens (human) | EC50 | 18.0000 | 1 | 1 |
1,3-dipropyl-7-methylxanthine | Homo sapiens (human) | EC50 | 0.6000 | 1 | 1 |
2-hexynyladenosine-5'-n-ethylcarboxamide | Homo sapiens (human) | EC50 | 0.1050 | 1 | 1 |
1,3-dipropylxanthine | Homo sapiens (human) | EC50 | 0.0500 | 1 | 1 |
zm 241385 | Homo sapiens (human) | Kd | 0.0014 | 15 | 5 |
sch 58261 | Homo sapiens (human) | Kd | 0.0065 | 5 | 0 |
2,4-diaminopteridine | Homo sapiens (human) | Kd | 9.6000 | 1 | 1 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | EC50 | 0.0776 | 16 | 16 |
1-deaza-2-chloro-n(6)-cyclopentyladenosine | Homo sapiens (human) | EC50 | 28.0000 | 1 | 1 |
n(6)-cyclopentyladenosine | Homo sapiens (human) | EC50 | 1.1316 | 2 | 2 |
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Homo sapiens (human) | EC50 | 3.9951 | 5 | 5 |
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine | Homo sapiens (human) | Kd | 0.0802 | 12 | 12 |
istradefylline | Homo sapiens (human) | Kd | 1.2589 | 1 | 1 |
mrs 1754 | Homo sapiens (human) | EC50 | 67.6083 | 1 | 1 |
mrs 1754 | Homo sapiens (human) | Kd | 0.0556 | 1 | 0 |
cv 1808 | Homo sapiens (human) | EC50 | 0.0182 | 1 | 1 |
cv 1808 | Homo sapiens (human) | Kd | 0.0091 | 1 | 1 |
binodenoson | Homo sapiens (human) | EC50 | 0.0003 | 1 | 1 |
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) | Kd | 0.0003 | 1 | 1 |
cgs 24012 | Homo sapiens (human) | EC50 | 0.0004 | 1 | 1 |
n-cyclopropyl adenosine-5'-carboxamide | Homo sapiens (human) | EC50 | 0.1414 | 2 | 2 |
sch 442416 | Homo sapiens (human) | Kd | 0.0033 | 2 | 0 |
atl 313 | Homo sapiens (human) | Kd | 0.0007 | 1 | 1 |
psb 36 | Homo sapiens (human) | Kd | 0.0024 | 1 | 0 |
v 2006 | Homo sapiens (human) | Kd | 0.0006 | 1 | 1 |
allopurinol | Homo sapiens (human) | Kd | 77.0000 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
1,3-diethyl-8-phenylxanthine | Homo sapiens (human) | Kb | 0.2100 | 1 | 1 |
1,3-dipropyl-8-cyclopentylxanthine | Homo sapiens (human) | ED50 | 10.0000 | 1 | 1 |
8-phenyltheophylline | Homo sapiens (human) | Affinity constant | 0.2000 | 1 | 1 |
8-phenyltheophylline | Homo sapiens (human) | Kb | 1.9000 | 1 | 1 |
theophylline | Homo sapiens (human) | Affinity constant | 10.0000 | 1 | 1 |
caffeine | Homo sapiens (human) | Affinity constant | 30.0000 | 1 | 1 |
cgs 15943 | Homo sapiens (human) | ED50 | 0.3000 | 1 | 1 |
1-methyl-3-isobutylxanthine | Homo sapiens (human) | Affinity constant | 5.0000 | 1 | 1 |
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine | Homo sapiens (human) | Kb | 0.0250 | 1 | 1 |
3-hydroxydiphenylamine | Homo sapiens (human) | Activity | 2,000.0000 | 1 | 1 |
2-chloroadenosine | Homo sapiens (human) | Affinity constant | 5.0000 | 1 | 1 |
adenosine | Homo sapiens (human) | Affinity constant | 15.0000 | 2 | 2 |
n(6)-benzyladenosine | Homo sapiens (human) | Affinity constant | 80.0000 | 1 | 1 |
phenylisopropyladenosine | Homo sapiens (human) | Affinity constant | 30.0000 | 1 | 1 |
n(6)-phenyladenosine | Homo sapiens (human) | Affinity constant | 50.0000 | 1 | 1 |
n-methyladenosine | Homo sapiens (human) | Affinity constant | 80.0000 | 1 | 1 |
bw a1433u | Homo sapiens (human) | Kb | 0.1100 | 1 | 1 |
8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine | Homo sapiens (human) | Kb | 2.4000 | 1 | 1 |
1,3-dipropyl-8-phenylxanthine | Homo sapiens (human) | Kb | 1.2000 | 2 | 2 |
1,3-dipropylxanthine | Homo sapiens (human) | Kb | 2.7000 | 1 | 1 |
zm 241385 | Homo sapiens (human) | K | 0.0024 | 1 | 1 |
sch 58261 | Homo sapiens (human) | ED50 | 0.3000 | 1 | 1 |
sch 58261 | Homo sapiens (human) | K | 0.0010 | 1 | 1 |
5'-methylthioadenosine | Homo sapiens (human) | Affinity constant | 10.0000 | 1 | 1 |
adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | Affinity constant | 2.0000 | 1 | 1 |
n-(1-methyl-2-phenylethyl)adenosine, (s)-isomer | Homo sapiens (human) | Affinity constant | 100.0000 | 1 | 1 |
n(6)-cyclohexyladenosine | Homo sapiens (human) | Affinity constant | 30.0000 | 1 | 1 |
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) | Kb | 0.0013 | 1 | 1 |
sch 442416 | Homo sapiens (human) | INH | 0.0000 | 1 | 1 |
v 2006 | Homo sapiens (human) | KA | 0.0006 | 1 | 1 |
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective AJournal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
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Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Further studies on pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective human A1 adenosine receptor antagonists.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
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
Synthesis of a series of 8-(substituted-phenyl)xanthines and a study on the effects of substitution pattern of phenyl substituents on affinity for adenosine A(1) and A(2A) receptors.European journal of medicinal chemistry, , Volume: 44, Issue:5, 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
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
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.Journal of medicinal chemistry, , Mar-27, Volume: 51, 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-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
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
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
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 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
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
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
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
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
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
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
Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 9, Issue:16, 1999
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists.Journal of medicinal chemistry, , Mar-01, Volume: 39, Issue:5, 1996
7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.Journal of medicinal chemistry, , Sep-18, Volume: 35, Issue:19, 1992
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
[no title available],
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
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
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.Journal of medicinal chemistry, , Jan-18, Volume: 44, Issue:2, 2001
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.ACS medicinal chemistry letters, , Jul-14, Volume: 13, Issue:7, 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
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
Biophysical mapping of the adenosine A2A receptor.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 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 theophylline derivatives and study of their activity as antagonists at adenosine receptors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
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
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
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
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
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.Journal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.Journal of medicinal chemistry, , Volume: 31, Issue:10, 1988
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
[no title available],
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.ACS medicinal chemistry letters, , Jul-14, Volume: 13, Issue:7, 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
[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
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
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
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Biophysical mapping of the adenosine A2A receptor.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
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
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
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
[no title available],
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-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.Chemistry & biology, , Volume: 12, Issue:2, 2005
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
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
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.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
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives: potent and selective A(2A) adenosine antagonists.Journal of medicinal chemistry, , Mar-01, Volume: 39, Issue:5, 1996
[no title available],
Exploring Non-orthosteric Interactions with a Series of Potent and Selective AACS medicinal chemistry letters, , Feb-10, Volume: 13, Issue:2, 2022
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective AJournal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Photoaffinity Labeling of the Human AACS medicinal chemistry letters, , Jun-08, Volume: 8, Issue:6, 2017
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Biophysical mapping of the adenosine A2A receptor.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
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
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors.Journal of medicinal chemistry, , Volume: 28, Issue:9, 1985
[no title available],
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
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 and Structure-Activity Relationship Studies of Novel Adenosine AJournal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
Design, synthesis and biological evaluation of 2-hydrazinyladenosine derivatives as AEuropean journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.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
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
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
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
Synthesis and biological evaluation of N4-substituted imidazo- and v-triazolo[4,5-d]pyridazine nucleosides.Journal of medicinal chemistry, , Dec-10, Volume: 36, Issue:25, 1993
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
2-aralkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.MedChemComm, , Jun-01, Volume: 9, Issue:6, 2018
Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.Journal of medicinal chemistry, , Sep-18, Volume: 35, Issue:19, 1992
[no title available],
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
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
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
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.Journal of medicinal chemistry, , May-07, Volume: 41, Issue:10, 1998
2-Alkynyl derivatives of adenosine and adenosine-5'-N-ethyluronamide as selective agonists at A2 adenosine receptors.Journal of medicinal chemistry, , Jun-26, Volume: 35, Issue:13, 1992
Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.Journal of medicinal chemistry, , Volume: 31, Issue:6, 1988
Adenosine receptors: targets for future drugs.Journal of medicinal chemistry, , Volume: 25, Issue:3, 1982
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors.Journal of medicinal chemistry, , Volume: 31, Issue:3, 1988
[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
[no title available]Journal of medicinal chemistry, , 12-22, Volume: 59, Issue:24, 2016
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
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 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
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
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
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
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
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.Journal of medicinal chemistry, , Apr-22, Volume: 42, Issue:8, 1999
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Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
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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
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Examining the Role of the Linker in Bitopic Journal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
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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
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
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
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
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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
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Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 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
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
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
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
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
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
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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 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
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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
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.Chemistry & biology, , Volume: 12, Issue:2, 2005
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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
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Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
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The discovery and synthesis of highly potent, A2a receptor agonists.Bioorganic & medicinal chemistry letters, , Feb-21, Volume: 10, Issue:4, 2000
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Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
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Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
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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
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High ligand efficiency quinazoline compounds as novel AEuropean journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
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[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
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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
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 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
Biophysical mapping of the adenosine A2A receptor.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.Journal of medicinal chemistry, , Feb-10, Volume: 54, Issue:3, 2011
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
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Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.Journal of medicinal chemistry, , Feb-14, Volume: 51, Issue:3, 2008
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
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
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AJournal of medicinal chemistry, , 04-25, Volume: 62, Issue:8, 2019
Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 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
Multi-target-directed ligands to combat neurodegenerative diseases.Journal of medicinal chemistry, , Feb-14, Volume: 51, Issue:3, 2008
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
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
[no title available],
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
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
2-(N'-alkylidenehydrazino)adenosines: potent and selective coronary vasodilators.Journal of medicinal chemistry, , Nov-27, Volume: 35, Issue:24, 1992
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
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
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
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
SAR of a series of inhaled A(2A) agonists and comparison of inhaled pharmacokinetics in a preclinical model with clinical pharmacokinetic data.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Adenosine A2A receptor as a drug discovery target.Journal of medicinal chemistry, , May-08, Volume: 57, Issue:9, 2014
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.Journal of medicinal chemistry, , Jul-11, Volume: 56, Issue:13, 2013
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
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
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
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
High ligand efficiency quinazoline compounds as novel AEuropean journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
[no title available]Journal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
[no title available]MedChemComm, , Jul-01, Volume: 10, Issue:7, 2019
Antagonists of the adenosine AEuropean journal of medicinal chemistry, , Jan-20, Volume: 144, 2018
Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
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
Biophysical mapping of the adenosine A2A receptor.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.Journal of medicinal chemistry, , Feb-10, Volume: 54, Issue:3, 2011
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
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
Biological Evaluation of 5'-(ACS medicinal chemistry letters, , Mar-11, Volume: 12, Issue:3, 2021
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
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
(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
N6-substituted N-alkyladenosine-5'-uronamides: bifunctional ligands having recognition groups for A1 and A2 adenosine receptors.Journal of medicinal chemistry, , Volume: 29, Issue:9, 1986
Development of Covalent, Clickable Probes for Adenosine AJournal of medicinal chemistry, , 06-24, Volume: 64, Issue:12, 2021
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
Fluorescent ligands for adenosine receptors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
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
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
Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 20, Issue:19, 2010
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
[no title available],
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
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
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
(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
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Design, synthesis and biological evaluation of Tozadenant analogues as adenosine AEuropean journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
[no title available]Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
[no title available]European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
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
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 adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.Bioorganic & medicinal chemistry, , May-15, Volume: 17, Issue:10, 2009
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
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
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
Dual-acting antitumor agents targeting the AEuropean journal of medicinal chemistry, , Jun-05, Volume: 236, 2022
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
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
Adenosine receptor antagonists: Recent advances and therapeutic perspective.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
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 9 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] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
calmodulin binding | molecular function | Binding to calmodulin, a calcium-binding protein with many roles, both in the calcium-bound and calcium-free states. [GOC:krc] |
lipid binding | molecular function | Binding to a lipid. [GOC:ai] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
type 5 metabotropic glutamate receptor binding | molecular function | Binding to a type 5 metabotropic glutamate receptor. [GOC:mah, GOC:nln] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
alpha-actinin binding | molecular function | Binding to alpha-actinin, one of a family of proteins that cross-link F-actin as antiparallel homodimers. Alpha-actinin has a molecular mass of 93-103 KDa; at the N-terminus there are two calponin homology domains, at the C-terminus there are two EF-hands. These two domains are connected by the rod domain. This domain is formed by triple-helical spectrin repeats. [PMID:10984498, PMID:11699871, PMID:15014165] |
Located In
This protein is located in 11 target(s):
Target | Category | Definition |
intermediate filament | cellular component | A cytoskeletal structure that forms a distinct elongated structure, characteristically 10 nm in diameter, that occurs in the cytoplasm of eukaryotic cells. Intermediate filaments form a fibrous system, composed of chemically heterogeneous subunits and involved in mechanically integrating the various components of the cytoplasmic space. Intermediate filaments may be divided into five chemically distinct classes: Type I, acidic keratins; Type II, basic keratins; Type III, including desmin, vimentin and others; Type IV, neurofilaments and related filaments; and Type V, lamins. [http://www.cytochemistry.net/Cell-biology/intermediate_filaments.htm, 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] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
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] |
axolemma | cellular component | The portion of the plasma membrane surrounding an axon; it is a specialized trilaminar random mosaic of protein molecules floating within a fluid matrix of highly mobile phospholipid molecules, 7-8 nm in thickness. [http://www.medik.sk/clanky/bio_jun.htm, ISBN:0124325653] |
asymmetric synapse | cellular component | A type of synapse occurring between an axon and a dendritic spine or dendritic shaft. Asymmetric synapses, the most abundant synapse type in the central nervous system, involve axons that contain predominantly spherical vesicles and contain a thickened postsynaptic density. Most or all synapses of this type are excitatory. [GOC:dgh, GOC:ef] |
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] |
neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
presynaptic active zone | cellular component | A specialized region of the plasma membrane and cell cortex of a presynaptic neuron; encompasses a region of the plasma membrane where synaptic vesicles dock and fuse, and a specialized cortical cytoskeletal matrix. [GOC:dh, GOC:dl, GOC:ef, GOC:jid, GOC:pr, PMID:3152289] |
glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 1 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] |
Involved In
This protein is involved in 50 target(s):
Target | Category | Definition |
synaptic transmission, dopaminergic | biological process | The vesicular release of dopamine. from a presynapse, across a chemical synapse, the subsequent activation of dopamine receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos, GOC:dph] |
response to amphetamine | 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 an amphetamine stimulus. Amphetamines consist of a group of compounds related to alpha-methylphenethylamine. [GOC:dph, GOC:ef] |
regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
phagocytosis | biological process | A vesicle-mediated transport process that results in the engulfment of external particulate material by phagocytes and their delivery to the lysosome. The particles are initially contained within phagocytic vacuoles (phagosomes), which then fuse with primary lysosomes to effect digestion of the particles. [ISBN:0198506732] |
apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
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] |
cellular defense response | biological process | A defense response that is mediated by cells. [GOC:ebc] |
adenylate cyclase-modulating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194] |
adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
protein kinase C-activating G protein-coupled receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand, where the pathway proceeds with activation of protein kinase C (PKC). PKC is activated by second messengers including diacylglycerol (DAG). [GOC:mah, GOC:signaling] |
cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
synaptic transmission, cholinergic | biological process | The vesicular release of acetylcholine from a presynapse, across a chemical synapse, the subsequent activation of dopamine receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos, Wikipedia:Cholinergic] |
central nervous system development | biological process | The process whose specific outcome is the progression of the central nervous system over time, from its formation to the mature structure. The central nervous system is the core nervous system that serves an integrating and coordinating function. In vertebrates it consists of the brain and spinal cord. In those invertebrates with a central nervous system it typically consists of a brain, cerebral ganglia and a nerve cord. [GOC:bf, GOC:jid, ISBN:0582227089] |
blood coagulation | biological process | The sequential process in which the multiple coagulation factors of the blood interact, ultimately resulting in the formation of an insoluble fibrin clot; it may be divided into three stages: stage 1, the formation of intrinsic and extrinsic prothrombin converting principle; stage 2, the formation of thrombin; stage 3, the formation of stable fibrin polymers. [PMID:30700128] |
sensory perception | biological process | The series of events required for an organism to receive a sensory stimulus, convert it to a molecular signal, and recognize and characterize the signal. This is a neurological process. [GOC:ai, GOC:dph] |
locomotory behavior | biological process | The specific movement from place to place of an organism in response to external or internal stimuli. Locomotion of a whole organism in a manner dependent upon some combination of that organism's internal state and external conditions. [GOC:dph] |
blood circulation | biological process | The flow of blood through the body of an animal, enabling the transport of nutrients to the tissues and the removal of waste products. [GOC:mtg_heart, ISBN:0192800825] |
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 xenobiotic stimulus | 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 from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
response to inorganic substance | 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 an inorganic substance stimulus. [GOC:sm] |
positive regulation of glutamate secretion | biological process | Any process that activates or increases the frequency, rate or extent of the controlled release of glutamate. [GOC:ef] |
positive regulation of acetylcholine secretion, neurotransmission | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of acetylcholine. [GOC:ef] |
regulation of norepinephrine secretion | biological process | Any process that modulates the frequency, rate or extent of the regulated release of norepinephrine. [GOC:ef] |
response to purine-containing compound | 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 purine-containing compound stimulus. [GOC:ef] |
response to caffeine | 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 caffeine stimulus. Caffeine is an alkaloid found in numerous plant species, where it acts as a natural pesticide that paralyzes and kills certain insects feeding upon them. [GOC:ef, GOC:mah] |
positive regulation of synaptic transmission, GABAergic | biological process | Any process that activates, maintains or increases the frequency, rate or extent of GABAergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter gamma-aminobutyric acid (GABA). [GOC:mah] |
synaptic transmission, glutamatergic | biological process | The vesicular release of glutamate from a presynapse, across a chemical synapse, the subsequent activation of glutamate receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos] |
positive regulation of urine volume | biological process | Any process that increases the amount of urine excreted from the body over a unit of time. [GOC:mtg_25march11, GOC:yaf] |
vasodilation | biological process | An increase in the internal diameter of blood vessels, especially arterioles or capillaries, due to relaxation of smooth muscle cells that line the vessels, and usually resulting in a decrease in blood pressure. [GOC:pr, ISBN:0192800981] |
eating behavior | biological process | The specific behavior of an organism relating to the intake of food, any substance (usually solid) that can be metabolized by an organism to give energy and build tissue. [GOC:jl, GOC:pr, PMID:19361967] |
negative regulation of vascular permeability | biological process | Any process that reduces the extent to which blood vessels can be pervaded by fluid. [GOC:jl] |
negative regulation of neuron apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process in neurons. [GOC:go_curators, GOC:mtg_apoptosis] |
positive regulation of circadian sleep/wake cycle, sleep | biological process | Any process that activates or increases the duration or quality of sleep, a readily reversible state of reduced awareness and metabolic activity that occurs periodically in many animals. [GOC:go_curators] |
negative regulation of alpha-beta T cell activation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of alpha-beta T cell activation. [GOC:ai] |
astrocyte activation | biological process | A change in morphology and behavior of an astrocyte resulting from exposure to a cytokine, chemokine, cellular ligand, or soluble factor. [GOC:mgi_curators, PMID:10526094, PMID:10695728, PMID:12529254, PMID:12580336, PMID:9585813] |
neuron projection morphogenesis | biological process | The process in which the anatomical structures of a neuron projection are generated and organized. A neuron projection is any process extending from a neural cell, such as axons or dendrites. [GOC:mah] |
positive regulation of protein secretion | biological process | Any process that activates or increases the frequency, rate or extent of the controlled release of a protein from a cell. [GOC:ai] |
negative regulation of inflammatory response | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the inflammatory response. [GOC:ai] |
regulation of mitochondrial membrane potential | biological process | Any process that modulates the establishment or extent of the mitochondrial membrane potential, the electric potential existing across the mitochondrial membrane arising from charges in the membrane itself and from the charges present in the media on either side of the membrane. [GOC:ai] |
membrane depolarization | biological process | The process in which membrane potential decreases with respect to its steady-state potential, usually from negative potential to a more positive potential. For example, the initial depolarization during the rising phase of an action potential is in the direction from the negative steady-state resting potential towards the positive membrane potential that will be the peak of the action potential. [GOC:dh, Wikipedia:Depolarization] |
regulation of calcium ion transport | biological process | Any process that modulates the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
positive regulation of synaptic transmission, glutamatergic | biological process | Any process that activates, maintains or increases the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |
excitatory postsynaptic potential | biological process | A process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
inhibitory postsynaptic potential | biological process | A process that causes a temporary decrease in postsynaptic membrane potential due to the flow of negatively charged ions into the postsynaptic cell. The flow of ions that causes an IPSP is an inhibitory postsynaptic current (IPSC) and makes it more difficult for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
prepulse inhibition | biological process | The process in which a startle magnitude is reduced when the startling stimulus is preceded by a low-intensity prepulse. [GOC:dph, PMID:10341260] |
apoptotic signaling pathway | biological process | The series of molecular signals which triggers the apoptotic death of a cell. The pathway starts with reception of a signal, and ends when the execution phase of apoptosis is triggered. [GOC:mtg_apoptosis] |
presynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
positive regulation of long-term synaptic potentiation | biological process | Any process that activates or increases the frequency, rate or extent of long-term synaptic potentiation. [GOC:BHF, GOC:TermGenie] |
positive regulation of apoptotic signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of apoptotic signaling pathway. [GOC:mtg_apoptosis] |
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] |