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Adenosine A1 receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
8-Cyclopentyl-1,3-dipropylxanthineIC5013.0 [1], 25.0 [2]
8-Cyclopentyl-1,3-dipropylxanthineKi2.52 [1], 3.0 [2]
5'-N-EthylcarboxamidoadenosineIC500.21 [1]
5'-N-EthylcarboxamidoadenosineKi5.0 [1]
2-Cl-IB-MecaKi220.0 [1]
IB-MecaKi51.0 [1]
CaffeineKi44900.0 [1]
IstradefyllineKi2830.0 [1]
N6-CyclopentyladenosineIC502.7 [1]
4-{2-[(7-Amino-2-Furan-2-Yl[1,2,4]triazolo[1,5-A][1,3,5]triazin-5-Yl)amino]ethyl}phenolKi255.0 [1]
2-Chloro-N6-cyclopentyladenosineIC500.5 [1], 1.3 [2]
2-(4-(2-Carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosineKi302.0 [1]
Mcp-necaKi1197.0 [1], 1200.0 [2]
2-(Furan-2-yl)-7-phenethyl-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amineKi549.0 [1]
1-[11-Ethyl-4-(furan-2-yl)-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(12),2,4,7,9-pentaen-7-yl]-3-(4-methoxyphenyl)ureaKi1026.0 [1]
CID 11248240Ki260.0 [1]
N-(2-Furan-2-yl-6-pyrazol-1-yl-pyrimidin-4-yl)-acetamideKi9.2 [1], 10.2 [2]
PreladenantKi295.0 [1], 996.0 [2], 1000.0 [3]
4-(Furan-2-yl)-10-[3-(4-methoxyphenyl)propyl]-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-7-amineKi1.11 [1], 3.8 [2], 1111.0 [3]
2-Butyl-9-methyl-8-(triazol-2-yl)purin-6-amineKi71.8 [1], 79.2 [2], 100.0 [3]
TecadenosonIC508.2 [1]
TecadenosonKi2.05 [1], 3.0 [2], 65.0 [3]
(2R,3R,4S,5R)-2-(6-Amino-2-(phenylethynyl)-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diolKi391.0 [1]
(2R,3R,4S)-2-(6-(3-Iodobenzylamino)-2-chloro-9H-purin-9-yl)-tetrahydrothiophene-3,4-diolKi2490.0 [1]
(2R,3S,4R,5R)-2-(Hydroxymethyl)-5-(6-(4-methoxyphenylamino)-9H-purin-9-yl)tetrahydrofuran-3,4-diolKi71.0 [1], 195.0 [2], 842.0 [3], 1990.0 [4]
8-(4-(4-Benzylpiperazin-1-ylsulfonyl)phenyl)-1-propyl-1H-purine-2,6(3H,7H)-dioneKi2067.0 [1], 2070.0 [2]
(2S,3S,4R,5R)-5-[2-Chloro-6-[(3-iodophenyl)methylamino]purin-9-yl]-3,4-dihydroxy-N,N-dimethyloxolane-2-carboxamideKi5870.0 [1]
(2S,3S,4R,5R)-5-[2-Chloro-6-[(3-iodophenyl)methylamino]purin-9-yl]-3,4-dihydroxy-N,N-dimethylthiolane-2-carboxamideKi6220.0 [1]
(2S,3S,4R,5R)-3,4-Dihydroxy-5-[6-[(3-iodophenyl)methylamino]purin-9-yl]-N-methylthiolane-2-carboxamideKi17.3 [1], 20.2 [2]
5-Methyl-2-phenylpyrazolo[4,3-d]pyrimidin-7-amineKi70.0 [1]
2,5-Diphenylpyrazolo[4,3-d]pyrimidin-7-amineKi75.0 [1]
5-Benzyl-2-phenylpyrazolo[4,3-d]pyrimidin-7-amineKi150.0 [1]
2-ChloroadenosineKi1.39 [1], 2.8 [2], 18.4 [3]
(R)-N-(1-Methyl-2-phenylethyl)adenosineIC50830.0 [1]
(R)-N-(1-Methyl-2-phenylethyl)adenosineKi2.0 [1]
RolofyllineKi0.29 [1], 0.72 [2]
FscpxIC5010.0 [1], 11.8 [2]
Cvt-6883Ki1940.0 [1], 10000.0 [2]
(+)-(R)-((E)-3-(2-Phenylpyrazolo(1,5-a)pyridin-3-yl)acryloyl)-2-piperidineethanolKi0.49 [1], 18.0 [2]
TonapofyllineKi7.0 [1], 7.4 [2]
BinodenosonKi169.0 [1], 48000.0 [2]
7-Chloro-4-hydroxy-2-phenyl-1,8-naphthyridineKi0.16 [1], 300.0 [2], 670.0 [3]
CID 10046145Ki2500.0 [1]
4-(Furan-2-yl)-11-(2-phenylethyl)-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(12),2,4,7,9-pentaen-7-amineKi1.0 [1]
1-[4-(Furan-2-yl)-11-methyl-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(12),2,4,7,9-pentaen-7-yl]-3-(4-methoxyphenyl)ureaKi1097.0 [1]
Unii-djf621DE4FKi369.0 [1], 1000.0 [2]
1-(3-Chlorophenyl)-3-[11-ethyl-4-(furan-2-yl)-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(12),2,4,7,9-pentaen-7-yl]ureaKi249.0 [1]
1-[11-Butyl-4-(furan-2-yl)-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(12),2,4,7,9-pentaen-7-yl]-3-(4-methoxyphenyl)ureaKi296.0 [1]
1-(3-Chlorophenyl)-3-[4-(furan-2-yl)-11-propyl-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(12),2,4,7,9-pentaen-7-yl]ureaKi30.0 [1]
TrabodenosonKi0.97 [1]
5-Butyl-8-[4-(trifluoromethyl)phenyl]-1H-[1,2,4]triazolo[5,1-f]purineIC5010000.0 [1]
5-Butyl-8-[4-(trifluoromethyl)phenyl]-1H-[1,2,4]triazolo[5,1-f]purineKi4.0 [1], 10000.0 [2]
N-[2-[[2-Phenyl-6-[4-(3-phenylpropyl)piperazine-1-carbonyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]ethyl]acetamideKi37.0 [1], 450.0 [2]
N-[4-(Furan-2-yl)-11-(3-phenylpropyl)-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(12),2,4,7,9-pentaen-7-yl]-2-naphthalen-1-ylacetamideKi710.0 [1], 1100.0 [2]
(2R,3S,4R,5R)-2-(Hydroxymethyl)-5-[6-(methylamino)-2-(2-phenylethynyl)purin-9-yl]oxolane-3,4-diolKi1690.0 [1]
4-Benzyl-7-methyl-2-propyl-6H-purino[7,8-a]imidazole-1,3-dioneKi1000.0 [1]
2-(4-Methyl-1H-1,3-benzodiazol-2-yl)quinoxalineKi8000.0 [1]
2-Amino-8-(2-morpholinoethoxy)-4-phenyl-5H-indeno[1,2-d]pyrimidin-5-oneKi48.2 [1]
(1S,2R,3S,4R,5S)-4-[2-Chloro-6-[(3-iodophenyl)methylamino]purin-9-yl]-2,3-dihydroxy-N-methylbicyclo[3.1.0]hexane-1-carboxamideKi136.0 [1]
7-Bromo-2-phenyl-[1,8]naphthyridin-4-olKi0.79 [1], 336.0 [2], 360.0 [3]
(5,6-Dimethyl-2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-((R)-1-phenyl-ethyl)-amineIC501607.0 [1], 1981.0 [2]
(5,6-Dimethyl-2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-((R)-1-phenyl-ethyl)-amineKi981.0 [1]
N-Cyclohexyl-7-methyl-2-phenyl-1,8-naphthyridin-4-amineKi31.62 [1], 448.0 [2], 560.0 [3]
N-(2,6-Diphenylpyrimidin-4-yl)acetamideKi31.2 [1], 37.5 [2]
4-Benzyl-7-ethyl-2-propyl-8H-purino[7,8-a]pyrrole-1,3-dioneKi1000.0 [1]
(2R,3S,4R,5R)-2-(Hydroxymethyl)-5-[6-(methylamino)-2-(4-pyridin-2-ylpyrazol-1-yl)purin-9-yl]oxolane-3,4-diolKi3800.0 [1]
2-(4-(2,6-Dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)phenoxy)-N-(4-iodophenyl)acetamideKi293.0 [1], 295.12 [2]
N-(2-Furan-2-yl-6-pyrazol-1-yl-pyrimidin-4-yl)-2-(4-methyl-piperazin-1-yl)-acetamideKi266.0 [1], 270.0 [2]
2-(3,4-Dimethoxyphenyl)-N-[5-(2,6-dioxo-1,3-dipropyl-7H-purin-8-yl)-1-methylpyrazol-3-yl]acetamideKi1000.0 [1]
N-[6-(3,5-Dimethylpyrazol-1-yl)-2-(5-methylfuran-2-yl)pyrimidin-4-yl]-2-(4-methylpiperazin-1-yl)acetamideKi850.0 [1]
2-(6-Amino-8-bromo-9H-purin-9-yl)ethanolKi1500.0 [1]
(1R,2R,3S,4R,5S)-4-[2-Chloro-6-[(3-chlorophenyl)methylamino]purin-9-yl]bicyclo[3.1.0]hexane-2,3-diolKi1600.0 [1], 3070.0 [2]
4-[6-Amino-9-methyl-8-(triazol-2-yl)purin-2-yl]butan-2-oneKi192.0 [1], 197.0 [2], 200.0 [3]
4-[6-Amino-9-methyl-8-(triazol-2-yl)purin-2-yl]butan-2-olKi24.0 [1], 27.0 [2], 34.0 [3]
(1R,2R,3S,4R,5S)-4-[2-Chloro-6-(dicyclopropylmethylamino)purin-9-yl]bicyclo[3.1.0]hexane-2,3-diolKi47.9 [1], 48.0 [2]
(2S,3S,4R,5R)-5-[2-Chloro-6-(methylamino)purin-9-yl]-3,4-dihydroxy-N-methylthiolane-2-carboxamideKi1330.0 [1]
Unii-29S2U9drgsKi200.0 [1], 10000.0 [2]
7-Dimethylamino-2-phenyl-[1,8]naphthyridin-4-olKi0.63 [1], 980.0 [2], 1370.0 [3]
8-Bromo-9-propyl-9H-purin-6-ylamineKi1100.0 [1]
2-Phenyl-5-(3-phenylpropyl)pyrazolo[4,3-d]pyrimidin-7-amineIC5043.0 [1]
2-Phenyl-5-(3-phenylpropyl)pyrazolo[4,3-d]pyrimidin-7-amineKi5.3 [1], 5.31 [2]
7-Methyl-2-propyl-[1,8]naphthyridin-4-olKi50.12 [1], 1447.0 [2], 1500.0 [3]
7-Amino-2-methyl-1,8-naphthyridin-4-olKi10000.0 [1]
2-(3-Amino-6-imino-4,5-disulfoxanthen-9-yl)-5-[6-[4-[4-[[9-chloro-2-(furan-2-yl)-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]amino]-4-oxobutyl]triazol-1-yl]hexylcarbamoyl]benzoic acidKi87.0 [1], 87.1 [2]
(2S,3R,4S,5S,6R)-2-[4-[[(3S,4R,5S)-4-[[(2R,3S,4S,5S)-3,4-Dihydroxy-5-(hydroxymethyl)-5-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxolan-2-yl]methoxymethyl]-3-hydroxy-5-(4-hydroxy-3-methoxyphenyl)oxolan-3-yl]methyl]-2-methoxyphenoxy]-6-(hydroxymethyl)oxane-3,4,5-triolKi26.0 [1], 23600.0 [2], 31000.0 [3]
(2S)-2-[(5,6-Dimethyl-2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-4-methylpentan-1-olIC501754.0 [1], 1910.0 [2]
(2S)-2-[(5,6-Dimethyl-2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-4-methylpentan-1-olKi951.0 [1]
(5,6-Dimethyl-2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-pyridin-4-ylmethyl-amineIC50222.0 [1], 262.0 [2]
(5,6-Dimethyl-2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-pyridin-4-ylmethyl-amineKi132.0 [1]
1-[2-[(5,6-Dimethyl-2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]ethyl]imidazolidin-2-oneIC50364.0 [1], 422.0 [2]
1-[2-[(5,6-Dimethyl-2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]ethyl]imidazolidin-2-oneKi144.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Adenosine A1 receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.20 Nov2024https://www.aatbio.com/data-sets/adenosine-a1-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 20). Quest Database™ Adenosine A1 receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/adenosine-a1-receptor-inhibitors-ic50-ki.
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