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P2X purinoceptor 7 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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KN-62IC50158.0 [1]
A-740003IC5082.0 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(5-fluoropyrimidin-2-yl)-4-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanoneIC503.0 [1], 3.47 [2], 7.94 [3], 19.95 [4]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(5-fluoropyrimidin-2-yl)-4-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanoneKi5.01 [1], 9.4 [2]
2-Chloro-5-(3,5-dioxo-4,5-dihydro-1,2,4-triazin-2(3H)-yl)-N-(2-ethylhexyl)benzamideIC50800.0 [1]
3-((5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl)methyl)pyridineIC50123.03 [1], 125.89 [2], 300.0 [3]
CE-224535IC501.3 [1], 1.4 [2], 4.0 [3]
3-(2,3-Dichlorophenyl)-4-[(2-methylphenyl)methyl]-1,2,4-triazoleIC5077.62 [1], 79.43 [2]
2-Chloro-N-((1-hydroxycycloheptyl)methyl)-5-(5-methylpyridin-2-yl)benzamideIC5031.0 [1], 32.0 [2], 95.0 [3], 125.89 [4], 514.0 [5]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneIC504.0 [1], 92.0 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneKi7.0 [1], 7.1 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-(4-pyridin-2-yl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl)methanoneIC5028.1 [1], 1995.0 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-(4-pyridin-2-yl-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl)methanoneKi58.9 [1]
(2,3-Dichlorophenyl)-[4-(triazol-2-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]methanoneIC504.5 [1], 1122.0 [2]
(2,3-Dichlorophenyl)-[4-(triazol-2-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]methanoneKi9.5 [1]
(2,3-Dichlorophenyl)-[4-(1H-pyrazol-5-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]methanoneIC5020.7 [1], 562.0 [2]
(2,3-Dichlorophenyl)-[4-(1H-pyrazol-5-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]methanoneKi15.4 [1]
N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamideIC505.01 [1], 25.12 [2], 199.53 [3]
N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamideKi12.59 [1]
2-Chloro-N-(2-chlorophenethyl)-5-(3,5-dioxo-4,5-dihydro-1,2,4-triazin-2(3H)-yl)benzamideIC50290.0 [1], 300.0 [2], 316.23 [3]
2-Chloro-N-[(1-hydroxycycloheptyl)methyl]-5-(5-methyl-1H-pyrazol-3-yl)benzamideIC503.0 [1], 7.0 [2], 10.0 [3], 121.0 [4]
2-Chloro-N-[(1-hydroxycycloheptyl)methyl]-5-(1H-pyrazol-5-yl)benzamideIC5012.0 [1], 180.0 [2], 199.53 [3], 610.0 [4]
N-(2-Adamantylmethyl)-2-chloro-5-[3-(3-hydroxypropylamino)propyl]benzamide;hydrochlorideIC501.5 [1], 2.0 [2], 3.0 [3], 10.0 [4]
2-Methyl-N-[[1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl]-3,4-dihydro-1H-isoquinoline-5-carboxamideIC5019.95 [1], 39.81 [2], 199.53 [3]
2-Methyl-N-[[1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl]-3,4-dihydro-1H-isoquinoline-5-carboxamideKi12.59 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-4-methyl-1-pyridin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneIC5015.0 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-4-methyl-1-pyridin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneKi31.6 [1], 32.0 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(4-fluorophenyl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneIC5060.3 [1], 67.0 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(4-fluorophenyl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneKi39.8 [1], 40.0 [2]
[2-Chloro-4-fluoro-3-(trifluoromethyl)phenyl]-[(6R)-2,6-dimethyl-4-(1H-pyrazol-5-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]methanoneIC5010.0 [1]
[2-Chloro-4-fluoro-3-(trifluoromethyl)phenyl]-[(6R)-2,6-dimethyl-4-(1H-pyrazol-5-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]methanoneKi50.1 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(5-fluoropyrimidin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneIC5034.0 [1], 53.2 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-1-(5-fluoropyrimidin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneKi22.0 [1], 22.4 [2]
CID 53325874IC509.0 [1], 93.0 [2]
1-(2,3-Dichlorophenyl)-N-[(2-pyridin-2-yloxyphenyl)methyl]tetrazol-5-amineIC506.61 [1], 20.0 [2], 37.15 [3]
[4-[(2S)-3-[4-(4-Chlorophenyl)piperazin-1-yl]-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxopropyl]phenyl] isoquinoline-5-sulfonateIC50100.0 [1], 105.0 [2]
[4-[(2S)-3-(4-Benzylpiperazin-1-yl)-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxopropyl]phenyl] isoquinoline-5-sulfonateIC5019.95 [1], 21.1 [2], 65.3 [3]
[4-[(2S)-3-[4-(2-Chlorophenyl)piperazin-1-yl]-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxopropyl]phenyl] isoquinoline-5-sulfonateIC5015.8 [1], 15.85 [2]
[4-[(2S)-3-[4-(3-Chlorophenyl)piperazin-1-yl]-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxopropyl]phenyl] isoquinoline-5-sulfonateIC5012.59 [1], 14.1 [2]
1-Benzyl-5-(2,3-dichlorophenyl)tetrazoleIC5039.81 [1]
5-(2,3-Dichlorophenyl)-1-[(2-methylphenyl)methyl]tetrazoleIC5015.85 [1], 17.78 [2]
N-[(2,4-Dichlorophenyl)methyl]-2-(3,5-dimethyl-1H-pyrazol-4-yl)acetamideIC507.94 [1]
CID 44250460IC5019.95 [1]
[4-[(2S)-3-[4-(4-Fluorophenyl)piperazin-1-yl]-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxopropyl]phenyl] isoquinoline-5-sulfonateIC501.26 [1], 1.3 [2]
2-Chloro-5-(3,5-dioxo-1,2,4-triazin-2-yl)-N-[(1-hydroxycycloheptyl)methyl]benzamideIC5015.0 [1], 83.0 [2], 100.0 [3]
N'-Quinolin-5-yladamantane-1-carbohydrazideIC505.01 [1], 10.0 [2], 10.23 [3]
N'-(3,5-Dichloropyridin-4-yl)-3,5-dimethyladamantane-1-carbohydrazideIC509.2 [1], 13.0 [2]
2-Chloro-N-[(1-hydroxycycloheptyl)methyl]-5-(6-methoxypyridazin-3-yl)benzamideIC5028.0 [1], 280.0 [2], 510.0 [3]
2-(3,5-Dimethyl-1H-pyrazol-4-yl)-N-[[4-fluoro-3-(trifluoromethyl)phenyl]methyl]acetamideIC5050.12 [1], 3162.28 [2], 19952.62 [3]
7-[(2,3-Dichlorophenyl)carbonyl]-3-(2-pyrazinyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazineIC501.58 [1], 1.9 [2], 10.0 [3]
[2-Chloro-3-(trifluoromethyl)phenyl]-[3-(4-fluorophenyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanoneIC503.98 [1], 10.0 [2], 13.5 [3]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-4-methyl-1-pyrazin-2-yl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanoneIC503.47 [1], 13366.0 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-4-methyl-1-pyrazin-2-yl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanoneKi13182.6 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-4-methyl-1-pyrimidin-2-yl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanoneIC502.2 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[(4R)-4-methyl-1-pyrimidin-2-yl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]methanoneKi12.6 [1], 12.88 [2]
[(6S)-1-(5-Fluoropyrimidin-2-yl)-6-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]-[2-fluoro-3-(trifluoromethyl)phenyl]methanoneIC504.8 [1]
[(6S)-1-(5-Fluoropyrimidin-2-yl)-6-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-5-yl]-[2-fluoro-3-(trifluoromethyl)phenyl]methanoneKi5.6 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-(1-pyridin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneIC504.0 [1], 6.1 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-(1-pyridin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneKi75.9 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-(1-phenyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneIC5012.0 [1], 18.4 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-(1-phenyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneKi87.1 [1]
(2,3-Dichlorophenyl)-(1-phenyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneIC5081.1 [1], 89.0 [2]
(2,3-Dichlorophenyl)-(1-phenyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneKi60.3 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-(1-pyrazin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneIC509.0 [1], 9.4 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-(1-pyrazin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneKi42.7 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneIC5014.0 [1], 22.3 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-[1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneKi125.9 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-(4-methyl-1-phenyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneIC505.0 [1], 6.1 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-(4-methyl-1-phenyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneKi85.1 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[1-(5-fluoropyrimidin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneIC5010.0 [1], 13.1 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-[1-(5-fluoropyrimidin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneKi125.9 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-(4-methyl-1-pyridin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneIC5025.9 [1], 34.0 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-(4-methyl-1-pyridin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneKi50.1 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[1-(4-fluorophenyl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneIC5077.3 [1], 78.0 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-[1-(4-fluorophenyl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneKi100.0 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-[1-(3-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneIC509.0 [1], 78.5 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-[1-(3-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl]methanoneKi125.9 [1]
[2-Chloro-3-(trifluoromethyl)phenyl]-(4-methyl-1-pyrimidin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneIC5030.0 [1], 34.4 [2]
[2-Chloro-3-(trifluoromethyl)phenyl]-(4-methyl-1-pyrimidin-2-yl-6,7-dihydro-4H-imidazo[4,5-c]pyridin-5-yl)methanoneKi39.8 [1]
(6S)-7-[(2-Chlorophenyl)methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC50216.0 [1], 248.3 [2]
(6S)-7-[(2-Chlorophenyl)methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi31.6 [1]
(6S)-6-Methyl-7-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC501.6 [1], 3.4 [2]
(6S)-6-Methyl-7-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi5.0 [1]
(6S)-7-[(2,6-Dichlorophenyl)methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC5072.0 [1], 97.1 [2]
(6S)-7-[(2,6-Dichlorophenyl)methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi63.1 [1]
(6S)-6-Methyl-3-pyrazin-2-yl-7-[[3-(trifluoromethyl)phenyl]methyl]-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC503.6 [1], 4.0 [2]
(6S)-6-Methyl-3-pyrazin-2-yl-7-[[3-(trifluoromethyl)phenyl]methyl]-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi5.0 [1]
7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC5044.2 [1], 440.0 [2]
7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi6.3 [1]
(6S)-7-[(2,3-Dichlorophenyl)methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC501.0 [1]
(6S)-7-[(2,3-Dichlorophenyl)methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi1.4 [1]
7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC502.1 [1], 3.4 [2]
7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi4.0 [1]
(6R)-7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC504710.0 [1], 9247.0 [2]
(6R)-7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi912.0 [1]
(6S)-7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC500.7 [1]
(6S)-7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyrazin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi1.6 [1]
(6S)-7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-3-(4-fluorophenyl)-6-methyl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC500.2 [1], 1.0 [2]
(6S)-7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-3-(4-fluorophenyl)-6-methyl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneKi7.9 [1]
(6S)-7-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-6-methyl-3-pyridin-2-yl-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8-oneIC500.5 [1], 1.0 [2]
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References

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MLA

"Quest Database™ P2X purinoceptor 7 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 8 May. 2024, https://www.aatbio.com/data-sets/p2x-purinoceptor-7-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 8). Quest Database™ P2X purinoceptor 7 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/p2x-purinoceptor-7-inhibitors-ic50-ki.
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