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P2X2/P2X3 heterotrimeric receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
2,4-Pyrimidinediamine, 5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-IC5025.0 [1], 79.43 [2]
2,4-Pyrimidinediamine, 5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-Ki41.69 [1]
CID 24883277IC505.01 [1]
CID 24883277Ki7.94 [1]
5-(5-Ethynyl-2-isopropyl-4-methoxy-phenoxy)-pyrimidine-2,4-diamineIC5012.59 [1]
5-(5-Ethynyl-2-isopropyl-4-methoxy-phenoxy)-pyrimidine-2,4-diamineKi11.48 [1]
2-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]ethanolIC5015.85 [1]
2-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]ethanolKi16.6 [1]
3-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propan-1-olIC5063.1 [1]
3-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propan-1-olKi64.57 [1]
2-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propan-1-olIC5015.85 [1]
2-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propan-1-olKi15.49 [1]
1-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propan-2-olIC5025.12 [1]
1-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propan-2-olKi26.92 [1]
3-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propane-1,2-diolIC5031.62 [1]
3-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propane-1,2-diolKi30.9 [1]
2-[[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]methyl]propane-1,3-diolIC5031.62 [1]
2-[[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]methyl]propane-1,3-diolKi35.48 [1]
2-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]-2-methylpropan-1-olIC50794.33 [1]
2-[[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]-2-methylpropan-1-olKi851.14 [1]
Tert-butyl (3S)-3-[[6-(4-chloro-2-cyanophenyl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]-3-(6-methoxypyridin-3-yl)propanoateIC5010000.0 [1]
N-[4-Amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]-2-methylpropanamideIC5039.81 [1]
4-(2,4-Diamino-pyrimidin-5-yloxy)-2-ethynyl-5-isopropyl-phenolIC5010.23 [1]
2-[4-[(6-Methoxypyridin-3-yl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC509.0 [1], 27.0 [2]
2-[4-(Imidazo[1,2-a]pyridin-7-ylmethylamino)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5018.0 [1], 33.0 [2]
2-[4-(1,3-Benzoxazol-5-ylmethylamino)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5015.0 [1], 45.0 [2]
5-Methyl-2-[4-[(2-methylpyrimidin-5-yl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5012.0 [1], 82.0 [2]
5-Methyl-2-[4-[[4-methyl-3-(1,2,4-triazol-1-yl)phenyl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5021.0 [1], 92.0 [2]
(3R)-3-[[6-(2-Cyano-4-methylphenyl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]-3-(6-methoxypyridin-3-yl)propanoic acidIC50207.0 [1], 1676.0 [2]
(3R)-3-[[6-(2-Cyano-4-methylphenyl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]-3-(6-methoxypyridin-3-yl)propanamideIC5026.0 [1], 174.0 [2]
(3R)-3-[[6-(2-Cyano-4-methylphenyl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]-3-(6-methoxypyridin-3-yl)-N,N-dimethylpropanamideIC50302.0 [1], 2211.0 [2]
5-Chloro-2-[4-(imidazo[1,2-a]pyridin-7-ylmethylamino)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50122.0 [1], 753.0 [2]
5-Chloro-2-[4-[(2-methylpyrimidin-5-yl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5028.0 [1], 246.0 [2]
2-[4-[[(1S)-2-Hydroxy-1-[6-(trifluoromethyl)pyridin-3-yl]ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5021.0 [1], 71.0 [2]
5-Chloro-2-[4-[[(1S)-2-hydroxy-1-[6-(trifluoromethyl)pyridin-3-yl]ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5054.0 [1], 671.0 [2]
2-[4-[(3-Fluoro-4-methylphenyl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5089.0 [1], 124.0 [2]
5-Methyl-2-[4-[(4-methyl-3-methylsulfanylphenyl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50474.0 [1], 925.0 [2]
2-[4-[[4-Chloro-3-(1,2,4-triazol-4-yl)phenyl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5031.0 [1], 63.0 [2]
5-Chloro-2-[4-[[3-(1,2,4-triazol-4-yl)phenyl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50284.0 [1], 1015.0 [2]
5-Chloro-2-[4-[[4-chloro-3-(1,2,4-triazol-4-yl)phenyl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5041.0 [1], 286.0 [2]
5-Methyl-2-[4-[[3-(1,2,4-triazol-4-yl)phenyl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5065.0 [1], 324.0 [2]
2-[4-[(4-Amino-2-methoxypyrimidin-5-yl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5032.0 [1], 62.0 [2]
2-[4-[(3-Iodo-4-methylphenyl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC50512.0 [1], 1296.0 [2]
2-[4-[[(1R)-1-(2-Methoxypyrimidin-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5010.0 [1], 164.0 [2]
5-Methyl-2-[4-[(4-methyl-3-methylsulfonylphenyl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5016.0 [1], 55.0 [2]
2-[4-[[(1S)-2-Hydroxy-1-(2-methoxypyrimidin-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5014.0 [1], 130.0 [2]
5-Methyl-2-[4-[(2-propan-2-ylpyrimidin-5-yl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50101.0 [1], 1346.0 [2]
5-Chloro-2-[4-[[(1R)-1-[6-(difluoromethyl)pyridin-3-yl]-3-hydroxypropyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5032.0 [1], 273.0 [2]
5-Methyl-2-[4-[(4-methyl-3-morpholin-4-ylphenyl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5096.0 [1], 1121.0 [2]
5-Methyl-2-[4-[[(1R)-1-(2-methylpyrimidin-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5014.0 [1], 30.0 [2]
5-Methyl-2-[4-[[(1S)-1-(2-methylpyrimidin-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50486.0 [1], 3797.0 [2]
2-[4-[(2-Methoxypyrimidin-5-yl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5013.0 [1], 42.0 [2]
5-Chloro-2-[4-[(2-methoxypyrimidin-5-yl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5042.0 [1], 224.0 [2]
2-[4-[[(1S)-1-[6-(Difluoromethyl)pyridin-3-yl]-2-hydroxyethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC507.0 [1], 33.0 [2]
2-[4-[(4-Chloro-3-methylsulfonylphenyl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5037.0 [1], 120.0 [2]
5-Chloro-2-[4-[[(1S)-1-[6-(difluoromethyl)pyridin-3-yl]-2-hydroxyethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5016.0 [1], 404.0 [2]
5-Chloro-2-[4-[[(1S)-2-hydroxy-1-(2-methylpyrimidin-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5015.0 [1], 225.0 [2]
2-[4-[[(1S)-2-Hydroxy-1-(2-methylpyrimidin-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC507.0 [1], 61.0 [2]
5-Chloro-2-[4-[[(1R)-1-(2-methylpyrimidin-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5015.0 [1], 180.0 [2]
5-Chloro-2-[4-[(4-methyl-3-methylsulfonylphenyl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5040.0 [1], 241.0 [2]
[(3R)-3-[[6-(2-Cyano-4-methylphenyl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]-3-[6-(trifluoromethyl)pyridin-3-yl]propyl] acetateIC50130.0 [1], 536.0 [2]
5-Chloro-2-[4-[[(1S)-2-hydroxy-1-(2-methoxypyrimidin-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5042.0 [1], 854.0 [2]
5-Methyl-2-(4-(quinoxalin-6-ylmethylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)benzonitrileIC5034.0 [1], 67.0 [2]
5-Methyl-2-(4-(quinolin-2-ylmethylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)benzonitrileIC50156.0 [1], 263.0 [2]
2-(4-((1H-Indol-6-yl)methylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)-5-methylbenzonitrileIC50423.0 [1], 2163.0 [2]
2-[4-(1,3-Benzodioxol-5-ylmethylamino)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5056.0 [1], 310.0 [2]
2-[4-[1-(1,3-Benzodioxol-5-yl)ethylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5054.0 [1], 125.0 [2]
5-Chloro-2-[4-(quinoxalin-6-ylmethylamino)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50125.0 [1], 478.0 [2]
5-Methyl-2-[4-(1-pyrazin-2-ylethylamino)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5037.0 [1], 663.0 [2]
5-Methyl-2-[4-(1-quinoxalin-6-ylethylamino)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5075.0 [1], 276.0 [2]
2-[4-[[(1S)-1-(2-Methoxypyrimidin-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC50481.0 [1], 5363.0 [2]
2-[4-[1-(4-Chloro-3-methylsulfonylphenyl)ethylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5019.0 [1], 36.0 [2]
2-[4-[[(1R)-1-(1,3-Benzodioxol-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5015.0 [1], 19.0 [2]
2-[4-[[(1S)-1-(1,3-Benzodioxol-5-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC502206.0 [1], 7074.0 [2]
5-Methyl-2-[4-[1-(4-methyl-3-methylsulfonylphenyl)ethylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5023.0 [1], 45.0 [2]
5-Methyl-2-(4-(quinolin-7-ylmethylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)benzonitrileIC5020.0 [1], 24.0 [2]
2-[4-[[(1R)-1-(4-Chloro-3-methylsulfonylphenyl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5012.0 [1], 17.0 [2]
2-[4-[[(1S)-1-(4-Chloro-3-methylsulfonylphenyl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC50430.0 [1], 4546.0 [2]
5-Methyl-2-[4-[[(1R)-1-quinoxalin-6-ylethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5015.0 [1], 45.0 [2]
5-Methyl-2-[4-[[(1S)-1-quinoxalin-6-ylethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50570.0 [1], 10000.0 [2]
5-Methyl-2-[4-[[6-(trifluoromethyl)pyridin-3-yl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5019.0 [1], 92.0 [2]
5-Chloro-2-[4-[[6-(trifluoromethyl)pyridin-3-yl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5037.0 [1], 842.0 [2]
5-Bromo-2-[4-[[(1R)-1-[6-(trifluoromethyl)pyridin-3-yl]ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5042.0 [1], 455.0 [2]
5-Methyl-2-[4-[[(1R)-1-[6-(trifluoromethyl)pyridin-3-yl]ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5022.0 [1], 42.0 [2]
5-Chloro-2-[4-[[(1R)-1-[6-(trifluoromethyl)pyridin-3-yl]ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5025.0 [1], 383.0 [2]
5-Fluoro-2-[4-[[6-(trifluoromethyl)pyridin-3-yl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5085.0 [1], 11432.0 [2]
2-[4-[[6-(Trifluoromethyl)pyridin-3-yl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5063.0 [1], 1814.0 [2]
5-Chloro-2-[4-[[2-methyl-6-(trifluoromethyl)pyridin-3-yl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50187.0 [1], 10000.0 [2]
5-Chloro-2-[4-[[6-(dimethylamino)pyridin-3-yl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50628.0 [1], 1190.0 [2]
5-Chloro-2-[4-[(6-methoxypyridin-3-yl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5059.0 [1], 169.0 [2]
5-Bromo-2-[4-[(6-methoxypyridin-3-yl)methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5078.0 [1], 325.0 [2]
5-Chloro-2-[4-[[3-chloro-5-(trifluoromethyl)pyridin-2-yl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5091.0 [1], 1128.0 [2]
5-Chloro-2-[4-[[5-(trifluoromethyl)pyridin-2-yl]methylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC50118.0 [1], 4886.0 [2]
(3R)-3-[[6-(4-Chloro-2-cyanophenyl)-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]-3-(6-methoxypyridin-3-yl)propanoic acidIC501379.0 [1], 10000.0 [2]
5-Chloro-2-[4-[[(1R)-3-hydroxy-1-[6-(trifluoromethyl)pyridin-3-yl]propyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]benzonitrileIC5090.0 [1], 903.0 [2]
2-[4-[[(1R)-3-Hydroxy-1-(6-methylpyridin-3-yl)propyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5012.0 [1], 31.0 [2]
2-[4-[[(1R)-1-[6-(Difluoromethyl)pyridin-3-yl]-3-hydroxypropyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5013.0 [1], 43.0 [2]
2-[4-[[(1S)-2-Hydroxy-1-(6-methoxypyridin-3-yl)ethyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC506.0 [1], 28.0 [2]
2-[4-[[(1R)-3-Hydroxy-1-(6-methoxypyridin-3-yl)propyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5014.0 [1], 20.0 [2]
2-[4-[[3-Hydroxy-1-[6-(trifluoromethyl)pyridin-3-yl]propyl]amino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl]-5-methylbenzonitrileIC5055.0 [1], 136.0 [2]



References

This online tool may be cited as follows

MLA

"Quest Database™ P2X2/P2X3 heterotrimeric receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/p2x2-p2x3-heterotrimeric-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ P2X2/P2X3 heterotrimeric receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/p2x2-p2x3-heterotrimeric-receptor-inhibitors-ic50-ki.
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