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Purinergic receptor P2Y1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
[(2R,3S,5R)-5-[6-(Methylamino)purin-9-yl]-2-(phosphonooxymethyl)oxolan-3-yl] dihydrogen phosphateIC50480.0 [1]
2-Methylthio-adenosine-5'-diphosphateIC50150.0 [1]
1-[2-(2-Tert-butylphenoxy)pyridin-3-yl]-3-[4-(trifluoromethoxy)phenyl]ureaIC5029.0 [1], 280.0 [2], 2100.0 [3]
1-[2-(2-Tert-butylphenoxy)pyridin-3-yl]-3-[4-(trifluoromethoxy)phenyl]ureaKi6.0 [1]
1-[2-[4-Chloro-1'-(2,2-dimethylpropyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-(5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl)ureaIC500.12 [1], 130.0 [2]
1-[2-[4-Chloro-1'-(2,2-dimethylpropyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-(5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl)ureaKi3.3 [1], 8.0 [2]
CID 44448831IC508.4 [1]
CID 44448831Ki0.78 [1]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC502.5 [1], 670.0 [2], 4900.0 [3]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi4.3 [1]
1-[2-(1'-Propan-2-ylspiro[2H-indole-3,4'-piperidine]-1-yl)phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC504700.0 [1], 29200.0 [2]
1-[2-(1'-Propan-2-ylspiro[2H-indole-3,4'-piperidine]-1-yl)phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi300.0 [1], 300.4 [2]
1-[2-[1'-(2-Methylpropyl)spiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC502200.0 [1], 8800.0 [2]
1-[2-[1'-(2-Methylpropyl)spiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi20.2 [1], 20.7 [2]
[(1R,2S,4S,5S)-4-[2-Chloro-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateIC5052.0 [1]
[(1R,2S,4S,5S)-4-[2-Chloro-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateKi2.5 [1]
[2-[[2-Chloro-6-(methylamino)purin-9-yl]methyl]-3-phosphonopropyl]phosphonic acidIC50616.6 [1], 620.0 [2]
[2-[[2-Chloro-6-(methylamino)purin-9-yl]methyl]-3-phosphonopropyl]phosphonic acidKi76.0 [1]
N-[2-(2-Tert-butylphenoxy)pyridin-3-yl]-5-[3-[3-(dimethylamino)-2,2-dimethylpropoxy]phenyl]-4-(trifluoromethyl)-1,3-thiazol-2-amineKi12.0 [1]
Benzyl 1-[2-[[4-(trifluoromethoxy)phenyl]carbamoylamino]phenyl]spiro[2H-indole-3,4'-piperidine]-1'-carboxylateIC505.9 [1], 10000.0 [2]
Benzyl 1-[2-[[4-(trifluoromethoxy)phenyl]carbamoylamino]phenyl]spiro[2H-indole-3,4'-piperidine]-1'-carboxylateKi36.6 [1]
1-(2-Spiro[2H-indole-3,1'-cyclobutane]-1-ylphenyl)-3-[4-(trifluoromethoxy)phenyl]ureaIC5010.5 [1], 4100.0 [2]
1-(2-Spiro[2H-indole-3,1'-cyclobutane]-1-ylphenyl)-3-[4-(trifluoromethoxy)phenyl]ureaKi7.6 [1]
Methyl 1-[2-[[4-(trifluoromethoxy)phenyl]carbamoylamino]phenyl]spiro[2H-indole-3,4'-piperidine]-1'-carboxylateIC505800.0 [1], 54200.0 [2]
Methyl 1-[2-[[4-(trifluoromethoxy)phenyl]carbamoylamino]phenyl]spiro[2H-indole-3,4'-piperidine]-1'-carboxylateKi13.3 [1]
1-(2-Spiro[2H-indole-3,1'-cyclohexane]-1-ylphenyl)-3-[4-(trifluoromethoxy)phenyl]ureaIC502.2 [1], 2000.0 [2]
1-(2-Spiro[2H-indole-3,1'-cyclohexane]-1-ylphenyl)-3-[4-(trifluoromethoxy)phenyl]ureaKi5.9 [1]
1-[2-(1'-Benzylspiro[2H-indole-3,4'-piperidine]-1-yl)phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC503300.0 [1], 18600.0 [2]
1-[2-(1'-Benzylspiro[2H-indole-3,4'-piperidine]-1-yl)phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi18.6 [1]
1-[2-[4-(4-Chlorophenyl)-1'-(2,2-dimethylpropyl)-5-fluoro-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC500.16 [1], 200.0 [2]
1-[2-[4-(4-Chlorophenyl)-1'-(2,2-dimethylpropyl)-5-fluoro-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi12.3 [1]
1-[2-[1'-(2,2-Dimethylpropyl)-5-fluoro-4-(4-fluorophenyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC500.09 [1], 140.0 [2]
1-[2-[1'-(2,2-Dimethylpropyl)-5-fluoro-4-(4-fluorophenyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi22.5 [1]
[3-(2-Iodo-6-methylaminopurin-9-yl)-2-phosphonomethylpropyl]-phosphonic acidIC50790.0 [1], 794.33 [2]
[3-(2-Iodo-6-methylaminopurin-9-yl)-2-phosphonomethylpropyl]-phosphonic acidKi66.0 [1]
[(1R,2S,4S,5S)-4-[2-Cyano-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateIC506900.0 [1], 6918.31 [2]
[(1R,2S,4S,5S)-4-[2-Cyano-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateKi540.0 [1]
[(1R,2S,4S,5S)-4-[2-Carbamoyl-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateIC501737.8 [1], 1750.0 [2]
[(1R,2S,4S,5S)-4-[2-Carbamoyl-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateKi650.0 [1]
6-(Methylamino)-9-[(1S,2S,4S,5R)-4-phosphonooxy-5-(phosphonooxymethyl)-2-bicyclo[3.1.0]hexanyl]purine-2-carboxylic acidIC50870.0 [1], 870.96 [2]
6-(Methylamino)-9-[(1S,2S,4S,5R)-4-phosphonooxy-5-(phosphonooxymethyl)-2-bicyclo[3.1.0]hexanyl]purine-2-carboxylic acidKi1430.0 [1]
[(1R,2S,4S,5S)-4-[2-Ethynyl-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateIC5093.0 [1], 93.33 [2]
[(1R,2S,4S,5S)-4-[2-Ethynyl-6-(methylamino)purin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateKi95.0 [1]
[(1R,2S,4S,5S)-4-[6-(Methylamino)-2-phenylpurin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateIC501940.0 [1], 1949.84 [2]
[(1R,2S,4S,5S)-4-[6-(Methylamino)-2-phenylpurin-9-yl]-2-phosphonooxy-1-bicyclo[3.1.0]hexanyl]methyl dihydrogen phosphateKi273.0 [1]
[(1R,2S,4S,5S)-1-(Hydroxymethyl)-4-[2-iodo-6-(methylamino)purin-9-yl]-2-bicyclo[3.1.0]hexanyl] dihydrogen phosphateIC501548.82 [1], 1560.0 [2]
[(1R,2S,4S,5S)-1-(Hydroxymethyl)-4-[2-iodo-6-(methylamino)purin-9-yl]-2-bicyclo[3.1.0]hexanyl] dihydrogen phosphateKi706.0 [1]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2H-pyrrolo[2,3-c]pyridine-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC5010.7 [1], 4000.0 [2]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2H-pyrrolo[2,3-c]pyridine-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi11.5 [1]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2H-pyrrolo[3,2-c]pyridine-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC50346.0 [1], 40000.0 [2]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2H-pyrrolo[3,2-c]pyridine-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi617.2 [1]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2H-pyrrolo[2,3-b]pyridine-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC50503.0 [1], 40000.0 [2]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2H-pyrrolo[2,3-b]pyridine-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi253.0 [1]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2,3-dihydroquinoline-4,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC509.9 [1], 6300.0 [2]
1-[2-[1'-(2,2-Dimethylpropyl)spiro[2,3-dihydroquinoline-4,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi4.6 [1]
1'-(2,2-Dimethylpropyl)-4-(trifluoromethyl)-1-[2-[[5-[4-(trifluoromethyl)phenyl]-1,3,4-thiadiazol-2-yl]amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olIC500.08 [1], 16.0 [2]
1'-(2,2-Dimethylpropyl)-4-(trifluoromethyl)-1-[2-[[5-[4-(trifluoromethyl)phenyl]-1,3,4-thiadiazol-2-yl]amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olKi16.0 [1]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[[5-(2,5-dimethylpyrazol-3-yl)-1,3,4-thiadiazol-2-yl]amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olIC500.2 [1], 6.6 [2]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[[5-(2,5-dimethylpyrazol-3-yl)-1,3,4-thiadiazol-2-yl]amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olKi6.6 [1]
4-Chloro-1-[2-[[5-(2-chlorophenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)spiro[2H-indole-3,4'-piperidine]-7-olIC509.8 [1], 28.0 [2]
4-Chloro-1-[2-[[5-(2-chlorophenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)spiro[2H-indole-3,4'-piperidine]-7-olKi28.0 [1]
4-Chloro-1-[2-[[5-(3-chlorophenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)spiro[2H-indole-3,4'-piperidine]-7-olIC503.6 [1], 16.0 [2]
4-Chloro-1-[2-[[5-(3-chlorophenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)spiro[2H-indole-3,4'-piperidine]-7-olKi16.0 [1]
4-Chloro-1-[2-[[5-(4-chlorophenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)spiro[2H-indole-3,4'-piperidine]-7-olIC501.6 [1], 13.0 [2]
4-Chloro-1-[2-[[5-(4-chlorophenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)spiro[2H-indole-3,4'-piperidine]-7-olKi13.0 [1]
1-[2-[[5-(4-Tert-butylphenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-4-carbonitrileIC500.34 [1], 10.0 [2]
1-[2-[[5-(4-Tert-butylphenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-4-carbonitrileKi9.7 [1]
Methyl 1-[2-[[5-(4-tert-butylphenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-4-carboxylateIC500.32 [1], 8.0 [2]
Methyl 1-[2-[[5-(4-tert-butylphenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-4-carboxylateKi8.0 [1]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[[5-[4-(trifluoromethoxy)phenyl]-1,3,4-thiadiazol-2-yl]amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olIC500.63 [1], 13.0 [2]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[[5-[4-(trifluoromethoxy)phenyl]-1,3,4-thiadiazol-2-yl]amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olKi13.0 [1]
1-[2-[1'-(2,2-Dimethylpropyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaIC500.23 [1]
1-[2-[1'-(2,2-Dimethylpropyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]-3-[4-(trifluoromethoxy)phenyl]ureaKi4.0 [1], 10.3 [2]
1'-(2,2-Dimethylpropyl)-1-[2-[(5-phenyl-1,3,4-thiadiazol-2-yl)amino]phenyl]-4-(trifluoromethyl)spiro[2H-indole-3,4'-piperidine]-7-olIC500.19 [1], 10.0 [2]
1'-(2,2-Dimethylpropyl)-1-[2-[(5-phenyl-1,3,4-thiadiazol-2-yl)amino]phenyl]-4-(trifluoromethyl)spiro[2H-indole-3,4'-piperidine]-7-olKi9.6 [1]
1-[2-[[5-(4-Tert-butylphenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)-4-(trifluoromethyl)spiro[2H-indole-3,4'-piperidine]-7-olIC500.21 [1], 26.0 [2]
1-[2-[[5-(4-Tert-butylphenyl)-1,3,4-thiadiazol-2-yl]amino]phenyl]-1'-(2,2-dimethylpropyl)-4-(trifluoromethyl)spiro[2H-indole-3,4'-piperidine]-7-olKi26.0 [1]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[(5-pyrazin-2-yl-1,3,4-thiadiazol-2-yl)amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olIC501.5 [1], 6.5 [2]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[(5-pyrazin-2-yl-1,3,4-thiadiazol-2-yl)amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olKi6.5 [1]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[(3-phenyl-1,2,4-thiadiazol-5-yl)amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olIC506.0 [1], 6.4 [2]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[(3-phenyl-1,2,4-thiadiazol-5-yl)amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olKi6.0 [1]
1-(5-Chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl)-3-[2-[1'-(2,2-dimethylpropyl)-5-fluoro-4-(4-fluorophenyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]ureaIC500.12 [1], 180.0 [2]
1-(5-Chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl)-3-[2-[1'-(2,2-dimethylpropyl)-5-fluoro-4-(4-fluorophenyl)-7-hydroxyspiro[2H-indole-3,4'-piperidine]-1-yl]phenyl]ureaKi10.2 [1]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[(5-phenyl-1,3-thiazol-2-yl)amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olIC502.3 [1], 16.0 [2]
4-Chloro-1'-(2,2-dimethylpropyl)-1-[2-[(5-phenyl-1,3-thiazol-2-yl)amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olKi17.0 [1]
1'-(2,2-Dimethylpropyl)-4-fluoro-1-[2-[[5-[4-(trifluoromethoxy)phenyl]-1,3,4-thiadiazol-2-yl]amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olIC502.7 [1], 5.0 [2]
1'-(2,2-Dimethylpropyl)-4-fluoro-1-[2-[[5-[4-(trifluoromethoxy)phenyl]-1,3,4-thiadiazol-2-yl]amino]phenyl]spiro[2H-indole-3,4'-piperidine]-7-olKi5.3 [1]
4-({[(3,4-Dichlorophenyl)amino]carbonyl}amino)-N-(3,4-dimethyl-5-isoxazolyl)benzenesulfonamideIC50140.0 [1]
4-({[(3,4-Dichlorophenyl)amino]carbonyl}amino)-N-(3,4-dimethyl-5-isoxazolyl)benzenesulfonamideKi13000.0 [1]
N-[2-(2-Tert-butylphenoxy)pyridin-3-yl]-5-phenyl-1,3-thiazol-2-amineKi15.0 [1]
N-[2-(2-Tert-butylphenoxy)pyridin-3-yl]-5-[4-(trifluoromethyl)phenyl]-1,3,4-thiadiazol-2-amineKi7.0 [1]
CID 46911435IC50630.0 [1]
CID 46911435Ki140.0 [1]
2-(2-(2-Tert-butylphenoxy)pyridin-3-ylamino)-4-(trifluoromethyl)thiazole-5-carbonitrileKi21.0 [1]
3-[2-[[2-(2-Tert-butylphenoxy)pyridin-3-yl]amino]-5-phenyl-1,3-thiazol-4-yl]-3-methylbutanoic acidKi207.0 [1]
N-[2-(2-Tert-butylphenoxy)pyridin-3-yl]-5-methyl-4-(trifluoromethyl)-1,3-thiazol-2-amineKi11.0 [1]
N-[2-(2-Tert-butylphenoxy)pyridin-3-yl]-4-ethyl-5-phenyl-1,3-thiazol-2-amineKi12.0 [1]
2-[2-[[2-(2-Tert-butylphenoxy)pyridin-3-yl]amino]-4-(trifluoromethyl)-1,3-thiazol-5-yl]phenolKi435.0 [1]
4-Tert-butyl-N-[2-(2-tert-butylphenoxy)pyridin-3-yl]-5-phenyl-1,3-thiazol-2-amineKi31.0 [1]
N-[2-(2-Tert-butylphenoxy)pyridin-3-yl]-5-(2-fluorophenyl)-4-(trifluoromethyl)-1,3-thiazol-2-amineKi7.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Purinergic receptor P2Y1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.8 May2024https://www.aatbio.com/data-sets/purinergic-receptor-p2y1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 8). Quest Database™ Purinergic receptor P2Y1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/purinergic-receptor-p2y1-inhibitors-ic50-ki.
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