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Polycomb protein EED Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
(3R,4S)-1-[(1S)-7-Fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amineIC50290.0 [1], 660.0 [2]
(3R,4S)-1-[(1S)-7-Fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amineKi1.0 [1], 11.0 [2]
(3r,4s)-1-[(2-Bromo-6-Fluorophenyl)methyl]-N,N-Dimethyl-4-(1-Methyl-1h-Indol-3-Yl)pyrrolidin-3-AmineIC504100.0 [1], 8300.0 [2]
(3r,4s)-1-[(2-Bromo-6-Fluorophenyl)methyl]-N,N-Dimethyl-4-(1-Methyl-1h-Indol-3-Yl)pyrrolidin-3-AmineKi10.0 [1], 13.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amineIC502400.0 [1]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amineKi4.0 [1], 12.0 [2]
1-[4-[4-[(3S,4R)-4-(Dimethylamino)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)pyrrolidin-3-yl]phenyl]piperazin-1-yl]ethanoneIC5033.0 [1], 50.0 [2]
1-[4-[4-[(3S,4R)-4-(Dimethylamino)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)pyrrolidin-3-yl]phenyl]piperazin-1-yl]ethanoneKi0.29 [1], 0.7 [2]
6-[4-[(3S,4R)-4-(Dimethylamino)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)pyrrolidin-3-yl]piperidin-1-yl]pyridine-3-carboxamideIC50230.0 [1], 280.0 [2]
6-[4-[(3S,4R)-4-(Dimethylamino)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)pyrrolidin-3-yl]piperidin-1-yl]pyridine-3-carboxamideKi0.45 [1]
4-[3-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-1-methylindol-7-yl]-1-methylpiperazin-2-oneIC50100.0 [1], 190.0 [2]
4-[3-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-1-methylindol-7-yl]-1-methylpiperazin-2-oneKi0.74 [1]
[3-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-1-methylindol-7-yl]-(3-fluoroazetidin-1-yl)methanoneIC5031.0 [1], 180.0 [2]
[3-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-1-methylindol-7-yl]-(3-fluoroazetidin-1-yl)methanoneKi1.0 [1]
(3R,4S)-1-[(2-Chloro-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amineIC506900.0 [1], 10000.0 [2]
(3R,4S)-1-[(2-Chloro-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amineKi53.0 [1]
(1S,2R)-4-(7-Fluoro-2,3-dihydro-1H-inden-1-yl)-N,N-dimethyl-2-[4-(4-methylsulfonylpiperazin-1-yl)phenyl]cyclopentan-1-amineIC5044.0 [1], 57.0 [2]
(1S,2R)-4-(7-Fluoro-2,3-dihydro-1H-inden-1-yl)-N,N-dimethyl-2-[4-(4-methylsulfonylpiperazin-1-yl)phenyl]cyclopentan-1-amineKi0.3 [1]
9-Benzyl-5-(furan-2-ylmethylamino)-8,10-dihydro-7H-[1,2,4]triazolo[3,4-a][2,7]naphthyridine-6-carbonitrileIC50620.0 [1], 3280.0 [2], 4030.0 [3]
TazemetostatIC502.0 [1], 40.0 [2]
N-(Furan-2-Ylmethyl)-8-(4-Methylsulfonylphenyl)-[1,2,4]triazolo[4,3-C]pyrimidin-5-AmineIC5022.0 [1], 220.0 [2]
CID 123132213IC507.0 [1]
CID 123132213Ki0.3 [1]
(3r,4s)-1-[(2-Methoxyphenyl)methyl]-N,N-Dimethyl-4-(1-Methylindol-3-Yl)pyrrolidin-3-AmineKi600.0 [1]
1-[4-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]piperazin-1-yl]ethanoneKi2.6 [1], 3.0 [2]
(3R,4S)-1-[(2-Bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-phenylpyrrolidin-3-amineKi78.0 [1], 110.0 [2]
1-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]-N,N-dimethylpiperidine-4-carboxamideIC5040.0 [1], 70.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-[4-[4-(4-methylphenyl)piperazin-1-yl]phenyl]pyrrolidin-3-amineIC50150.0 [1], 220.0 [2]
1-[1-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]piperidin-4-yl]pyrrolidin-2-oneIC5080.0 [1], 120.0 [2]
[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methylphenyl]-(4-ethylpiperazin-1-yl)methanoneIC50290.0 [1], 460.0 [2]
(3R,4S)-4-[4-(6,8-Dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl)phenyl]-1-[(2-fluoro-6-methylphenyl)methyl]-N,N-dimethylpyrrolidin-3-amineIC50130.0 [1], 210.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methyl-N-pyridin-3-ylbenzamideIC5080.0 [1], 100.0 [2]
1-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]-N-methylpiperidine-4-carboxamideIC5050.0 [1], 110.0 [2]
6-(1,3-Benzodioxol-4-ylmethyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amineIC501000.0 [1], 1300.0 [2]
8-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-oneIC5060.0 [1], 140.0 [2]
1-[4-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methylbenzoyl]piperazin-1-yl]ethanoneIC50180.0 [1], 510.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methyl-N-pyridin-4-ylbenzamideIC5080.0 [1], 90.0 [2]
(3R,4S)-4-[4-(6,8-Dihydro-5H-imidazo[1,2-a]pyrazin-7-yl)phenyl]-1-[(2-fluoro-6-methylphenyl)methyl]-N,N-dimethylpyrrolidin-3-amineIC5070.0 [1], 100.0 [2]
4-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]-1-ethylpiperazin-2-oneIC5060.0 [1], 120.0 [2]
Methyl 4-[4-[(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]piperazine-1-carboxylateIC5030.0 [1], 40.0 [2]
N-[1-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]piperidin-4-yl]acetamideIC5040.0 [1], 160.0 [2]
Cyclopropyl-[4-[4-[(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methylbenzoyl]piperazin-1-yl]methanoneIC50340.0 [1], 440.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-[4-(4-phenylpiperazin-1-yl)phenyl]pyrrolidin-3-amineIC5050.0 [1], 90.0 [2]
1-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]-N,N-dimethylpiperidin-4-amineIC5040.0 [1], 100.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methyl-N-[2-(1-methylpyrrolidin-2-yl)ethyl]benzamideIC5080.0 [1], 100.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-[4-[4-(2-methylsulfonylphenyl)piperazin-1-yl]phenyl]pyrrolidin-3-amineIC5070.0 [1], 190.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-4-[4-[4-(3-fluorophenyl)sulfonylpiperazin-1-yl]phenyl]-N,N-dimethylpyrrolidin-3-amineIC5040.0 [1], 50.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methyl-N-(pyridin-3-ylmethyl)benzamideIC5080.0 [1], 100.0 [2]
N-[(3S)-1-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]pyrrolidin-3-yl]acetamideIC5090.0 [1], 240.0 [2]
6-[(2-Fluoro-5-methoxyphenyl)methyl]-1-propan-2-yl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amineIC501300.0 [1], 2900.0 [2]
2-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]-3,6,7,8,9,9a-hexahydro-1H-pyrido[1,2-a]pyrazin-4-oneIC50100.0 [1], 170.0 [2]
[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methylphenyl]-[4-(2-hydroxyethyl)piperazin-1-yl]methanoneIC50270.0 [1], 380.0 [2]
[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methylphenyl]-pyrrolidin-1-ylmethanoneIC50140.0 [1], 260.0 [2]
4-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]-N,N-dimethylpiperazine-1-sulfonamideIC5020.0 [1], 60.0 [2]
[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methylphenyl]-(4-methyl-1,4-diazepan-1-yl)methanoneIC50310.0 [1], 390.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-N,N,2-trimethylbenzamideIC50110.0 [1], 180.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-[4-[4-(4-methylphenyl)sulfonylpiperazin-1-yl]phenyl]pyrrolidin-3-amineIC5050.0 [1], 80.0 [2]
3-(1-Benzofuran-7-ylmethyl)piperidine-1-carboximidamideIC502500.0 [1], 2800.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methyl-N-(pyridin-2-ylmethyl)benzamideIC5070.0 [1], 80.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-[4-(4-pyridin-4-ylpiperazin-1-yl)phenyl]pyrrolidin-3-amineIC5010.0 [1]
6-(1-Benzofuran-4-ylmethyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amineIC502700.0 [1], 12400.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methyl-N-(pyridin-4-ylmethyl)benzamideIC5070.0 [1], 110.0 [2]
1-[4-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]-1,4-diazepan-1-yl]ethanoneIC50160.0 [1], 270.0 [2]
(4-Chlorophenyl)-[4-[4-[(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]piperazin-1-yl]methanoneIC5020.0 [1], 40.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methyl-N-[2-(4-methylpiperazin-1-yl)ethyl]benzamideIC5090.0 [1], 120.0 [2]
8-(2-Fluorophenyl)-5-(furan-2-ylmethylamino)-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrileIC5030.0 [1], 210.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-[4-(4-morpholin-4-ylpiperidin-1-yl)phenyl]pyrrolidin-3-amineIC5040.0 [1], 60.0 [2]
1-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]piperidine-4-carbonitrileIC5070.0 [1], 140.0 [2]
[4-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]piperazin-1-yl]-pyrrolidin-1-ylmethanoneIC5030.0 [1], 40.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-[4-(4-pyrimidin-2-ylpiperazin-1-yl)phenyl]pyrrolidin-3-amineIC5030.0 [1], 70.0 [2]
3-(1-Benzofuran-4-ylmethyl)piperidine-1-carboximidamideIC502100.0 [1], 2500.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-N,N-diethyl-2-methylbenzamideIC50100.0 [1], 250.0 [2]
3-(1,3-Benzodioxol-4-ylmethyl)piperidine-1-carboximidamideIC501600.0 [1], 3900.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-[4-[4-(1,3-thiazol-2-yl)piperazin-1-yl]phenyl]pyrrolidin-3-amineIC5030.0 [1], 40.0 [2]
[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methylphenyl]-(4-methylpiperazin-1-yl)methanoneIC50260.0 [1], 480.0 [2]
N-(Furan-2-ylmethyl)-8-[4-(pyrrolidin-1-ylmethyl)phenyl]-[1,2,4]triazolo[4,3-c]pyrimidin-5-amineIC507.0 [1], 32.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-N-(2-methoxyethyl)-N,2-dimethylbenzamideIC50130.0 [1], 140.0 [2]
N-[2-(Dimethylamino)ethyl]-4-[(3S,4R)-4-(dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-2-methylbenzamideIC5080.0 [1], 150.0 [2]
4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]-N,2-dimethyl-N-(oxolan-2-ylmethyl)benzamideIC50110.0 [1], 290.0 [2]
N-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]-N,1-dimethylpiperidin-4-amineIC5090.0 [1], 350.0 [2]
8-(1,3-Benzodioxol-4-ylmethyl)-1-propan-2-yl-5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-3-amineIC50430.0 [1], 2000.0 [2]
(3R,4S)-1-[(2-Fluoro-6-methylphenyl)methyl]-N,N-dimethyl-4-[4-(4-methylpiperidin-1-yl)phenyl]pyrrolidin-3-amineIC5040.0 [1], 140.0 [2]
AstemizoleIC5093800.0 [1]
3-BenzylpiperidineIC50500000.0 [1]
5-(2-Fluoro-phenyl)-2,3-dihydro-imidazo[2,1-a]isoquinolineIC506040.0 [1]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinolineKi950.0 [1]
9-Benzyl-5-chloro-7,8,9,10-tetrahydro-[1,2,4]triazolo[3,4-a][2,7]naphthyridine-6-carbonitrileIC50100000.0 [1]
[(5S)-6-[[(2S)-1-[[(2S)-1-Amino-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-[[(2S)-3-hydroxy-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]amino]-6-oxohexyl]-trimethylazaniumIC501650.0 [1]
2-[4-[4-[(3S,4R)-4-(Dimethylamino)-1-[(2-fluoro-6-methylphenyl)methyl]pyrrolidin-3-yl]phenyl]pyrazol-1-yl]acetamideKi2.6 [1]
(3R,4S)-1-[(1R)-7-Fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amineKi129.0 [1]
1-[4-[4-[(3R,4S)-4-(Dimethylamino)-1-[(1R)-7-fluoro-2,3-dihydro-1H-inden-1-yl]pyrrolidin-3-yl]phenyl]piperazin-1-yl]ethanoneKi18.0 [1]
1-[4-[4-[(3S,4R)-4-(Dimethylamino)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]pyrrolidin-3-yl]phenyl]piperazin-1-yl]ethanoneKi0.3 [1]
1-[4-[4-[(3S,4R)-4-(Dimethylamino)-1-[(1R)-7-fluoro-2,3-dihydro-1H-inden-1-yl]pyrrolidin-3-yl]phenyl]piperazin-1-yl]ethanoneKi3.0 [1]
1-[4-[4-[(3R,4S)-4-(Dimethylamino)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]pyrrolidin-3-yl]phenyl]piperazin-1-yl]ethanoneKi42.0 [1]
(3R,4As,10aS)-6-methoxy-3-[(3-methoxyphenyl)methyl]-1-methyl-3,4,4a,5,10,10a-hexahydro-2H-benzo[g]quinolineIC502500.0 [1]
5-(Furan-2-ylmethylamino)-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrileIC501000.0 [1]
8-[4-[(Dimethylamino)methyl]phenyl]-N-[(3-methylthiophen-2-yl)methyl]-[1,2,4]triazolo[4,3-c]pyrimidin-5-amineIC5049.0 [1]
8-[4-[(Dimethylamino)methyl]phenyl]-5-[(5-fluorothiophen-2-yl)methylamino]-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrileIC50510.0 [1]
5-(Furan-2-ylmethylamino)-8-phenyl-[1,2,4]triazolo[4,3-a]pyridine-6-carbonitrileIC5062.0 [1]
(3S,4R)-1-[(2-Bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methylindol-3-yl)pyrrolidin-3-amineKi80.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Polycomb protein EED Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Nov2024https://www.aatbio.com/data-sets/polycomb-protein-eed-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 21). Quest Database™ Polycomb protein EED Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/polycomb-protein-eed-inhibitors-ic50-ki.
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