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Presenilin 1 Inhibitors (IC50, Ki)

Structure
▲
▼
Compound Name
▲
▼
Standard Type
▲
▼
Standard Values (in nM)
▲
▼
CID 25164607IC501.3 [1], 4.0 [2], 46.0 [3]
DL-alpha-TocopherolIC50100000.0 [1]
(4S,4As,10bS)-10b-(4-chlorophenyl)sulfonyl-4-(2-ethylsulfonylethyl)-7,10-difluoro-2,4,4a,5-tetrahydro-1H-pyrano[3,4-c]chromeneIC503.0 [1], 5.0 [2]
(4S,4As,10bS)-10b-(4-chlorophenyl)sulfonyl-7,10-difluoro-4-(2-propan-2-ylsulfonylethyl)-2,4,4a,5-tetrahydro-1H-pyrano[3,4-c]chromeneIC5024.0 [1], 26.0 [2]
2-[[2,5,7,8-Tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydrochromen-6-yl]oxy]acetic acidIC5012000.0 [1], 26000.0 [2]
Methyl 2-[[2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydrochromen-6-yl]oxy]acetateIC50100000.0 [1]
2-[(4S,4As,10bS)-10b-(4-chlorophenyl)sulfonyl-7,10-difluoro-2,4,4a,5-tetrahydro-1H-pyrano[3,4-c]chromen-4-yl]ethanolIC5018.0 [1], 20.0 [2]
2-[(4S,4As,10bS)-10b-(4-chlorophenyl)sulfonyl-7,10-difluoro-2,4,4a,5-tetrahydro-1H-pyrano[3,4-c]chromen-4-yl]ethyl N-methylcarbamateIC508.0 [1]
3-[(4S,4As,10bS)-10b-(4-chlorophenyl)sulfonyl-7,10-difluoro-2,4,4a,5-tetrahydro-1H-pyrano[3,4-c]chromen-4-yl]propanenitrileIC5022.0 [1], 37.0 [2]
2-[(4S,4As,10bS)-10b-(4-chlorophenyl)sulfonyl-7,10-difluoro-2,4,4a,5-tetrahydro-1H-pyrano[3,4-c]chromen-4-yl]ethyl N-ethylcarbamateIC5024.0 [1], 48.0 [2]
2-[6-Chloro-9-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienyl]carbazol-2-yl]propanoic acidIC5026000.0 [1], 31622.78 [2]
2-[6-Chloro-9-[(E,7R,11R)-3,7,11,15-tetramethylhexadec-2-enyl]carbazol-2-yl]propanoic acidIC5023000.0 [1], 50000.0 [2]
2,5,7,8-Tetramethyl-6-octoxy-3,4-dihydrochromene-2-carboxylic acidIC5050000.0 [1], 57000.0 [2]
2,5,7,8-Tetramethyl-6-undecoxy-3,4-dihydrochromene-2-carboxylic acidIC5028000.0 [1], 50000.0 [2]
2,5,7,8-Tetramethyl-6-tetradecoxy-3,4-dihydrochromene-2-carboxylic acidIC5014000.0 [1], 29000.0 [2]
2,5,7,8-Tetramethyl-6-[(E,7R,11R)-3,7,11,15-tetramethylhexadec-2-enoxy]-3,4-dihydrochromene-2-carboxylic acidIC5026000.0 [1], 42000.0 [2]
2,5,7,8-Tetramethyl-6-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienoxy]-3,4-dihydrochromene-2-carboxylic acidIC5028000.0 [1], 39000.0 [2]
2-[(2,5,7,8-Tetramethyl-2-octoxycarbonyl-3,4-dihydrochromen-6-yl)oxy]acetic acidIC5035000.0 [1], 42000.0 [2]
2-[(2,5,7,8-Tetramethyl-2-undecoxycarbonyl-3,4-dihydrochromen-6-yl)oxy]acetic acidIC5012000.0 [1], 23000.0 [2]
2-[(2,5,7,8-Tetramethyl-2-tetradecoxycarbonyl-3,4-dihydrochromen-6-yl)oxy]acetic acidIC5022000.0 [1], 34000.0 [2]
2-[[2,5,7,8-Tetramethyl-2-[(E,7R,11R)-3,7,11,15-tetramethylhexadec-2-enoxy]carbonyl-3,4-dihydrochromen-6-yl]oxy]acetic acidIC5024000.0 [1], 36000.0 [2]
2-[[2,5,7,8-Tetramethyl-2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienoxy]carbonyl-3,4-dihydrochromen-6-yl]oxy]acetic acidIC5025000.0 [1], 27000.0 [2]
2-[[2,5,7,8-Tetramethyl-2-[(4R,8R)-4,8,12-trimethyltridecyl]-3,4-dihydrochromen-6-yl]oxy]acetic acidIC5011000.0 [1], 24000.0 [2]
2-(4,6-Diphenethoxypyrimidin-2-ylthio)hexanoic acidIC5022800.0 [1]
2-(4,6-Bis(2-cyclohexylethoxy)pyrimidin-2-ylthio)hexanoic acidIC505100.0 [1]
(2E)-2-[[2,5-Bis[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC501200.0 [1]
(2E)-2-[[5-Phenyl-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC5011900.0 [1]
(2E)-2-[[5-Phenoxy-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC5014900.0 [1]
(2E)-2-[[5-Phenylmethoxy-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC5019300.0 [1]
(2E)-2-[[5-[(E)-3-Phenylprop-2-enoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC504100.0 [1]
(2E)-2-[[5-[(4-Butylphenyl)methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC504900.0 [1]
(2E)-2-[[5-[(4-Phenylphenyl)methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC5011900.0 [1]
(2E)-2-[[5-[(4-Phenylmethoxyphenyl)methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC508500.0 [1]
(2E)-2-[[5-[(4-Fluorophenyl)methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC507000.0 [1]
(2E)-2-[[5-[(3,4-Dichlorophenyl)methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC502000.0 [1]
(2E)-2-[[5-[[3,5-Bis(trifluoromethyl)phenyl]methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC50790.0 [1]
(2E)-2-[[5-(Pyridin-3-ylmethoxy)-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC5032100.0 [1]
(2E)-2-[[5-(1-Benzothiophen-2-ylmethoxy)-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC504600.0 [1]
(2E)-2-[[2-[[4-(Trifluoromethyl)phenyl]methoxy]-5-[[2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-4-yl]methoxy]phenyl]methylidene]hexanoic acidIC502300.0 [1]
(2E)-2-[[5-[[4-Methoxy-2-(trifluoromethyl)quinolin-6-yl]methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC50630.0 [1]
(2E)-2-[[5-[[4-(2-Methyl-1,3-thiazol-4-yl)phenyl]methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC5020200.0 [1]
(2E)-2-[[5-[(4-Pyridin-2-yloxyphenyl)methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC505000.0 [1]
(2E)-2-[[5-[[4-(2-Morpholin-4-ylethoxy)phenyl]methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC502200.0 [1]
(2E)-2-[[5-Hydroxy-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC5040000.0 [1]
(2E)-2-[[5-(2,2-Diphenylethoxy)-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC5011400.0 [1]
(2E)-2-[[5-[[4-(Trifluoromethyl)cyclohexyl]methoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC501000.0 [1]
(2E)-2-[[5-[2-[4-(Trifluoromethyl)phenyl]ethoxy]-2-[[4-(trifluoromethyl)phenyl]methoxy]phenyl]methylidene]hexanoic acidIC501500.0 [1]
2-[(4R,4Ar,10bR)-10b-(4-chlorophenyl)sulfonyl-7,10-difluoro-2,4,4a,5-tetrahydro-1H-pyrano[3,4-c]chromen-4-yl]ethanolIC50320.0 [1]
(4R,4Ar,10bR)-10b-(4-chlorophenyl)sulfonyl-7,10-difluoro-4-(2-methylsulfonylethyl)-2,4,4a,5-tetrahydro-1H-pyrano[3,4-c]chromeneIC50377.0 [1]
2-[(1S)-1-[(2S,5R)-5-[4-Chloro-2-(trifluoromethyl)phenyl]oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC509.1 [1]
2-[(1S)-1-[(2S,5R)-5-[4-Chloro-5-fluoro-2-(trifluoromethyl)phenyl]oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC507.84 [1]
2-[[3-(4-Chlorophenyl)cyclohexyl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5098.0 [1]
2-[(1R,2R)-2-(3,5-Difluorophenyl)cyclopentyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50563.0 [1]
2-[(1R,2R)-2-[(3,5-Difluorophenyl)methyl]cyclopentyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50561.0 [1]
2-[3-[[4-Fluoro-2-(trifluoromethyl)phenoxy]methyl]cyclobutyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50303.0 [1]
7-(4-Methylimidazol-1-yl)-2-[(1R,2R)-2-naphthalen-1-yloxycyclobutyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50164.0 [1]
2-[(1S)-1-[(2S,5R)-5-(4-Chloro-2,5-difluorophenyl)oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5011.4 [1]
2-[(1S)-1-[(2S,5R)-5-(4-Chloro-5-fluoro-2-methoxyphenyl)oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5011.1 [1]
7-(4-Methylimidazol-1-yl)-2-[[(2R,5S)-5-[4-(1,1,2,2,2-pentafluoroethyl)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50157.0 [1]
7-(4-Methylimidazol-1-yl)-2-[[(2S,5R)-5-[2-(trifluoromethyl)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5073.3 [1]
7-(4-Methylimidazol-1-yl)-2-[[(2S,4R,5R)-4-methyl-5-[4-(trifluoromethyl)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5073.5 [1]
2-[(1S)-1-[(2S,5R)-5-(3,4-Dichloro-5-fluorophenyl)oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC505.78 [1]
(3R)-3-Methyl-7-(4-methylimidazol-1-yl)-2-[[(2R,5S)-5-[4-(trifluoromethyl)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5046.4 [1]
(3S)-3-Methyl-7-(4-methylimidazol-1-yl)-2-[[(2R,5S)-5-[4-(trifluoromethyl)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5019.8 [1]
2-[(1S)-1-[(2S,5R)-5-[3,5-Difluoro-4-(trifluoromethyl)phenyl]oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC503.34 [1]
7-(4-Methylimidazol-1-yl)-2-[(1S)-1-[(2S,5R)-5-[4-(trifluoromethyl)phenyl]oxolan-2-yl]ethyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5014.3 [1]
2-[(1S)-1-[(2S,5R)-5-(4-Chloro-3,5-difluorophenyl)oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC505.48 [1]
2-[(1S)-1-[(2S,5R)-5-[4,5-Difluoro-2-(trifluoromethyl)phenyl]oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5033.5 [1]
2-[(1S)-1-[(2S,5R)-5-[4-Chloro-3-fluoro-2-(trifluoromethyl)phenyl]oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5010.0 [1]
2-[(1S)-1-[(2S,5R)-5-[4-Fluoro-2-(trifluoromethyl)phenyl]oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5024.2 [1]
2-[(1S)-1-[(2S,5R)-5-[3-Fluoro-4-(trifluoromethyl)phenyl]oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC508.35 [1]
2-[(1R,2R)-2-(3-Chloro-4-fluoro-2-methylphenoxy)cyclobutyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50146.0 [1]
7-(4-Methylimidazol-1-yl)-2-[[(2S,4S,5R)-4-methyl-5-[4-(trifluoromethyl)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5038.4 [1]
7-(4-Methylimidazol-1-yl)-2-[[(2R,6S)-6-[4-(trifluoromethyl)phenyl]oxan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5096.6 [1]
7-(4-Methylimidazol-1-yl)-2-[[(2S,3S,5R)-3-methyl-5-[4-(trifluoromethyl)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5025.0 [1]
2-[(1R,2R)-2-[(7-Fluoro-2,3-dihydro-1H-inden-4-yl)oxy]cyclobutyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50162.0 [1]
7-(4-Methylimidazol-1-yl)-2-[(1S)-1-[(2S,5R)-5-[5-(trifluoromethyl)thiophen-2-yl]oxolan-2-yl]ethyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5052.4 [1]
2-[[(2S,5R)-5-(4-Chloro-2-methoxyphenyl)oxolan-2-yl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5021.6 [1]
7-(4-Methylimidazol-1-yl)-2-[[(2S,5R)-5-[4-(trifluoromethyl)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5027.6 [1]
7-(4-Methylimidazol-1-yl)-2-[(1R,2S)-2-[2-(trifluoromethyl)phenoxy]cyclobutyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50469.0 [1]
7-(4-Methylimidazol-1-yl)-2-[[2-methyl-5-[4-(trifluoromethyl)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC501040.0 [1]
7-(4-Methylimidazol-1-yl)-2-[3-[2-(trifluoromethyl)phenoxy]cyclobutyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50789.0 [1]
2-[[3-[2-Chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-1,2-oxazol-5-yl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50711.0 [1]
2-[(1R,2R)-2-(6,7-Difluoronaphthalen-1-yl)oxycyclobutyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5060.6 [1]
2-[(1S)-1-[(2S,5R)-5-[2-Methoxy-4-(trifluoromethyl)phenyl]oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5015.0 [1]
2-[[5-(3,4-Dichlorophenyl)oxolan-2-yl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50117.0 [1]
2-[(1R,2R)-2-(4-Chloro-3-propan-2-ylphenoxy)cyclobutyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50158.0 [1]
2-[[3-[2-Chloro-3-(trifluoromethyl)phenyl]-4,5-dihydro-1,2-oxazol-5-yl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50429.0 [1]
2-[[3-[4-Chloro-3-(trifluoromethyl)phenyl]-4,5-dihydro-1,2-oxazol-5-yl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50483.0 [1]
7-(4-Methylimidazol-1-yl)-2-[(1R,2R)-2-[3-(trifluoromethyl)phenoxy]cyclobutyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50217.0 [1]
2-[[(2S,5R)-5-[3-Fluoro-4-(trifluoromethyl)phenyl]oxolan-2-yl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5015.7 [1]
7-(4-Methylimidazol-1-yl)-2-[[(2S,5R)-5-[4-(trifluoromethoxy)phenyl]oxolan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5060.3 [1]
2-[2-(4-Chlorophenoxy)cyclohexyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50591.0 [1]
2-[(1R,2S)-2-[4-Fluoro-2-(trifluoromethyl)phenoxy]cyclopentyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50140.0 [1]
2-[[(2S,5R)-5-(4-Cyclopropylphenyl)oxolan-2-yl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5063.8 [1]
7-(4-Methylimidazol-1-yl)-2-[[(2R,6R)-6-[4-(trifluoromethyl)phenyl]oxan-2-yl]methyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5029.9 [1]
7-(4-Methylimidazol-1-yl)-2-[(1R,2R)-2-[2-(trifluoromethyl)phenoxy]cyclopentyl]-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC50300.0 [1]
2-[[(2S,5R)-5-[4-(1,1-Difluoroethyl)phenyl]oxolan-2-yl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5073.3 [1]
2-[(1S)-1-[(2S,5R)-5-[4-Chloro-2-(trifluoromethoxy)phenyl]oxolan-2-yl]ethyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5014.5 [1]
2-[[(1R,3S)-3-(4-Chlorophenyl)cyclohexyl]methyl]-7-(4-methylimidazol-1-yl)-3,4-dihydropyrido[1,2-a]pyrazine-1,6-dioneIC5080.0 [1]
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References

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MLA

"Quest Database™ Presenilin 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 8 May. 2024, https://www.aatbio.com/data-sets/presenilin-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 8). Quest Database™ Presenilin 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/presenilin-1-inhibitors-ic50-ki.
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