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LDL-associated phospholipase A2 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
DarapladibIC500.25 [1]
DarapladibKi0.11 [1]
8-Hydroxy-4-oxo-N-phenyl-1H-quinoline-2-carboxamideIC5074.0 [1]
8-(Methanesulfonamido)-4-oxo-N-phenyl-1H-quinoline-2-carboxamideIC5027.0 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-[(1-methylpyrazol-4-yl)methyl]-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC500.01 [1], 0.06 [2], 3.0 [3]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-[(1-methylpyrazol-4-yl)methyl]-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideKi0.03 [1]
1-[2-[4-(3,4-Dichlorophenyl)piperazin-1-yl]-2-oxoethyl]-2-[(4-fluorophenyl)methylsulfanyl]-5-[(2-methoxypyrimidin-5-yl)methyl]pyrimidin-4-oneIC508.0 [1], 8.8 [2]
2-Fluoro-5-[2-[4-(4-methylpiperidin-4-yl)-2-oxopyrrolidin-1-yl]ethoxy]benzonitrile;formic acidIC50620.0 [1], 870.0 [2]
N-(3,4-Difluorophenyl)-8-hydroxy-4-oxo-1H-quinoline-2-carboxamideIC5023.0 [1], 24.0 [2], 48.0 [3]
8-Hydroxy-N-(2-methylphenyl)-4-oxo-1H-quinoline-2-carboxamideIC5016.0 [1], 32.0 [2], 44.0 [3]
N-(2,4-Difluorophenyl)-8-hydroxy-4-oxo-1H-quinoline-2-carboxamideIC5030.0 [1], 96.0 [2], 177.0 [3]
8-Hydroxy-N-(3-methylphenyl)-4-oxo-1H-quinoline-2-carboxamideIC5053.0 [1], 64.0 [2], 97.0 [3]
N-Cyclohexyl-8-hydroxy-4-oxo-1H-quinoline-2-carboxamideIC5034.0 [1], 48.0 [2], 98.0 [3]
N-[(2S)-Hexan-2-yl]-8-(methanesulfonamido)-4-oxo-1H-quinoline-2-carboxamideIC5032.0 [1], 170.0 [2], 830.0 [3]
N-[(2R)-Hexan-2-yl]-8-(methanesulfonamido)-4-oxo-1H-quinoline-2-carboxamideIC50980.0 [1], 9700.0 [2], 11000.0 [3]
N-(2,4-Difluorophenyl)-8-(methanesulfonamido)-4-oxo-1H-quinoline-2-carboxamideIC504.0 [1], 10.0 [2], 41.0 [3]
N-(4-Fluoro-2-methylphenyl)-8-(methanesulfonamido)-4-oxo-1H-quinoline-2-carboxamideIC503.0 [1], 10.0 [2], 59.0 [3]
N-(3-Fluoro-2-methylphenyl)-8-(methanesulfonamido)-4-oxo-1H-quinoline-2-carboxamideIC503.0 [1], 9.0 [2], 49.0 [3]
8-HydroxyquinolineIC50100000.0 [1]
Xanthurenic acidIC50100000.0 [1]
Lp-PLA2-IN-2IC5032.0 [1], 120.0 [2]
4-[2-[(4-Fluorophenyl)methylsulfanyl]-4-oxo-5-(pyrimidin-5-ylmethyl)pyrimidin-1-yl]-N-[(E)-octadec-9-enyl]butanamideIC500.4 [1], 0.7 [2]
2-[8-(4-Chlorophenyl)-8-oxooctylthio]-5-(5-pyrimidinylmethyl)-1,4-dihydropyrimidine-4-oneIC5054.0 [1]
Benzaldehyde O-benzoyloximeIC503800.0 [1]
4-Fluorobenzaldehyde O-benzoyloximeIC504400.0 [1]
3,4-Difluorobenzaldehyde O-benzoyloximeIC502000.0 [1]
N-[[4-(4-Chlorophenyl)phenyl]methyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-[(2-methoxypyrimidin-5-yl)methyl]-4-oxopyrimidin-1-yl]-N-methylacetamideIC500.2 [1]
2-Benzylsulfanyl-5-pyrimidin-5-ylmethyl-1H-pyrimidin-4-oneIC501100.0 [1], 1110.0 [2]
8-Hydroxy-N-phenylquinoline-2-carboxamideIC50100000.0 [1]
N-[[4-(4-Chlorophenyl)phenyl]methyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-[(1-methylpyrazol-4-yl)methyl]-4-oxopyrimidin-1-yl]-N-methylacetamideIC501.0 [1]
3-{2-[(2',6-Dimethyl[1,1'-Biphenyl]-3-Yl)amino]-1,3-Thiazol-4-Yl}propan-1-OlIC50230.0 [1], 7100.0 [2]
5-[2-(4,4-Dimethyl-2-Oxidanylidene-Pyrrolidin-1-Yl)ethoxy]-2-Fluoranyl-BenzenecarbonitrileIC503000.0 [1], 15000.0 [2]
2-Methoxy-3-[2-[2-methoxy-4-methyl-5-(2-methylphenyl)anilino]-1,3-thiazol-4-yl]propan-1-olIC503.6 [1], 320.0 [2]
3-[2-[2-(2-Aminoethoxy)-4-methyl-5-(2-methylphenyl)anilino]-1,3-thiazol-4-yl]-2-methoxypropan-1-olIC502.4 [1], 28.0 [2]
3-[3-[2-(2-Aminoethoxy)-4-methyl-5-(2-methylphenyl)anilino]pyrazol-1-yl]-2-methoxypropan-1-olIC501.4 [1], 18.0 [2]
2-Methoxy-3-[2-[4-methyl-3-(2-methylphenyl)anilino]-1,3-thiazol-4-yl]propan-1-olIC509.5 [1], 560.0 [2]
5-[2-[4-(1,4-Dimethylpiperidin-4-yl)-2-oxopyrrolidin-1-yl]ethoxy]-2-fluorobenzonitrileIC5075.0 [1], 270.0 [2]
5-[2-[4-(1,1-Dioxothian-4-yl)-2-oxopyrrolidin-1-yl]ethoxy]-2-fluorobenzonitrileIC503900.0 [1], 7900.0 [2]
1-[2-(4-Fluorophenoxy)ethyl]-4-(4-methyl-1,1-dioxothian-4-yl)pyrrolidin-2-oneIC50760.0 [1], 1500.0 [2]
5-[2-[(4R)-4-(1,4-Dimethylpiperidin-4-yl)-2-oxopyrrolidin-1-yl]ethoxy]-2-fluorobenzonitrileIC502700.0 [1], 7900.0 [2]
2-Fluoro-5-[2-[(4R)-4-methyl-2-oxo-4-propan-2-ylpyrrolidin-1-yl]ethoxy]benzonitrileIC505400.0 [1], 13000.0 [2]
2-Fluoro-5-[2-[(4S)-4-methyl-2-oxo-4-propan-2-ylpyrrolidin-1-yl]ethoxy]benzonitrileIC502300.0 [1], 6200.0 [2]
1-[2-(3,4-Difluorophenoxy)ethyl]-4-(4-methyl-1,1-dioxothian-4-yl)pyrrolidin-2-oneIC50160.0 [1], 290.0 [2]
2-Fluoro-5-[2-[(4R)-4-(4-methyl-1,1-dioxothian-4-yl)-2-oxopyrrolidin-1-yl]ethoxy]benzonitrileIC504300.0 [1], 6300.0 [2]
2-Fluoro-5-[2-[4-(4-methyl-1,1-dioxothian-4-yl)-2-oxopyrrolidin-1-yl]ethoxy]benzonitrileIC50110.0 [1], 180.0 [2]
5-[2-(4-Tert-butyl-2-oxopyrrolidin-1-yl)ethoxy]-2-fluorobenzonitrileIC50980.0 [1], 5100.0 [2]
2-Fluoro-5-[2-[4-(4-methyloxan-4-yl)-2-oxopyrrolidin-1-yl]ethoxy]benzonitrileIC50160.0 [1], 260.0 [2]
(4S)-1-[2-(3,4-Difluorophenoxy)ethyl]-4-(4-methyl-1,1-dioxothian-4-yl)pyrrolidin-2-oneIC5086.0 [1], 100.0 [2]
5-[2-[4-(1-Acetyl-4-methylpiperidin-4-yl)-2-oxopyrrolidin-1-yl]ethoxy]-2-fluorobenzonitrileIC50250.0 [1], 660.0 [2]
5-[2-[(4S)-4-(1,4-Dimethylpiperidin-4-yl)-2-oxopyrrolidin-1-yl]ethoxy]-2-fluorobenzonitrileIC5072.0 [1], 200.0 [2]
2-[8-(4-Chlorophenyl)-8-oxooctyl]sulfanyl-5-[(1-methyl-2-oxopyridin-4-yl)methyl]-1H-pyrimidin-6-oneIC5072.0 [1]
2-[8-(4-Chlorophenyl)-8-oxooctyl]sulfanyl-5-[(1-methyl-2-oxopyridin-4-yl)methyl]-1H-pyrimidin-6-oneKi41.0 [1]
N-(4-Fluorophenyl)-8-hydroxy-4-oxo-1H-quinoline-2-carboxamideIC5031.0 [1], 82.0 [2]
N-(2,3-Difluorophenyl)-8-hydroxy-4-oxo-1H-quinoline-2-carboxamideIC5055.0 [1], 154.0 [2]
N-(1-Adamantyl)-8-hydroxy-4-oxo-1H-quinoline-2-carboxamideIC5056.0 [1], 88.0 [2]
N-[(4-Fluorophenyl)methyl]-8-hydroxy-4-oxo-1H-quinoline-2-carboxamideIC5091.0 [1], 1200.0 [2]
8-Hydroxy-2-(piperidine-1-carbonyl)-1H-quinolin-4-oneIC502900.0 [1], 200000.0 [2]
N-(4-Chlorophenyl)-8-hydroxy-4-oxo-1H-quinoline-2-carboxamideIC5061.0 [1], 180.0 [2]
8-Hydroxy-N-(4-methylphenyl)-4-oxo-1H-quinoline-2-carboxamideIC50130.0 [1], 560.0 [2]
8-Hydroxy-N-(4-methoxyphenyl)-4-oxo-1H-quinoline-2-carboxamideIC50270.0 [1], 4100.0 [2]
8-Hydroxy-4-oxo-N-pentyl-1H-quinoline-2-carboxamideIC50360.0 [1], 11000.0 [2]
2'-Chloro-6-Methyl[1,1'-Biphenyl]-3-AmineIC50100000.0 [1]
OrlistatIC5050.0 [1]
BenzenesulfonamideIC501000000.0 [1]
1,6-Bis(cyclohexyloximinocarbonyl)hexaneIC5011000.0 [1]
N-(6-Methoxy-8-quinolyl)-4-toluenesulfonamideIC50100000.0 [1]
5,5-DimethylhydantoinIC501000000.0 [1]
RilapladibIC500.25 [1]
1-Methyl-3-(2-phenoxyethyl)imidazolidine-2,4-dioneIC501000000.0 [1]
Lp-PLA2-IN-3IC5014.0 [1]
3-[2-(4-Fluorophenoxy)ethyl]-5,5-dimethylimidazolidine-2,4-dioneIC5044000.0 [1]
(1E,2E)-3-Phenylacrylaldehyde O-benzoyloximeIC5025000.0 [1]
3,4-Difluorobenzaldehyde O-(3,4-difluorobenzoyl)oximeIC5038000.0 [1]
4-[[4-[4-Chloro-3-(trifluoromethyl)phenoxy]-3,5-difluorophenyl]methoxy]-6-(1,1-dioxo-1,4-thiazinan-4-yl)-1-methylpyrimidin-2-oneIC501.7 [1]
N-Dodecyl-2-(4-fluorobenzylthio)-4-oxo-5-(5-pyrimidinylmethyl)-1,4-dihydropyrimidine-1-acetamideIC500.3 [1]
N-Dodecyl-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-5-(pyrimidin-5-ylmethyl)pyrimidin-1-yl]-N-methylacetamideIC501.0 [1]
N-Octyl-2-(4-fluorobenzylthio)-4-oxo-5-(5-pyrimidinylmethyl)-1,4-dihydropyrimidine-1-acetamideIC507.0 [1]
N-Dodecyl-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-[(2-methoxypyrimidin-5-yl)methyl]-4-oxopyrimidin-1-yl]-N-methylacetamideIC501.0 [1]
2-[2-[(4-Fluorophenyl)methylsulfanyl]-4-oxo-5-(pyrimidin-5-ylmethyl)pyrimidin-1-yl]-N-methyl-N-octylacetamideIC5015.0 [1]
2-[2-[(4-Fluorophenyl)methylsulfanyl]-5-[(1-methylpyrazol-4-yl)methyl]-4-oxopyrimidin-1-yl]-N-(2-piperidin-1-ylethyl)-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC500.17 [1]
N-[[4-(4-Chlorophenyl)phenyl]methyl]-N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-5,6,7,8-tetrahydroquinazolin-1-yl]acetamideIC500.25 [1]
2-[5-Chloro-2-[(4-fluorophenyl)methylsulfanyl]-4-oxopyrimidin-1-yl]-N-[2-(diethylamino)ethyl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC503.0 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-5,6,7,8-tetrahydroquinazolin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC500.1 [1]
N-[[4-(4-Chlorophenyl)phenyl]methyl]-N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]acetamideIC500.4 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-5-propylpyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC500.8 [1]
2-[5-(2-Aminoethyl)-2-[(4-fluorophenyl)methylsulfanyl]-4-oxopyrimidin-1-yl]-N-[2-(diethylamino)ethyl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC5038.0 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-[2-(methanesulfonamido)ethyl]-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC501.0 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-(hydroxymethyl)-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC501.5 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-(2-hydroxyethyl)-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC502.0 [1]
N-[[4-(4-Chlorophenyl)phenyl]methyl]-N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-methyl-4-oxopyrimidin-1-yl]acetamideIC505.0 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-methyl-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC501.0 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-methylsulfanyl-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC500.8 [1]
N-[[4-(4-Chlorophenyl)phenyl]methyl]-N-[2-(diethylamino)ethyl]-2-[5-ethyl-2-[(4-fluorophenyl)methylsulfanyl]-4-oxopyrimidin-1-yl]acetamideIC501.0 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5,6-dimethyl-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC500.5 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-methoxy-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC5019.0 [1]
N-[2-(Diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-methylsulfinyl-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC500.8 [1]
2-[5-Bromo-2-[(4-fluorophenyl)methylsulfanyl]-4-oxopyrimidin-1-yl]-N-[2-(diethylamino)ethyl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC501.0 [1]
2-[5-(2-Acetamidoethyl)-2-[(4-fluorophenyl)methylsulfanyl]-4-oxopyrimidin-1-yl]-N-[2-(diethylamino)ethyl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamideIC506.0 [1]
2-[8-Oxo-8-(4-chlorophenyl)octyloxy]-5-(3-pyridinylmethyl)-1,4-dihydropyrimidine-4-oneIC5064.0 [1]
(E)-(Furan-2-ylmethylidene)amino benzoateIC5026000.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ LDL-associated phospholipase A2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.8 May2024https://www.aatbio.com/data-sets/ldl-associated-phospholipase-a2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 8). Quest Database™ LDL-associated phospholipase A2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/ldl-associated-phospholipase-a2-inhibitors-ic50-ki.
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