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(1S,2S)-1,2-dihydroxypropane-1,2,3-tricarboxylic acid
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50% inhibition at 0.00015 mM
(2E)-3-phenylprop-2-en-1-yl 2-[[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]amino]benzoate
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50% inhibition at 0.00034 mM
(2R)-2-[(2S)-8-(3,5-dichlorophenyl)-2-hydroxyoctyl]-2-hydroxysuccinic acid
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50% inhibition at 0.0021 mM
1,3,8-trihydroxy-2-(3-methoxyphenyl)-6-methylanthracene-9,10-dione
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-
1,3,8-trihydroxy-2-(4-methoxyphenyl)-6-methylanthracene-9,10-dione
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1,3,8-trihydroxy-2-iodo-6-methylanthracene-9,10-dione
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1,3,8-trihydroxy-6-methyl-2-(1-methyl-1H-pyrazol-4-yl)anthracene-9,10-dione
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1,3,8-trihydroxy-6-methyl-2-(3-methylphenyl)anthracene-9,10-dione
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1,3,8-trihydroxy-6-methyl-2-(pyridin-3-yl)anthracene-9,10-dione
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1,3,8-trihydroxy-6-methyl-2-phenylanthracene-9,10-dione
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1,3,8-trihydroxy-6-methyl-2-[(morpholin-4-yl)methyl]anthracene-9,10-dione
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1,3,8-trihydroxy-6-methyl-2-[(piperidin-1-yl)methyl]anthracene-9,10-dione
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1,3,8-trihydroxy-6-methyl-2-[[methyl(phenyl)amino]methyl]anthracene-9,10-dione
-
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1,3-dibromo-2,4,5-trihydroxy-7-methylanthracene-9,10-dione
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1-chloro-2,4,5-trihydroxy-7-methylanthracene-9,10-dione
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2,4,5-trihydroxy-7-methyl-1,3-di(pyridin-3-yl)anthracene-9,10-dione
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-
2-chloro-1,3,8-trihydroxy-6-methylanthracen-9(10H)-one
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2-chloro-1,3,8-trihydroxy-6-methylanthracene-9,10-dione
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2-hydroxy-2-[(S-methylsulfonimidoyl)methyl]butanedioic acid
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weak, reversible
3,3,14,14-tetramethylhexadecanedioic acid
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i.e. Medica-16
3,5-dichloro-2-hydroxy-N-(4-methoxybiphenyl-3-yl)benzenesulfonamide
3,5-dichloro-N-(2,4,6-triphenyl-phenyl)-2-hydroxybenzenesulfonamide
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50% inhibition at 0.00019 mM
3,5-dichloro-N-(3,5-di-tert-butylphenyl)-2-hydroxybenzenesulfonamide
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50% inhibition at 0.0011 mM
3-(1,3-benzoxazol-5-yl)-5,7-dihydroxy-9-methyl-3,4-dihydro-2H-anthra[2,3-e][1,3]oxazine-6,11-dione
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-
4-chloro-1,3,8-trihydroxy-6-methylanthracen-9(10H)-one
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-
4-[[(2-hexyl-6-oxo-7,8,9,10-tetrahydro-6H-dibenzo[b,d]pyran-3-yl)oxy]methyl]-5-methylfuran-2-carboxylic acid
0.01 mM, 95% inhibition. 0.1 mM, 100% inhibition
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4-[[(3,4-dibenzyl-2-oxo-2H-1-benzopyran-7-yl)oxy]methyl]-5-methylfuran-2-carboxylic acid
0.01 mM, 3% inhibition. 0.1 mM, 64% inhibition
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4-[[(3,4-dibenzyl-6-methyl-2-oxo-2H-1-benzopyran-7-yl)oxy]methyl]-5-methylfuran-2-carboxylic acid
0.01 mM, 32% inhibition. 0.1 mM, 84% inhibition
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4-[[(6-hexyl-2-oxo-4-phenyl-2H-1-benzopyran-7-yl)oxy]methyl]-5-methylfuran-2-carboxylic acid
0.01 mM, 53% inhibition. 0.1 mM, 92% inhibition
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5,7-dihydroxy-9-methyl-3-phenyl-3,4-dihydro-2H-anthra[2,3-e][1,3]oxazine-6,11-dione
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5-methyl-2-(1-methylethyl)cyclohexyl 2-[[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]amino]benzoate
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50% inhibition at 0.00037 mM
5-methyl-4-[[(2-oxo-4-phenyl-2H-1-benzopyran-7-yl)oxy]methyl]furan-2-carboxylic acid
0.01 mM,32% inhibition. 0.1 mM, 84% inhibition
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5-methyl-4-[[(2-oxo-4-phenyl-6-propyl-2H-1-benzopyran-7-yl)oxy]methyl]furan-2-carboxylic acid
0.01 mM, 97% inhibition. 0.1 mM, 97% inhibition
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5-methyl-4-[[(4-methyl-2-oxo-3-phenyl-2H-1-benzopyran-7-yl)oxy]methyl]furan-2-carboxylic acid
0.01 mM, 45% inhibition. 0.1 mM, 101% inhibition
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5-methyl-4-[[(4-methyl-6-oxo-7,8,9,10-tetrahydro-6H-dibenzo[b,d]pyran-3-yl)oxy]methyl]furan-2-carboxylic acid
0.01 mM, 17% inhibition. 0.1 mM, 90% inhibition
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5-[(2,3-dimethylbenzene-1-sulfonyl)amino]-2-methyl-1-benzofuran-3-carboxylic acid
0.01 mM, 11% inhibition. 0.1 mM, 43% inhibition
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5-[(4-fluoro-2-methylbenzene-1-sulfonyl)amino]-2-methyl-1-benzofuran-3-carboxylic acid
0.01 mM, 3% inhibition. 0.1 mM, 9% inhibition
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5-[(4-fluorobenzene-1-sulfonyl)amino]-2-phenyl-1-benzofuran-3-carboxylic acid
0.01 mM, 19% inhibition. 0.1 mM, 70% inhibition
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5-[(4-methyl-3-nitrobenzene-1-sulfonyl)amino]-2-phenyl-1-benzofuran-3-carboxylic acid
0.01 mM,21% inhibition. 0.1 mM, 89% inhibition
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5-[(4-methylbenzene-1-sulfonyl)amino]-2-phenyl-1-benzofuran-3-carboxylic acid
0.01 mM, 23% inhibition. 0.1 mM, 93% inhibition
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5-[(benzenesulfonyl)amino]-2-phenyl-1-benzofuran-3-carboxylic acid
0.01 mM, 11% inhibition. 0.1 mM, 56% inhibition
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5-[[(3,4-dibenzyl-2-oxo-2H-1-benzopyran-7-yl)oxy]methyl]furan-2-carboxylic acid
0.01 mM, 9% inhibition. 0.1 mM, 49% inhibition
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5-[[(4-methyl-6-oxo-7,8,9,10-tetrahydro-6H-dibenzo[b,d]pyran-3-yl)oxy]methyl]furan-2-carboxylic acid
0.01 mM, 18% inhibition. 0.1 mM, 88% inhibition
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6,7-dibenzyl-2-methyl-5-[(4-methylbenzene-1-sulfonyl)amino]-1-benzofuran-3-carboxylic acid
0.01 mM, 12% inhibition. 0.1 mM, 42% inhibition
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6,7-dibenzyl-5-[(4-ethylbenzene-1-sulfonyl)amino]-2-methyl-1-benzofuran-3-carboxylic acid
0.01 mM, 42% inhibition. 0.1 mM, 97% inhibition
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6,7-dibenzyl-5-[(4-fluorobenzene-1-sulfonyl)amino]-2-methyl-1-benzofuran-3-carboxylic acid
0.01 mM, 28% inhibition. 0.1 mM, 95% inhibition
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6,7-dibenzyl-5-[(4-tert-butylbenzene-1-sulfonyl)amino]-2-methyl-1-benzofuran-3-carboxylic acid
0.01 mM, 16% inhibition. 0.1 mM, 59% inhibition
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D-fructose 2,6-diphosphate
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18% inhibition
D-glucose 6-phosphate
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-
diethyldicarbonate
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the addition of 0.5 mM ATP in the preincubation reaction mixture provided complete protection of enzyme activity from inactivation by diethyldicarbonate
GSSG
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inactivation involves formation of a protein-protein disulfide rather than a protein-glutathione complex
L-Leu
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2 mM, 20% inhibition
malonyl-CoA
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0.4 mM, 70% inhibition
methyl 3-chloro-5-(N-(4,6-difluoro-[1,1'-biphenyl]-3-yl)sulfamoyl)-4-hydroxybenzoate
radicicol biotinylated at the C-17 position
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no inhibition with the derivative biotinylated at the C-18 position
(+)-2,2-difluorocitrate
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(+)-2,2-difluorocitrate
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-
(-)-2,2-difluorocitrate
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-
(-)-2,2-difluorocitrate
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(-)-Hydroxycitrate
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potent inhibitor
(-)-Hydroxycitrate
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potent inhibitor
3,5-dichloro-2-hydroxy-N-(4-methoxybiphenyl-3-yl)benzenesulfonamide
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50% inhibition of enzyme at 0.00013 mM, 50% inhibition of total lipid synthesis in HepG-2 cells at 0.008 mM, no cytotoxicity up to 0.05 mM
3,5-dichloro-2-hydroxy-N-(4-methoxybiphenyl-3-yl)benzenesulfonamide
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shows an oral availability of 55%, but a half-life of only 2.1 h. After 20 days of treatment, there is a modest lowering of both plasma cholesterol and triglycerides in high-fat fed mice
ADP
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2 mM, 82% inhibition
ADP
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competitive inhibitor of ATP
bempedoic acid
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bempedoic acid
i.e. ETC-1002 is a first-in-class, prodrug-based direct competitive inhibitor of ATP citrate lyase which regulates lipid metabolism by upregulating hepatic LDL receptor (LDLr) expression and activity. Pharmacological inhibition of ACLY by bempedoic acid, prevents dyslipidemia and attenuates atherosclerosis in hypercholesterolemic ApoE-/- mice, LDLr-/- mice, and LDLr-/- miniature pigs
BMS-303141
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-
dATP
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weak
Glu
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10 mM, inhibition is unlikely to be due to any direct interaction of L-Glu and ATP citrate lyase
Hydroxycitrate
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Hydroxycitrate
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competitive
lauroyl-CoA
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10 mM, 52% inhibition
methyl 3-chloro-5-(N-(4,6-difluoro-[1,1'-biphenyl]-3-yl)sulfamoyl)-4-hydroxybenzoate
i.e. NDI-091143, the structure of the full-length human ACLY homo-tetramer in complex NDI-091143 is determined by cryo-electron microscopy. The compound is located in an allosteric, mostly hydrophobic cavity next to the citrate-binding site, and requires extensive conformational changes in the enzyme that indirectly disrupt citrate binding
methyl 3-chloro-5-(N-(4,6-difluoro-[1,1'-biphenyl]-3-yl)sulfamoyl)-4-hydroxybenzoate
i.e. NDI-091143, allosteric inhibition
myristoyl-CoA
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10 mM, 5% inhibition
oleoyl-CoA
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10 mM, 21% inhibition
oxaloacetate
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-
palmitoyl-CoA
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10 mM, 5% inhibition
radicicol
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noncompetitive inhibitor
radicicol
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noncompetitive inhibitor
radicicol
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noncompetitive
SB-204990
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-
SB-204990
in addition to lowering lipids by inhibiting ACLY, the chemical inhibitor SB-204990 also displays tumor suppressive effects
stearoyl-CoA
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10 mM, 45% inhibition
Tartrate
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