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((1-(2H-tetrazol-5-yl)methyl)-1H-pyrrol-3-yl)(phenyl)-methanone
-
40% inhibition
((3aR,4R,6S,6aR)-6-((Z)-(((4-hydroperoxybenzyl)oxy)imino)methyl)-4-hydroxy-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-yl)methyl 3-chlorobenzoate
83% inhibition at 0.1 mM, oxyimino derivative, obtained by reaction of a 1,5-dicarbonyl substrate with O-(arylmethyl)hydroxylamine. Inhibitor reduces both cell death and the apoptotic process when tested in an in vitro model of diabetic retinopathy
(1,1-dihydroxy-3-oxo-1,3-dihydro-2H-1,2-benzisothiazol-2-yl)acetic acid
i.e. BiT, 1,1-dioxide-benzo[d]isothiazol-3-one alkanoic acid derivatives
(1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
IC50: 0.010 mM
(1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester
-
(1,3,3-trioxo-2,3-dihydronaphtho[2,3-d]isothiazol-2-yl)acetic acid ethyl ester
-
(1-(2-(2H-tetrazol-5-yl)ethyl)-1H-pyrrol-3-yl)(phenyl)-methanone
-
6% inhibition
(1-(2H-tetrazole-5-yl)-1H-pyrrol-2-yl)(phenyl)-methanone
-
-
(1-(2H-tetrazole-5-yl)-1H-pyrrol-3-yl)(phenyl)-methanone
-
-
(1-(3-(2H-tetrazol-5-yl)propyl)-1H-pyrrol-3-yl)(phenyl)-methanone
-
41% inhibition
(10-benzyl-3,4-dioxo-3,4-dihydro[1,2,4]triazino[4,3-a]benzimidazol-2(10H)-yl)acetic acid
-
(1H-indol-1-yl)acetic acid
-
(2,3-dihydrocyclopenta[b]indol-4(1H)-yl)acetic acid
-
(2,4-dioxo-5-[(6,8-dimethyl-4-oxo-4H-chromen-3-yl)methylene]-1,3-thiazolidine-3-yl) acetic acid
-
-
(2,4-dioxo-5-[(6-isopropyl-4-oxo-4H-chromen-3-yl)methylene]-1,3-thiazolidine-3-yl) acetic acid
-
-
(2,4-dioxo-5-[(6-methyl-4-oxo-4H-chromen-3-yl)methylene]-1,3-thiazolidine-3-yl)acetic acid
-
-
(2,4-dioxo-5-[(6-nitro-4-oxo-4H-chromen-3-yl)methylene]-1,3-thiazolidine-3-yl)acetic acid
-
-
(2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-8-yl)-acetic acid
-
an aldose reductase inhibitor and antioxidant of zwitterionic nature
(2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid
-
uncompetitive with both D,L-glyceraldehyde and NADPH
(2-carbamoyl-5-fluorophenoxy)acetic acid
the carboxamide nitrogen can undergo a further H-bond to the additionally recruited water molecule W2 that in turn mediates H-bonded contacts involving the additional water molecule W3 to the amide bonds next to Leu300. Using water molecules W2 and W3 as mediating partners, the compound forms additional polar contacts to the protein
(2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid
7fold selectivity for ALR2 over ALR1
(2-oxo-8-phenyl-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid
-
(2-oxo-8-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid
24fold selectivity for ALR2 over ALR1
(2-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid
-
uncompetitive with both D,L-glyceraldehyde and NADPH
(2-[(4-bromo-2-fluorobenzyl)carbamoyl]-5-chlorophenoxy)acetic acid
thermodynamic binding data for isoform ALR2 and mutants
(2-[[2-(hydroxymethyl)phenyl]methyl]-3-oxo-2,3-dihydro-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
-
410fold selectivity for ALR2 over ALR1
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
(2R)-1-[(benzyloxy)carbonyl]-2,3-dihydro-1H-indole-2-carboxylic acid
CC-13401
(2R)-2,3-dihydroxypropanamide
-
(2R)-2-hydroxypropanamide
-
(2R,3S,4R,5R)-2,3,4,5,6-pentahydroxyhexanamide
-
(2R,3S,4S)-2,3,4,5-tetrahydroxypentanamide
-
(2R,4S)-6-fluoro-2',5'-dioxospiro-[chroman-4,4'-imidazoline]-2-carboxamide
-
IC50: 570 nM, mechanism, active site binding modeling, the stereochemistry of the exocyclic amide group influences the affinity for the enzyme
(2S)-2'-methoxykurarinone
-
potent inhibitor of rat lens aldose reductase
(2S)-2,3-dihydroxypropanamide
-
(2S)-3beta,7,4'-trihydroxy-5-methoxy-8-(gamma,gamma-dimethylallyl)-flavanone
(2S)-7,4'-dihydroxy-5-methoxy-8-(gamma,gamma-dimethylallyl)-flavanone
-
potent inhibitor of recombinant human aldose reductase
(2S,3R,4R)-2,3,4,5-tetrahydroxypentanamide
-
(2S,3S)-2,3,4-trihydroxybutanamide
-
(2Z)-3-(3,4-dihydroxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
-
(2Z)-3-(3-methoxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
-
(3,3-dihydroxy-1-oxo-1,3-dihydro-2H-3lambda4-naphtho[1,2-d]isothiazol-2-yl)acetic acid
i.e. NiT
(3-benzothiazol-2-yl-pyrrol-1-yl)acetic acid
-
50% inhibition at 49 nM
(3-benzyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
(3-methyl-1-oxo-5-phenylpyrimido[4,5-c]quinolin-2(1H)-yl)acetic acid
14fold selectivity for isoform AKR1B1 over AKR1B10
(3-sulfanyl-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
-
(3-sulfanyl[1,2,5]triazepino[4,3-b]indol-6(3H)-yl)acetic acid
-
(3-[(5-chloro-1,3-benzothiazol-2-yl)methyl]-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)acetic acid
thermodynamic binding data for isoform ALR2 and mutants
(3-[[(2-fluorophenyl)methyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
-
(3-[[2-oxo-2-(2,4,6-trimethylanilino)ethyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
-
(4-benzothiazol-2-yl-2-benzoylpyrrol-1-yl)acetic acid
-
50% inhibition at 45 nM
(4-benzyl-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)acetic acid
-
(4-hydroxy-3-methoxyphenyl)acetonitrile
-
IC50: 0.0244 mM
(4-hydroxy-3-methoxyphenyl)methamine
-
IC50: 0.0634 mM
(4-hydroxyphenyl)(6-hydroxypyrazin-2-yl)methanone
-
isolated from red ascidian Botryllus leachi, pyrazine derivative, IC50: 0.0414 mM
(4-hydroxyphenyl)[4-(4-hydroxyphenyl)-1H-imidazol-2-yl]methanone
-
isolated from red ascidian Botryllus leachi, imidazole derivative, IC50: 0.0214 mM
(4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indol-5-yl)acetic acid
-
(4S)-6-fluoro-2,3-dihydro-2'H,5'H-spiro[1-benzopyran-4,4'-imidazolidine]-2',5'-dione
-
(5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid
-
IC50: 0.0017 mM
(5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid methyl ester
-
15% inhibition of ALR2 at 0.05 mM
(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-acetic acid
-
IC50: 0.00026 mM
(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-acetic acid methyl ester
-
35% inhibition of ALR2 at 0.05 mM
(5-chloro-2-[(3-nitrobenzyl)carbamoyl]phenoxy)acetic acid
thermodynamic binding data for isoform ALR2 and mutants
(5-chloro-2-[(4-cyanobenzyl)carbamoyl]phenoxy)acetic acid
-
-
(5-methylIndoleDs)1-(3-(3,4,5-trimethoxyphenyl)-3-(5-methyl-1H-indol-3-yl)propanoyl)-4-(5-methyl-1H-indol-3-yl)piperidin-2-one
-
-
(5-methylIndoleMs)1-(3-(3,4,5-trimethoxyphenyl)-3-(5-methyl-1H-indol-3-yl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
-
(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetic acid
-
IC50: 0.00017 mM
(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetic acid methyl ester
-
12% inhibition of ALR2 at 0.05 mM
(5E)-5-[4-(4-oxo-4H-chromen-2-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
-
(5Z)-3-chloro-4-(3,5-dibromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.019 mM
(5Z)-3-chloro-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-4-(4-hydroxyphenyl)furan-2(5H)-one
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.0008 mM
(5Z)-4-(3,5-dibromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.020 mM
(5Z)-4-(3-bromo-4-hydroxyphenyl)-3-chloro-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.013 mM
(5Z)-4-(3-bromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.048 mM
(5Z)-4-(3-bromo-4-hydroxyphenyl)-5-[(3-bromo-4-hydroxyphenyl)methylidene]-3-chlorofuran-2(5H)-one
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.017 mM
(5Z)-5-(3-aminobenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.69
(5Z)-5-(3-fluorobenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 5.04
(5Z)-5-(3-hydroxybenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.97
(5Z)-5-(3-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.88
(5Z)-5-(3-methylbenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 5.03
(5Z)-5-(3-phenoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 5.21
(5Z)-5-(3-{(E)-[(4-hydroxyphenyl)imino]methyl}benzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 5.73
(5Z)-5-(4-fluorobenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 5.09
(5Z)-5-(4-hydroxy-3-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.93
(5Z)-5-(4-hydroxybenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 5.05
(5Z)-5-(4-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.39
(5Z)-5-(4-{(E)-[(4-hydroxyphenyl)imino]methyl}benzylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.64
(5Z)-5-(naphthalen-1-ylmethylidene)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.97
(5Z)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-4-(4-hydroxyphenyl)furan-2(5H)-one
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.057 mM
(5Z)-5-[(3-bromo-4-hydroxyphenyl)methylidene]-3-chloro-4-(4-hydroxyphenyl)furan-2(5H)-one
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.046 mM
(5Z)-5-[(4-oxo-2-phenyl-4H-chromen-6-yl)methylidene]-1,3-thiazolidine-2,4-dione
-
-
(5Z)-5-[3-(trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.89
(5Z)-5-[4-(trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.50
(6-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
IC50: 0.10 mM
(6-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester
-
(6-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
IC50: 0.180 mM
(6-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester
-
(6H-indolo[2,3-b]quinoxalin-6-yl)acetic acid
-
(7H-indolo[2',3':5,6][1,2,4]triazino[2,3-a]benzimidazol-7-yl)acetic acid
uncompetitive
(8-methyl-3-[[2-oxo-2-(propylamino)ethyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
-
(9-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
IC50: 0.10 mM
(9-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester
-
(9-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
IC50: 0.190 mM
(9-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid ethyl ester
-
(E)-1-(3-(1,3-diphenyl-1H-pyrazol-4-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(2,5-dimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)piperidin-2-one
-
-
(E)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)pyrrolidin-2-one
-
-
(E)-1-(3-(3-(trifluoromethyl)phenyl)acryloyl)-5,6-dihydropyridin-2(1)-one
-
-
(E)-1-(3-(3-methyl-1-phenyl-1H-pyrazol-4-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(3-phenoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(4-bromophenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(4-chlorophenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(benzo[d][1,3]dioxol-5-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(furan-2-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(naphthalen-2-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(pyridin-2-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-(thiophen-2-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(3-mesitylacryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-1-(4-benzylpiperazin-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(E)-1-(4-methylpiperazin-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(E)-1-(4-phenylpiperazin-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(E)-1-(piperidin-1-yl)-3-(3,4,5-trimethoxyphenyl) prop-2-en-1-one
-
-
(E)-1-(pyrrolidin-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
-
(E)-2-(3-(3,4,5-trimethoxyphenyl)acryloyl)benzo[d]isothiazol-3(2H)-one
-
-
(E)-2-(3-(3,4,5-trimethoxyphenyl)acryloyl)isoindolin-1-one
-
-
(E)-3-((4-chlorophenyl)(hydroxy)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-3-((4-fluorophenyl)(hydroxy)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-3-(3-(3,4,5-trimethoxyphenyl)acryloyl)benzo[d]oxazol-2(3H)-one
-
-
(E)-3-(5-(3-nitrophenyl)furan-2-yl)acrylic acid
-
(E)-3-(hydroxy(2-nitrophenyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-3-(hydroxy(4-nitrophenyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-3-(hydroxy(naphthalen-2-yl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-3-(hydroxy(p-tolyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-3-(hydroxy(phenyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-3-(hydroxy(pyridin-2-yl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-3-(hydroxy(thiophen-2-yl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
-
(E)-4-(hydroxy(2-oxo-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-1,2,5,6-tetrahydropyridin-3-yl)methyl)benzonitrile
-
-
(E)-methyl 3-(3,4,5-trimethoxyphenyl)acrylate
-
-
(E)-N-ethanethioyl-3-(3,4,5-trimethoxyphenyl)acrylamide
-
-
(E,E)-5[2-methyl-3-phenyl-2-propenylidene-4-oxo-2-thioxo-3-thiazolidine]acetic acid
(S)-6-fluorospiro[chroman-4,5'-imidazolidine]-2',4'-dione
(Z)-2-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-N-hydroxyacetamide
-
(Z)-2-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide
18% inhibition at 0.0125 mM
(Z)-2-(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide
32% inhibition at 0.0125 mM
(Z)-2-(5-naphthalen-2-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide
3% inhibition at 0.0125 mM
(Z)-2-[2,4-dioxo-5-(3-phenoxybenzylidene)thiazolidin-3-yl]acetamide
8% inhibition at 0.0125 mM
(Z)-2-[5-(3-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
16% inhibition at 0.0125 mM
(Z)-2-[5-(3-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
10% inhibition at 0.0125 mM
(Z)-2-[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]-N-hydroxyacetamide
-
(Z)-2-[5-(4-hydroxy-3-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
-
(Z)-2-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
31% inhibition at 0.0125 mM
(Z)-5-(naphthalen-1-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
52% inhibition at 0.025 mM
(Z)-5-(naphthalen-2-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
59% inhibition at 0.025 mM
(Z)-5-[(3-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(3-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(3-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
64% inhibition at 0.025 mM
(Z)-5-[(4-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(4-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(4-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(4-phenylphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
45% inhibition at 0.025 mM
(Z)-N-hydroxy-2-(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide
-
(Z)-N-hydroxy-2-(5-naphthalen-2-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide
39% inhibition at 0.025 mM
(Z)-N-hydroxy-2-[2,4-dioxo-5-(3-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
-
(Z)-N-hydroxy-2-[2,4-dioxo-5-(4-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
-
(Z)-N-hydroxy-2-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
-
([2-[(4-methoxy-1-methyl-1H-indazol-3-yl)amino]-2-oxoethyl]sulfanyl)acetic acid
HTS-03834
([5-(5-nitrofuran-2-yl)-1,3,4-oxadiazol-2-yl]sulfanyl)acetic acid
crystallization data
1'-(4-bromophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(4-chlorophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(4-fluorobenzene-1-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
no selectivity for ALR2 over ALR1
1'-(4-methoxyphenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(4-methylphenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(4-nitrophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(5-chlorothiophene-2-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
3.4fold selectivity for ALR2 over ALR1
1'-(9,10-dioxo-9,10-dihydroanthracen-2-ylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(naphthalen-2-ylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1,1-dioxidenaphtho[2,3-d]isothiazole-3(2H)-one
-
1,2,7-trihydroxy-3,8-dimethoxy-6-methylanthracene-9,10-dione 2-O-beta-D-glucoside
-
-
1,2-benzothiazin-1,1-dioxide
-
1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
-
1,3,7-trihydroxy-2,8-dimethoxy-6-methylanthracene-9,10-dione
-
-
1,3,8-trihydroxy-6-methylanthracene-9,10-dione
-
-
1,5-bis(3,4-dihydroxyphenyl)-1,4-pentadiene-3-one
-
IC50: 0.0034 mM
1,5-bis(3,5-di-tert-butyl-4-hydroxyphenyl)-1,4-pentadiene-3-one
-
31.0% inhibition at 0.1 mM
1,5-bis(4-hydroxy-3,5-dimethoxyphenyl)-1,4-pentadiene-3-one
-
IC50: 0.0253 mM
1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one
-
IC50: 0.0359 mM
1,5-bis(4-hydroxyphenyl)-1,4-pentadiene-3-one
-
IC50: 0.0331 mM
1-((2E,4E)-5-(benzo[d][1,3]dioxol-5-yl)penta-2,4-dienoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-((2E,4E,6E)-7-(3,4,5-trimethoxyphenyl)hepta-2,4,6-trienoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(2-chlorobenzoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(2-iodobenzoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(3-(1-benzyl-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(1-benzyl-1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(1-benzyl-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(3-(1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(3-(3,4,5-trimethoxyphenyl)-3-(1-methyl-1H-indol-3-yl)propanoyl)-4-(1-methyl-1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(3,4,5-trimethoxyphenyl)-3-(1-methyl-1H-indol-3-yl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(3-(3,4,5-trimethoxyphenyl)-3-(2-methyl-1H-indol-3-yl)propanoyl)-4-(2-methyl-1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(3,4,5-trimethoxyphenyl)-3-(2-phenyl-1H-indol-3-yl)propanoyl)-4-(2-phenyl-1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(3,4,5-trimethoxyphenyl)-3-(5-methoxy-1H-indol-3-yl)propanoyl)-4-(5-methoxy-1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(3,4,5-trimethoxyphenyl)-3-(5-nitro-1H-indol-3-yl)propanoyl)-4-(5-nitro-1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(3,4,5-trimethoxyphenyl)-3-(5-nitro-1H-indol-3-yl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(3-(5-bromo-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(5-bromo-1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(5-bromo-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(3-(5-fluoro-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(5-fluoro-1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(5-fluoro-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(3-(5-iodo-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(5-iodo-1H-indol-3-yl)piperidin-2-one
-
-
1-(3-(5-iodo-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(3-(5-methoxy-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(4-fluorobenzoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(4-fluorophenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
2.1fold selectivity for ALR2 over ALR1
1-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
8.5fold selectivity for ALR2 over ALR1
1-(4-methylphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
1.5fold selectivity for ALR2 over ALR1
1-(4-nitrobenzoyl)-5,6-dihydropyridin-2(1H)-one
-
-
1-(4-nitrobenzyl)-3-(4-(2-morpholinoethyl)piperazin-1-yl)quinoxalin-2(1H)-one
-
1-(4-nitrobenzyl)-3-(4-(4-methoxyphenyl)piperazin-1-yl)quinoxalin-2(1H)-one
-
1-(4-nitrobenzyl)-3-(4-(pyrazin-2-yl)piperazin-1-yl)quinoxalin-2(1H)-one}
-
1-(4-nitrobenzyl)-3-styryl-quinoxalin-2(1H)-one
-
1-(5-chlorothiophen-2-yl)-1,3-diazaspiro[4.5]decane-2,4-dione
1.9fold selectivity for ALR2 over ALR1
1-butyl-2-[[(4-oxo-3,4-dihydroquinazolin-2-yl)methyl]sulfanyl]-1H-benzimidazole-5-sulfonamide
classical competitive mechanism. No significant influence on 11beta-HSD activities
1-cinnamoyl-5,6-dihydropyridin-2(1H)-one
-
-
1-O-Galloyl-beta-D-glucose
1-[3-(2-phenyl-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl]-5,6-dihydropyridin-2(1H)-one
-
-
1-[4-benzoyl-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]-2,2,2-trifluoroethan-1-one
-
413fold selectivity for isoform ALR2 over ALR1
2,1,3-benzoxadiazol-5-yl 5-chlorothiophene-2-sulfonate
KM-07100
2,2'-[sulfonylbis(benzene-4,1-diyliminomethylylidene)]dipropanedinitrile
BTB-06667
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(3-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one
-
370fold selectivity for isoform ALR2 over ALR1
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one
-
468fold selectivity for isoform ALR2 over ALR1
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-phenoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one
-
190fold selectivity for isoform ALR2 over ALR1
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methanesulfonyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one
-
775fold selectivity for isoform ALR2 over ALR1
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one
2,2,2-trifluoro-1-[4-(3-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one
-
339fold selectivity for isoform ALR2 over ALR1
2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one
2,3-dihydrospiro[4H-thiopyrano[2,3-b]pyridin-4,4'imidazolidine]-2',5'-dione
-
50% inhibition at 0.0034 mM
2,3-dihydrospiro[4H-thiopyrano[2,3-b]pyridin-4,4'imidazolidine]-2',5'-dione, sulfone derivative
-
50% inhibition at 0.0014 mM
2,5-bis(3,4-dihydroxybenzylidene)cyclopentanone
-
IC50: 0.0026 mM
2,5-bis(3,5-di-tert-butyl-4-hydroxybenzylidene)cyclopentanone
-
38.2% inhibition at 0.1 mM
2,5-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)cyclopentanone
-
IC50: 0.0208 mM
2,5-bis(4-hydroxy-3,5-dimethoxybenzylidene)cyclopentanone
-
IC50: 0.0234 mM
2,5-bis(4-hydroxy-3-methoxybenzylidene)cyclopentanone
-
IC50: 0.0258 mM
2,5-bis(4-hydroxybenzylidene)cyclopentanone
-
IC50: 0.0274 mM
2,5-dihydro-3H-[1,2,4]triazino[5,6-b]indole-3-thione
-
2,5-dihydrobenzoic acid
-
-
2,6-bis(3,4-dihydroxybenzylidene)cyclohexanone
-
IC50: 0.0029 mM
2,6-bis(3,5-di-tert-butyl-4-hydroxybenzylidene)cyclohexanone
-
35.8% inhibition at 0.1 mM
2,6-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)cyclohexanone
-
IC50: 0.021 mM
2,6-bis(4-hydroxy-3,5-dimethoxybenzylidene)cyclohexanone
-
IC50: 0.0249 mM
2,6-bis(4-hydroxy-3-methoxybenzylidene)cyclohexanone
-
IC50: 0.0264 mM
2,6-bis(4-hydroxybenzylidene)cyclohexanone
-
IC50: 0.0275 mM
2,6-dichlorophenylacetic acid
-
competitive
2-(2-oxo-3-((3,4,5-trifluorophenyl)amino)quinoxalin-1(2H)-yl)acetic acid
-
-
2-(2-oxo-3-phenethylquinoxalin-1(2H)-yl)acetic acid
22% inhibition
2-(2-oxo-3-styrylquinoxalin-1(2H)-yl)acetic acid
32% inhibition
2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-1-benzopyran-4-one
-
2-(3,4-dihydroxyphenyl)-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(3,4-dihydroxyphenyl)-6-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(3,4-dihydroxyphenyl)-9-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(3,4-dimethoxyphenyl)-6-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(3,4-dimethoxyphenyl)-ethanoic acid
-
IC50: 0.0303 mM
2-(3,7-bis(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(3-((2,4-difluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-((4-bromo-2-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
-
2-(3-((4-bromophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-((4-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid}
41% inhibition
2-(3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(3-(3-(tert-butylamino)-3-oxoprop-1-en-1-yl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
25% inhibition
2-(3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(3-(4-(4-methoxyphenyl) piperazin-1-yl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
48% inhibition
2-(3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromo-2-fluorophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromo-2-fluorophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromo-2-fluorophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromo-2-fluorophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
40% inhibition
2-(3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
47% inhibition
2-(3-(4-fluorostyryl)-6-nitro-2-oxoquinoxalin-1(2H)-yl)acetic acid}
25% inhibition
2-(3-(4-hydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(3-benzoyl-1H-pyrrol-1-yl)acetic acid
-
-
2-(3-phenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(3-phenyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(3-thiophenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(4-((E)-4-oxo-5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((E)-4-oxo-5-((1-phenyl-3-m-tolyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((E)-4-oxo-5-((1-phenyl-3-p-tolyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((E)-5-((3-(3-bromophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((E)-5-((3-(3-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((E)-5-((3-(3-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((E)-5-((3-(3-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido)acetic acid
-
-
2-(4-((E)-5-((3-(3-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((E)-5-((3-(4-bromophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido) acetic acid
-
-
2-(4-((E)-5-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((E)-5-((3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((E)-5-((3-(4-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido)acetic acid
-
-
2-(4-((E)-5-((3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(2,3-dichlorobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido) acetic acid
-
-
2-(4-((Z)-5-(2-bromobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(2-chlorobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)aceticacid
-
-
2-(4-((Z)-5-(2-fluorobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(2-methoxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(2-methylbenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(2-nitrobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(3,4,5-trimethoxybenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido) acetic acid
-
-
2-(4-((Z)-5-(3-bromobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(3-chlorobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(3-fluorobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(3-methoxybenzylidene)-4-oxo-2-thioxothiazolidin-3yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(3-methylbenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(3-nitrobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(4-bromobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(4-chlorobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(4-fluorobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(4-formylbenzylidene) 4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(4-methoxybenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(4-methylbenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-(4-nitrobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-((Z)-5-benzylidene-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
-
2-(4-(4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
-
i.e. rhodanine-3-hippuric acid
2-(4-hydroxy-3-methoxyphenyl)-7-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(4-hydroxy-3-methoxyphenyl)ethanoic acid
-
derived from ginger rhizom, Zingiber officinale, IC50: 0.0185 mM, suppresses nt only sorbitol accumulation in human erythrocytes
2-(4-hydroxy-3-methoxyphenyl)ethanol
-
derived from ginger rhizom, Zingiber officinale, IC50: 0.0192 mM, suppresses sorbitol accumulation in human erythrocytes
2-(6-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(6-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(6-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(6-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(6-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(6-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(6-chloro-3-(4-fluoro-styryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
25% inhibition
2-(6-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(6-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(6-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(6-nitro-1,1,3-trioxo-1,3-dihydro-2H-1lambda~6~,2-benzothiazol-2-yl)propanoic acid
-
2-(7-(4-fluorobenzyl)-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(7-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-bromo-3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(7-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(7-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(7-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-bromo-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(7-chloro-2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid}
35% inhibition
2-(7-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-chloro-3-(2-benzothiophene)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-chloro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-chloro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(7-chloro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(7-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-fluoro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-fluoro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
2-(7-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(7-fluoro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
2-(carboxymethyl)-1-oxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid 3,3-dioxide
crystallization data
2-amino-4-oxo-3,4-dihydropteridine-6-carboxylic acid
-
2-amino-4-oxo-3,4-dihydropteridine-7-carboxylic acid
-
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
IC50: 0.068 mM; IC50: 0.10 mM
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid methyl ester
-
2-benzyl-1,3,3-trioxo-2,3-dihydro-1H-3lambda~6~-naphtho[1,2-d][1,2]thiazole-4-carboxylic acid
-
2-bromophenylacetic acid
-
competitive
2-carboxymethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
IC50: 140 nM, binding structure analysis
2-carboxymethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid carboxymethyl ester
IC50: 550 nM, binding structure analysis
2-Chlorophenylacetic acid
-
competitive
2-ethoxycarbonyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid ethoxycarbonylmethyl ester
-
2-hydroxyphenylacetic acid
-
competitive
2-isopropoxycarbonylmethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid isopropyl ester
-
2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
IC50: 0.088 mM
2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid ethoxycarbonyl methylester
-
2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid methyl ester
-
2-naphthylacetic acid
-
competitive
2-oxo-3-(3,4,5-trihydroxyphenoxy)-1,8-naphthyridine-1(2H)-carboxylic acid
21.7fold selectivity for AKR1B1 over AKR1A1
2-oxo-3-(3,4,5-trimethoxyphenoxy)-1,8-naphthyridine-1(2H)-carboxylic acid
20.8fold selectivity for AKR1B1 over AKR1A1
2-oxo-3-phenoxy-1,8-naphthyridine-1(2H)-carboxylic acid
27fold selectivity for AKR1B1 over AKR1A1
2-phenyl-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-tert-butylsulfonylnaphthalene-1,3-dicarboxylic acid
-
2-tert-butylsulfonylnaphthalene-1-carboxylic acid
-
2-[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino]-4-phenylbutanoic acid
-
2-[(3,4-dihydroxyphenyl)methyl]-6-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-[(4-fluorobenzyl)[(2-fluorophenyl)sulfonyl]amino]-N-[2-(3-fluorophenyl)ethyl]acetamide
-
2-[2-(carboxymethoxy)-2-oxoethyl]-1-oxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid 3,3-dioxide
crystallization data
2-[5-fluoro-2-methyl-1-p-(methylsulphinyl)benzylidine]indene-3-acetic acid
-
non-competitive
2-[[5-(carboxymethyl)-3-oxo-3,5-dihydro-2H-[1,2,4]triazino[5,6-b]indol-2-yl]methyl]benzoic acid
-
424fold selectivity for ALR2 over ALR1
3',3'',5',5''-tetrabromophenolphthalein
-
less than 25% inhibition at 0.1 mM
3'-(4-bromophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(4-chlorophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(4-fluorobenzene-1-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
10fold selectivity for ALR2 over ALR1
3'-(4-methoxyphenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(4-methylphenylsulfonyl)spiro[fluorene-9,50-imidazolidine]-2',4'-dione
-
3'-(4-nitrophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(5-chlorothiophene-2-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
1.1fold selectivity for ALR2 over ALR1
3'-(9,10-dioxo-9,10-dihydroanthracen-2-ylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(naphthalen-2-ylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3,3-dioxidenaphtho[1,2-d]isothiazole-1(2H)-one
-
3,3-Tetramethylene glutaric acid
-
-
3,3-Tetramethyleneglutaric acid
-
-
3,4-dihydroxyphenylacetic acid
able to prevent the formation of the tubulin/aldose reductase complex and the activation of aldose reductase by tubulin
3,4-dinitro-2,5-bis(phenylsulfanyl)thiophene
SEW-05367
3,5-bis(3,4-dihydroxybenzylidene)-4-piperidone
-
IC50: 0.0049 mM
3,5-bis(3,5-di-tert-butyl-4-hydroxybenzylidene)-4-piperidone
-
29.2% inhibition at 0.1 mM
3,5-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)-4-piperidone
-
IC50: 0.0208 mM
3,5-bis(4-hydroxy-3,5-dimethoxybenzylidene)-4-piperidone
-
IC50: 0.0223 mM
3,5-bis(4-hydroxy-3-methoxybenzylidene)-4-piperidone
-
IC50: 0.0299 mM
3,5-bis(4-hydroxyphenyl)-4-piperidone
-
IC50: 0.0311 mM
3,5-dichlorosalicylic acid
uncompetitive inhibition
3,6,7-trichloroquinoxalin-2(1H)-one
-
-
3,6-dichloroquinoxalin-2(1H)-one
-
-
3,7-dichloroquinoxalin-2(1H)-one
-
-
3-(1H-indol-1-yl)propanoic acid
-
3-(2,4-dihydroxyphenyl)-5-hydroxy-7-methoxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
3-(2-phenylthiazole-4-yl)propanoic acid
-
3-(3,4,5-trimethoxyphenyl)-3-(2-methyl-1H-indol-3-yl)propanoic acid
-
-
3-(3,4-dihydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
16.9fold selectivity for AKR1B1 over AKR1A1
3-(3,4-dimethoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
17.6fold selectivity for AKR1B1 over AKR1A1
3-(3,5-dihydroxy-4-methoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
25.8fold selectivity for AKR1B1 over AKR1A1
3-(3,5-dihydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
20.8fold selectivity for AKR1B1 over AKR1A1
3-(3,5-dimethoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
21.5fold selectivity for AKR1B1 over AKR1A1
3-(3-benzoyl-1H-pyrrol-1-yl)propanoic acid
-
-
3-(3-hydroxy-4,5-dimethoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
31.6fold selectivity for AKR1B1 over AKR1A1
3-(3-hydroxy-4-methoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
19.3fold selectivity for AKR1B1 over AKR1A1
3-(3-hydroxy-5-methoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
15.1fold selectivity for AKR1B1 over AKR1A1
3-(4-fluorophenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
2.3fold selectivity for ALR2 over ALR1
3-(4-fluorostyryl)-1-(4-nitrobenzyl)quinoxalin-2(1H)-one
-
3-(4-hydroxy-3-methoxyphenyl)propanol
-
IC50: 0.283 mM
3-(4-hydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
15.9fold selectivity for AKR1B1 over AKR1A1
3-(4-methoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
20fold selectivity for AKR1B1 over AKR1A1
3-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
1.2fold selectivity for ALR2 over ALR1
3-(4-methylphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
11fold selectivity for ALR2 over ALR1
3-(4-nitro-1,1,3-trioxo-1,3-dihydro-2H-1lambda~6~,2-benzothiazol-2-yl)propanoic acid
-
3-(4-nitrophenyl)-2-[(phenylsulfonyl)amino]propanoic acid
SPB-08302
3-(5-(3-(trifluormethyl)phenyl)thiophene-2-yl)propanoic acid
-
3-(5-(3-acetylphenyl)furan-2-yl)propanoic acid
-
3-(5-(3-aminophenyl)furan-2-yl)propanoic acid
-
3-(5-(3-methoxyphenyl)furan-2-yl)propanoic acid
-
3-(5-(3-methoxyphenyl)thiophene-2-yl)propanoic acid
-
3-(5-(3-methylphenyl)furan-2-yl)propanoic acid
-
3-(5-(3-methylphenyl)thiophene-2-yl)propanoic acid
-
3-(5-(3-methylsulfonyl)phenylfuran-2-yl)propanoic acid
-
3-(5-(3-nitrophenyl)furan-2-yl)propanoic acid
-
3-(5-(3-nitrophenyl)thiophene-2-yl)propanoic acid
-
3-(5-(3-trifluormethyl)phenylfuran-2-yl)propanoic acid
-
3-(5-chlorothiophen-2-yl)-1,3-diazaspiro[4.5]decane-2,4-dione
127fold selectivity for ALR2 over ALR1, 79% reduction in blood glucose level
3-(5-phenylfuran-2-yl)propanoic acid
-
3-(5-phenylthiophene-2-yl)propanoic acid
-
3-(5-pyridine-2-yl-furan-2-yl)propanoic acid
-
3-(5-pyridine-3-yl-furan-2-yl)propanoic acid
-
3-(6-acetamido-1,1,3-trioxo-1,3-dihydro-2H-1lambda~6~,2-benzothiazol-2-yl)propanoic acid
-
3-(benzo[b] thiophen-3-yl)-1-(4-nitrobenzylquinoxalin-2(1H)-one
-
3-benzyl-1-methyl-2-oxo-1,2-dihydroquinolin-4-yl 4-methylbenzenesulfonate
NRB-05245
3-chloro-6-fluoroquinoxalin-2(1H)-one
-
-
3-chloro-6-methylquinoxalin-2(1H)-one
-
-
3-chloro-6-nitroquinoxalin-2(1H)-one
-
-
3-chloro-7-fluoroquinoxalin-2(1H)-one
-
-
3-chloro-7-methoxyquinoxalin-2(1H)-one
-
-
3-chloro-7-methylquinoxalin-2(1H)-one
-
-
3-chloroquinoxalin-2(1H)-one
-
-
3-hydroxy-4-methoxymandelic acid
able to prevent the formation of the tubulin/aldose reductase complex and the activation of aldose reductase by tubulin
3-hydroxybutyric acid
-
-
3-morpholino syndnonimine
-
1 mM, 76% inhibition, reversed by incubation with fresh media
3-nitro-L-tyrosine
able to prevent the formation of the tubulin/aldose reductase complex and the activation of aldose reductase by tubulin
3-O-caffeoylquinic acid
-
-
3-tert-butylsulfonylnaphthalene-2-carboxylic acid
-
3-[(4-bromo-2-fluorophenyl)methyl]-3,4-dihydro-4-oxo-1-phthalazineacetic acid
-
recombinant from baculovirus system in Spodoptera frugiperda cells
3-[2-(carboxymethoxy)-4-fluorobenzamido]benzoic acid
the ligand directs its acid group toward the surrounding solvent and accommodates the hydrophobic cleft adjacent to the sealed specificity pocket
3-[3,4-dihydroxy-5-(3-methylbut-2-en-1-yl)phenyl]-5,7-dihydroxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
3-[3-[(diethylamino)methyl]-1H-indol-1-yl]propanoic acid
-
3-[6-(3-methylbutanamido)-1,1,3-trioxo-1,3-dihydro-2H-1lambda~6~,2-benzothiazol-2-yl]propanoic acid
-
4-(3-benzoyl-1H-pyrrol-1-yl)butanoic acid
-
-
4-(4-hydroxy-3-methoxyphenyl)-2-butanone
-
IC50: 0.197 mM
4-(4-hydroxy-3-methoxyphenyl)butanol
-
IC50: 0.642 mM
4-(5-(3-methylphenyl)thiophene-2-yl)butanoic acid
-
4-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-2-butenoic acid
-
21% inhibition of ALR2 at 0.05 mM
4-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-2-butenoic acid methyl ester
-
6% inhibition of ALR2 at 0.05 mM
4-(5-phenylthiophene-2-yl)butanoic acid
-
4-amino-N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamide
-
-
4-androsten-17alpha-ol-3-one
i.e. epitestosterone
4-androsten-17beta-ol-3-one
i.e. testosterone
4-androstene-3,17-dione
-
4-hydroxy-3-methoxymandelic acid
able to prevent the formation of the tubulin/aldose reductase complex and the activation of aldose reductase by tubulin
4-hydroxy-3-methoxyphenol
-
IC50: 0.273 mM
4-hydroxy-3-methoxyphenyl methanol
-
IC50: 0.0244 mM
4-hydroxy-3-methoxyphenylacetic acid
able to prevent the formation of the tubulin/aldose reductase complex and the activation of aldose reductase by tubulin
4-hydroxy-3-methoxyphenyllactic acid
able to prevent the formation of the tubulin/aldose reductase complex and the activation of aldose reductase by tubulin
4-hydroxy-trans-2-nonenal
4-hydroxybenzoic acid
-
-
4-O-butylpaeoniflorin
-
-
4-oxo-4-(5-(3-methylphenyl)thiophene-2-yl)butanoic acid
-
4-oxo-4-(5-phenylthiophen-2-yl)butanoic acid
-
4-pregenene-21-ol-3,20-dione
i.e. 11-deoxycorticosterone
4-pregnene-11beta,17alpha,21-triol-3,20-dione
i.e. cortisol
4-pregnene-11beta,21-diol-3,20-dione
i.e. corticosterone
4-pregnene-17alpha,21-diol-3,11,20-trione
i.e. cortisone
4-pregnene-18-al-11beta,21-diol-3,20-dione
i.e. aldosteron
4-[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino]butanoic acid
-
4-[(3-nitrophenyl)methyl]-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidine-6-carboxylic acid
-
4-[2,4-dioxo-5-(3-phenoxybenzylidene)thiazolidin-3-yl]-2-butenoic acid
-
19% inhibition of ALR2 at 0.05 mM
4-[2,4-dioxo-5-(3-phenoxybenzylidene)thiazolidin-3-yl]-2-butenoic acid methyl ester
-
25% inhibition of ALR2 at 0.05 mM
4-[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]-2-butenoic acid
-
57% inhibition of ALR2 at 0.05 mM
4-[3-(3-nitrophenyl)-1,2,4-oxadiazol-5-yl]butanoic acid
crystallization data
4-[3-(5-oxo-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-6-yl)-1,2,4-oxadiazol-5-yl]butanoic acid
SB-02066; SEW-01456
4-[5,7-dimethoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
4-[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]-2-butenoic acid methyl ester
-
23% inhibition of ALR2 at 0.05 mM
4-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]-2-butenoic acid
-
IC50: 0.0042 mM
4-[7-hydroxy-5-methoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
5,6-dihydro-1-((E)-3-(3,4,5-trimethoxyphenyl)acryloyl)pyridin-2(1H)-one
-
-
5-(3-aminobenzylidene)-2,4-thiazolidinedione
-
IC50: 0.0202 mM
5-(3-hydroxybenzylidene)-2,4-thiazolidinedione
-
IC50: 0.0107 mM
5-(3-methoxybenzyl)-2,4-thiazolidinedione
-
16% inhibition of ALR2 at 0.05 mM
5-(3-nitrobenzylidene)-2,4-thiazolidinedione
-
21% inhibition of ALR2 at 0.05 mM
5-(3-phenoxybenzyl)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.10
5-(3-phenoxybenzyl)-2,4-thiazolidinedione
-
IC50: 0.0789 mM
5-(4-aminobenzylidene)-2,4-thiazolidinedione
-
44% inhibition of ALR2 at 0.05 mM
5-(4-benzyloxybenzyl)-2,4-thiazolidinedione
-
IC50: 0.0314 mM
5-(4-benzyloxybenzylidene)-2,4-thiazolidinedione
-
10% inhibition of ALR2 at 0.05 mM
5-(4-hydroxybenzylidene)-2,4-thiazolidinedione
-
IC50: 0.009 mM
5-(4-methoxybenzyl)-2,4-thiazolidinedione
-
21% inhibition of ALR2 at 0.05 mM
5-(4-nitrobenzylidene)-2,4-thiazolidinedione
-
37% inhibition of ALR2 at 0.05 mM
5-(4-phenoxybenzyl)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.39
5-(4-phenoxybenzyl)-2,4-thiazolidinedione
-
IC50: 0.0404 mM
5-(biphenyl-4-ylmethyl)-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.18
5-androsten-3beta-ol-17-one
i.e. dehydroepiandrosterone
5-biphenyl-4-ylmethyl-2,4-thiazolidinedione
-
IC50: 0.0658 mM
5-biphenyl-4-ylmethylene-2,4-thiazolidinedione
-
20% inhibition of ALR2 at 0.05 mM
5-cholenic acid-3beta-ol
-
5-hydroxy-3S-hydroxymethyl-6-methyl-2,3-dihydrobenzofuran
-
-
5-naphthalen-1-ylmethylene-2,4-thiazolidinedione
-
IC50: 0.0107 mM
5-oxo-3-phenyl-5-(quinolin-2-ylamino)pentanoic acid
HTS-06058
5-[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino]pentanoic acid
-
5-[(4-oxo-2-phenyl-4H-chromen-6-yl)methyl]-1,3-thiazolidine-2,4-dione
-
-
5-[(6-isopropyl-4-oxo-4H-chromen-3-yl)methylene]thiazolidine-2,4-dione
-
-
5-[(6-methyl-4-oxo-4H-chromen-3-yl)methylene]thiazolidine-2,4-dione
-
-
5-[3-(4-oxo-4H-chromen-2-yl)benzyl]-1,3-thiazolidine-2,4-dione
-
-
5-[4-(4-oxo-4H-chromen-2-yl)benzyl]-1,3-thiazolidine-2,4-dione
-
-
5-[4-(benzyloxy)benzyl]-1,3-thiazolidine-2,4-dione
-
pIC50 is 4.50
5alpha-Androstan-17alpha-ol-3-one
-
5alpha-androstan-17beta-ol-3-one
i.e. 5alpha-dehydrotestosterone
5alpha-Androstan-3alpha-ol-17-one
-
5alpha-Androstan-3beta-ol-17-one
competitive inhibition with respect to geraniol
5alpha-androstane-3,17-dione
competitive inhibition with respect to geraniol
5alpha-androstane-3alpha,17beta-diol
-
5alpha-Androstane-3beta,17beta-diol
-
5alpha-cholanic acid-3beta-ol
-
5alpha-pregnan-3beta-ol-20-one
-
5alpha-pregnane-21-ol-3,20-dione
-
5alpha-pregnane-3,20-dione
competitive inhibition with respect to geraniol
5beta-androstan-17beta-ol-3-one
-
5beta-Androstan-3alpha-ol-17-one
-
5beta-androstan-3beta-ol-17-one
-
5beta-androstane-3,17-dione
-
5beta-androstane-3beta,17beta-diol
-
5beta-cholanic acid
competitive inhibition with respect to geraniol
5beta-cholanic acid methyl ester
-
5beta-cholanic acid-3-one
-
5beta-cholanic acid-3alpha,12alpha-diol
i.e. chenodeoxycholic acid
5beta-cholanic acid-3alpha,6alpha-diol
i.e. hyodeoxycholic acid
5beta-cholanic acid-3alpha,7alpha,12alpha-triol
i.e. cholic acid
5beta-cholanic acid-3alpha,7alpha-diol
i.e. deoxycholic acid
5beta-cholanic acid-3alpha,7beta-diol
i.e. ursodeoxycholic acid
5beta-cholanic acid-3alpha-ol
i.e. lithocholic acid
5beta-cholanic acid-3beta-ol
i.e. isolithocholic acid
5beta-Pregnan-3alpha-ol-20-one
-
5beta-Pregnan-3beta-ol-20-one
-
5beta-pregnane-3,20-dione
-
6',6''-dinitrorosmarinic acid
docking structure with ALR2, overview
6'-nitrorosmarinic acid
docking structure with ALR2, overview
6,7-dichloro-3-(4-methylpiperazin-1-yl)quinoxalin-2(1H)-one
-
-
6,7-dihydroxy-4-methylcoumarin
-
-
6,7-dihydroxy-4-phenylcoumarin
-
binds to ALR2 in a different manner from epalrestat, molecular docking, overview. Suppresses galactitol accumulation
6,7-dihydroxycoumarin
-
-
6-(2,3-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 55 nM
6-(2,3-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 35 nM
6-(2,3-difluorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 390 nM
6-(2,3-difluorophenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 257 nM
6-(2,4-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 190 nM
6-(2,4-dichlorophenylsulfonyl)-2H-pyridazin-3-one
-
-
6-(2,4-difluorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 870 nM
6-(2,5-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 73 nM
6-(2,6-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 50 nM
6-(2,6-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 52 nM
6-(2-bromobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 210 nM
6-(2-chloro-4-fluorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 280 nM
6-(2-chloro-6-fluorophenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 26 nM
6-(2-chlorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 170 nM
6-(2-chlorophenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 118 nM
6-(2-fluoro-3-chlorophenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 54 nM
6-(2-fluoro-3-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 44 nM
6-(2-fluoro-4-bromophenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 667 nM
6-(2-fluorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 540 nM
6-(2-fluorophenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 422 nM
6-(2-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 500 nM
6-(3,4-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
-
-
6-(3,5-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
-
-
6-(3,5-dimethylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 13 nM
6-(3-chlorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 240 nM
6-(3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 140 nM
6-(3-phenylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 23 nM
6-(3-trifluoromethylbenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 175 nM
6-(3-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 72 nM
6-(3-[4-fluorophenyl]benzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 49 nM
6-(4-bromo-2-fluorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 140 nM
6-(4-bromobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 350 nM
6-(4-chlorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 380 nM
6-(4-fluorobenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 474 nM
6-(4-methoxybenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 0.002 mM
6-(4-trifluoromethylbenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 360 nM
6-(5,6-methylenedioxyindole-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 0.0038 mM
6-(5,7-dichlorobenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 87 nM
6-(5,7-dichloroindole-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 200 nM
6-(5-chloro,3-methylbenzofuran-2-sulfonyl)2H-pyridazin-3-one
-
6-(5-chloro-3-ethylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 6 nM
6-(5-chloro-3-isopropylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 92 nM
6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 0.001 mM
6-(5-chloro-3-methylbenzothiophene-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 55 nM
6-(5-chloro-3-phenylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 34 nM
6-(5-chlorobenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 25 nM
6-(5-chloroindole-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 0.0011 mM
6-(5-fluoro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 3 nM
6-(5-methoxybenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 230 nM
6-(5-methylbenzothiophene-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 160 nM
6-(5-trifluoromethyl-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 5 nM
6-(6-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 190 nM
6-(6-chloroindole-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 645 nM
6-(6-fluoroindole-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 0.0014 mM
6-(7-chloroindole-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 450 nM
6-(alpha-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 150 nM
6-(benzofuran-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 150 nM
6-(benzothiazole-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 450 nM
6-(benzothiophene-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 180 nM
6-(beta-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one
-
IC50: 360 nM
6-(biphenyl-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 0.0022 mM
6-(indole-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 590 nM
6-bromo-3-(3,5-dihydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
19.8fold selectivity for AKR1B1 over AKR1A1
6-bromo-3-chloroquinoxalin-2(1H)-one
-
-
6-chloro-3-(3,5-dihydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
18.4fold selectivity for AKR1B1 over AKR1A1
6-hydroxy-2-phenyl-4H-pyrido[1,2-a]pyrimidin-4-one
-
6-hydroxy-7-methoxycoumarin
-
-
6-methoxypaeoniflorigenone
-
-
6-[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino]hexanoic acid
-
6-[(5-chloro-3-methyl-1-benzofuran-2-yl)sulfonyl]pyridazin-3(2H)-one
binding structure, inhibition mechanism, residues Trp111, His110, Thr113, Tyr48, Trp20, and Phe122, and the residues of the C-terminal loop Ala299, Leu300, Leu301, Ser302, Cys303 are involved, overview
6-[[(di(2,4-dimethoxyphenyl)methylidene)amino]oxy]hexanoic acid
-
-
6-[[(di(3,5-dimethoxyphenyl)methylidene)amino]oxy]hexanoic acid
-
-
6-[[(di(4-methoxy-3-methylphenyl)methylidene)amino]oxy]hexanoic acid
-
-
7-bromo-3-chloroquinoxalin-2(1H)-one
-
-
7-hydroxy-4-methylcoumarin
-
-
7-Hydroxy-4-oxo-4H-chromen-2-carboxylic acid
-
-
7-hydroxy-4-phenylcoumarin
-
-
7-hydroxy-6-methoxycoumarin
-
-
7-hydroxylcoumarin-4-acetic acid
-
-
7-hydroxylcoumarinyl-4-acetic acid
-
-
7-methyl-2,3-dihydrospiro[4H-thiopyrano[2,3-b]pyridin-4,4'imidazolidine]-2',5'-dione
-
50% inhibition at 0.0011 mM
8-bromo-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid
-
4fold decreased inhibitory potency compared to the nonsubstituted parent compound
8-chloro-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid
-
4fold decreased inhibitory potency compared to the nonsubstituted parent compound
8-methoxy-N-[(1S)-2-methyl-1-(5-phenyl-1H-imidazol-2-yl)propyl]-2H-1-benzopyran-3-carboxamide
-
8-methoxy-N-[(5-phenyl-1H-imidazol-2-yl)methyl]-2H-1-benzopyran-3-carboxamide
-
8-methoxy-N-[[5-(4-methoxyphenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
-
8-methyl-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid
-
2fold decreased inhibitory potency compared to the nonsubstituted parent compound
8-O-benzoylpaeonidanin
-
-
8-phenylsulfonylphthalazin-2H-3-one
-
IC50: 55 nM
alpha-benzoyloxypaeoniflorin
-
-
berberine chloride
-
50% inhibition at 13.98 nM
berberine iodide
-
50% inhibition at 32.84 nM
berberine sulfate
-
50% inhibition at 13.45 nM
beta-benzoyloxypaeoniflorin
-
-
bezafibrate
-
noncompetitive, IC50: 0.003 mM, recombinant enzyme
bisdemethoxycurcumin
-
i.e. 1,7-bis(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0137 mM
butein
-
89.9% inhibition at 0.002 mM
Ca2+
-
10 mM inhibits complex formation of ALR 2 with alpha-crystallin
capsaicin
-
noncompetitive
Cibacron blue F3GA
competitive inhibition with respect to NADP+, noncompetitive inhibition with respect to geraniol
ciprofibrate
-
competitive, IC50: 0.00086 mM, recombinant enzyme
citrate
-
inhibition is pH-dependent
Clofibric acid
-
noncompetitive, IC50: 0.0012 mM, recombinant enzyme
delphinidin 3-O-beta-galactopyranoside
-
most potent inhibitor
delphinidin 3-O-beta-galactopyranoside-3',5'-di-O-beta-glucopyranoside
-
-
demethoxycurcumin
-
i.e. 1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0159 mM
Diphenic acid
-
less than 25% inhibition at 0.5 mM
disodium 4,6-dioxo-10-propyl-4H,6H-pyranol[3,2-g-]-quinoline-2,8-dicarboxylate
-
non-competitive
DL-dihydrolipoic acid
-
binds very tight to the enzyme, best inhibitor of the investigated, competitive
DL-lipoamide
-
binds three-fold more weakly than D,L-lipoic acid, competitive
DL-lipoic acid
-
is effective in the treatment of diabetic complications, binds tightly to the enzyme, competitive
DTT
-
activates the enzyme in healthy heart slightly, but slightly inhibits the ischemic heart enzyme
estriol
i.e. 16alpha-hydroxyestradiol
ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate
-
an AR inhibitor, abolishes the accumulation of TPA-treated cells in S phase was almost completely
Euphorbia regis-jubae aqueous extract
-
-
-
Euphorbia regis-jubae hydroethanolic extract
-
-
-
fenofibrate
-
competitive, IC50: 0.00056 mM, recombinant enzyme
fisetin
-
31.1% inhibition at 0.002 mM
fustin
-
20.1% inhibition at 0.002 mM
gemfibrozil
-
noncompetitive, IC50: 0.0065 mM, recombinant enzyme
gigantol
-
the binding of gigantol to aldose reductase is concentration-dependent and the maximum stoichiometric ratio of non-covalent bonding is 1:24.4. pH and temperature do not influence the interaction. Gigantol is protective against diabetic cataracts in rats induced by streptozotocin
glutathionyl-1,4-dihydroxynonene
-
i.e. GS-DHN, the mitogenic effects of HNE, but not GS-HNE or GSDHN, are abolished by glutathione depletion, stimulates protein kinase C, NF-kappaB, and AP-1, and increases cell growth in vascular smooth muscle cells
glutathionyl-4-hydroxynonenal
-
i.e. GS-HNE, the mitogenic effects of HNE, but not GS-HNE or GSDHN, are abolished by glutathione depletion, stimulates protein kinase C, NF-kappaB, and AP-1, and increases cell growth in vascular smooth muscle cells
glyceraldehyde
-
substrate inhibition
glycerol
-
uncompetitive to DL-glyceraldehyde
glycochenodeoxycholic acid
-
glycolithocholic acid
competitive inhibition with respect to geraniol
hexanoic acid
-
competitive
isolithocholic acid
uncompetitive inhibition with respect to NADP+, competitive inhibition with respect to geraniol
isorhamnetin 3-O-beta-D-galactopyranoside
-
-
isorhamnetin 3-O-beta-D-glucopyranoside
-
-
jateorrhizine
-
12.68-14.08% inhibition at 0.05 mg/ml
kaempferol 3-O-rutinoside
-
KCl
0.5 M, 76% residual activity, 1 M, 37% residual activity
kuraridin
-
potent inhibitor of recombinant human aldose reductase
kurarinol
-
potent inhibitor of rat lens aldose reductase
kurarinone
-
potent inhibitor of rat lens aldose reductase
L-tyrosine
able to prevent the formation of the tubulin/aldose reductase complex and the activation of aldose reductase by tubulin
lithocholic acid
competitive inhibition with respect to geraniol
lukianol B
-
IC50: 0.0006 mM
Ly-294002
-
0.05 mM, little decrease in sorbitol-induced activity
magnoflorine
-
18.33-29.85% inhibition at 0.05 mg/ml
malondialdehyde
-
at concentration above 0.8 mM substrate inhibition
Mandelic acid
-
competitive
Medroxyprogesterone acetate
-
less than 25% inhibition at 0.01 mM
methyl 2-(2-oxo-3-((3,4,5-trifluorophenyl)amino)quinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-((2,4-difluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-((4-bromo-2-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-((4-bromophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-((4-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-bromo-2-fluorophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-bromo-2-fluorophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-bromo-2-fluorophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-bromo-2-fluorophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetat
-
-
methyl 2-(3-(4-bromophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-bromophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-bromophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-bromophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(6-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(6-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(6-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(6-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(6-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(7-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(7-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(7-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(7-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(7-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 3-methyl-2-([2-nitro-4-(trifluoromethyl)phenyl]amino)butanoate
-
methyl [(5Z)-2,4-dioxo-5-(3-phenoxybenzylidene)-1,3-thiazolidin-3-yl]acetate
-
pIC50 is 5.88
methyl [(5Z)-5-(3-aminobenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetate
-
pIC50 is 4.41
methyl [(5Z)-5-(3-methoxybenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetate
-
pIC50 is 5.05
methyl [(5Z)-5-(3-methylbenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetate
-
pIC50 is 5.00
methyl [(5Z)-5-(4-fluorobenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetate
-
pIC50 is 4.89
methyl [(5Z)-5-(4-hydroxybenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetate
-
pIC50 is 5.21
methyl [5-(3-methoxybenzyl)-2,4-dioxo-1,3-thiazolidin-3-yl]acetate
-
pIC50 is 4.68
methyl {(5Z)-2,4-dioxo-5-[3-(trifluoromethyl)benzylidene]-1,3-thiazolidin-3-yl}acetate
-
pIC50 is 4.54
methyl {(5Z)-2,4-dioxo-5-[4-(trifluoromethyl)benzylidene]-1,3-thiazolidin-3-yl}acetate
-
pIC50 is 5.46
Mg2+
-
10 mM inhibits complex formation of ALR 2 with alpha-crystallin, induces ALR 2 aggregation and precipitation
Morin hydrate
-
14.1% inhibition at 0.002 mM
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-beta-alanine
-
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-alanine
-
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-isoleucine
-
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-leucine
-
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-phenylalanine
-
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-serine
-
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-tyrosine
-
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-valine
-
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)glycine
-
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)glycyl-L-phenylalanine
9% inhibition at 10.5 mM
N-(2-phenylethyl)-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
-
-
N-(2-phenylethyl)-N-[(3-nitrophenyl)sulfonyl]glycine
-
-
N-(2-phenylethyl)-N-[(4-bromophenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-(2-phenylethyl)-N-[(4-chlorophenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-(2-phenylethyl)-N-[(4-fluorophenyl)sulfonyl]glycine
-
-
N-(2-phenylethyl)-N-[(4-methylphenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-(2-phenylethyl)-N-[(4-nitrophenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-(2-phenylethyl)-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-(2-phenylethyl)-N-{[4-(trifluoromethyl)phenyl]sulfonyl}glycine
-
-
N-(3,5-difluoro-4-hydroxyphenyl)-4-methoxybenzenesulfonamide
-
-
N-(3,5-difluoro-4-hydroxyphenyl)-4-nitrobenzenesulfonamide
-
-
N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamide
-
compound exhibits high antioxidant potential. Determination of intestine permeability
N-(tert-butyl)-3-(4-(4-nitrobenzyl)-3-oxo-3,4-dihydroquinoxalin-2-ylacryl amide
-
N-acetyl-2,3-dihydrospiro[4H-thiopyrano[2,3-b]pyridin-4,4'imidazolidine]-2',5'-dione
-
50% inhibition at 0.050 mM
N-benzyl-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
-
-
N-benzyl-N-[(2-naphthalenyl)sulfonyl]glycine
-
-
N-benzyl-N-[(3-nitrophenyl)sulfonyl]glycine
-
-
N-benzyl-N-[(4-bromophenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-benzyl-N-[(4-chlorophenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-benzyl-N-[(4-fluorophenyl)sulfonyl]glycine
-
-
N-benzyl-N-[(4-methylphenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-benzyl-N-[(4-nitrophenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-benzyl-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-cyclopropyl-N-[cyclopropyl(5-phenyl-1H-imidazol-2-yl)methyl]-2H-1-benzopyran-3-carboxamide
-
N-cyclopropyl-N-[cyclopropyl(5-phenyl-1H-imidazol-2-yl)methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
-
N-cyclopropyl-N-[cyclopropyl[5-(pyridin-3-yl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
-
N-cyclopropyl-N-[cyclopropyl[5-(pyridin-3-yl)-1H-imidazol-2-yl]methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
-
N-galloyl beta-D-glucopyranosylamine
N-tert-butyl-2-(2-chloro-6-methoxy-4-([(3-methyl-5-sulfanyl-4H-1,2,4-triazol-4-yl)amino]methyl)phenoxy)acetamide
-
N-[(1S)-1-[5-(4-bromophenyl)-1H-imidazol-2-yl]-2-methylpropyl]-2H-1-benzopyran-3-carboxamide
-
N-[(1S)-1-[5-(4-bromophenyl)-1H-imidazol-2-yl]-2-methylpropyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
-
N-[(1S)-2-methyl-1-(5-phenyl-1H-imidazol-2-yl)propyl]-2H-1-benzopyran-3-carboxamide
-
N-[(5-phenyl-1H-imidazol-2-yl)methyl]-2H-1-benzopyran-3-carboxamide
-
N-[2-(2-thienyl)ethyl]-N-[(1,10-biphenyl)-4-sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(1-naphthalenyl)sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(2-naphthalenyl)sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(3-nitrophenyl)sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(4-bromophenyl)sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(4-chlorophenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-[2-(2-thienyl)ethyl]-N-[(4-fluorophenyl)sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(4-nitrophenyl)sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(5-dimethylamino-1 naphthalenyl)sulfonyl]glycine
-
-
N-[2-(2-thienyl)ethyl]-N-[(5-dimethylamino-1-naphthalenyl)sulfonyl]glycine
-
-
N-[[5-(4-bromophenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
-
N-[[5-(4-bromophenyl)-1H-imidazol-2-yl]methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
-
N-[[5-(4-chlorophenyl)-1H-imidazol-2-yl](cyclopropyl)methyl]-N-cyclopropyl-2H-1-benzopyran-3-carboxamide
-
N-[[5-(4-chlorophenyl)-1H-imidazol-2-yl](cyclopropyl)methyl]-N-cyclopropyl-8-methoxy-2H-1-benzopyran-3-carboxamide
-
N-[[5-(4-chlorophenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
-
N-[[5-(4-chlorophenyl)-1H-imidazol-2-yl]methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
-
N-[[5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
-
N-[[5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
-
N-[[5-(4-methoxyphenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
-
N-[[6-methoxy-5(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglycine
N2-(2-methylaminobenzoyl)tetrahydro-1H-pyrido[3,4-b]indol-1-one
-
i.e. rhetsinine, from Evodia rutaecarpa hot water extract. Rhetsinine inhibits sorbitol accumulation by 79.3% at 0.1 mM in erythrocytes
naphtho[1,2-d]isothiazole acetic acid derivatives
-
-
naringenin
uncompetitive. The interaction is enthalpy driven and the microenvironment of aromatic residues is also altered. Naringenin inhibits fructosamine content by approximately 31.6% at 0.01 mM, and more than 93% inhibition of fluorescent advanced glycation end-products is achieved. Naringenin forms hydrogen bonds (Asn160 and Ile260), and two Pi-Pi interactions with Trp20 and one with His110
nitazoxanide
-
partial inhibition
p-Carboxybenzaldehyde
-
substrate inhibition at higher concentration
p-nitrobenzaldehyde
-
at concentration above 2 mM substrate inhibition
palmatine iodide
-
50% inhibition at 68 nM
palmatine sulfate
-
50% inhibition at 51.78 nM
PD-98059
-
0.05 mM, decrease of sorbitol-induced activity to control level
pentagalloyl glucose
-
46.6% inhibition at 0.002 mM
phenylacetic acid
-
competitive
protocatechuic acid
-
12.6% inhibition at 0.002 mM
puerariafuran
-
a 2-arylbenzofuran from Pueraria lobata, collected in Kyonggi-do, Seongnam, Kyungwon University, Korea. Xylose-induced opacity of lenses is significantly improved when treated with puerariafuran
pyrazolo[5,1-c][1,2,4]benzotriazin-8-yl dimethylcarbamate
EN-00263
quercetin 3-O-(2''-O-acetyl)-beta-D-glucopyranoside
-
-
quercetin 3-O-(6''-O-acetyl)-beta-D-glucopyranoside
-
-
quercetin 3-O-(6''-O-benzoyl)-beta-D-galactopyranoside
-
-
quercetin 3-O-beta-D-apiofuranosyl-(1->2)-beta-D-glucopyranoside
-
rhamnocitrin-3-O-rhamnoside
-
rosmarinic acid
docking structure with ALR2, overview
S-nitroso-N-acetylpenicillamine
-
1 mM, 86% inhibition, reversed by incubation with fresh media
S-nitrosoglutathione monoethylester
-
1 mM, 73% inhibition, reversed by incubation with fresh media
S12728
-
inhibitor of ALR2, but no inhibition of ALR1
SB-203580
-
0 0.01 mM, decrease of sorbitol-induced activity below control level
sorbitol
-
competitive inhibition with NADP+ and glucose
Statil
molecular modeling redicts an enhancement of net binding energy of the complex by 33% through replacement of the fluorine atom of statil by a carboxylate group
stobadine
-
i.e. (-)-cis-2,8-dimethyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3,-b]indole
sulfhydryl inhibitors
-
-
-
sulfuretin
-
69.8% inhibition at 0.002 mM
sulindac
exhibits both the highest inhibitory activity towards human aldose reductase among popular non-steroidal anti-inflammatory drugs and clear beneficial clinical effects on Type 2 diabetes, uncompetitive inhibition, enzyme binding structure, overview
sulindac sulfide
enzyme binding structure, overview
sulindac sulfone
enzyme binding structure, overview
tetramethylene glutaric acid
-
-
thienocinnolinone alkanoic acid derivatives
-
i.e. 8-halogen-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid derivatives, synthesis and inhibitory potency, IC50 as low as 0.0314 mM, the length of the N2 alkanoic chain strongly influences the inhibitory activity, overview
-
tizoxanide
-
partial inhibition
Tolmetin
enzyme binding structure, overview
Valproate
-
less than 25% inhibition at 0.5 mM
zofenoprilat-glutathione disulfide
-
the enzyme is specifically S-thionylated and inactivated by ZSSG, a homodisulfide formed by GSH and zofenoprilat, an angiotensin-converting enzyme inhibitor carrying a thiol group, which is more stable than glutathione, optimization, overview
[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino](phenyl)acetic acid
-
[(2E)-2-[2-(carboxymethyl)hydrazinylidene]-3-[[4-(trifluoromethyl)phenyl]methyl]-2,3-dihydro-1H-benzimidazol-1-yl](oxo)acetic acid
-
[(3-[[(3-nitrophenyl)methyl]carbamoyl][1,1'-biphenyl]-4-yl)oxy]acetic acid
-
[(5H-[1,2,4]triazino[5,6-b]indol-3-yl)sulfanyl]acetic acid
-
[(5Z)-2,4-dioxo-5-(3-phenoxybenzylidene)-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.89
[(5Z)-2,4-dioxo-5-(4-phenoxybenzylidene)-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.09
[(5Z)-5-(3-fluorobenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.13
[(5Z)-5-(3-hydroxy-4-methoxybenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.25
[(5Z)-5-(3-hydroxybenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.18
[(5Z)-5-(3-methoxybenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.32
[(5Z)-5-(3-methylbenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.19
[(5Z)-5-(3-nitrobenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.31
[(5Z)-5-(4-fluorobenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 5.94
[(5Z)-5-(4-hydroxy-3-methoxybenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.15
[(5Z)-5-(4-hydroxybenzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.82
[(5Z)-5-(biphenyl-4-ylmethylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.59
[(5Z)-5-(naphthalen-1-ylmethylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.77
[(5Z)-5-[(2E)-2-methyl-3-phenylprop-2-en-1-ylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]acetic acid
-
[2,4-dioxo-5-(3-phenoxybenzyl)-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 6.00
[2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid
-
IC50: 0.0010 mM
[2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid methyl ester
-
26% inhibition of ALR2 at 0.05 mM
[2,4-dioxo-5-(4-phenoxybenzyl)-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 5.55
[2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid
-
IC50: 0.0028 mM
[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]acetic acid
-
IC50: 0.00082 mM
[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]acetic acid methyl ester
-
33% inhibition of ALR2 at 0.05 mM
[2-(ethynylcarbamoyl)-5-fluorophenoxy]acetic acid
the ligand exhibits a terminal pi-electron rich substituent at the amide function, which fills the cleft between Leu300 and Trp219 next to the sealed specificity pocket
[2-oxo-3-(2-phenylethyl)quinoxalin-1(2H)-yl]acetic acid
-
[2-oxo-3-[(Z)-2-phenylethenyl]quinoxalin-1(2H)-yl]acetic acid
-
[2-oxo-8-[(E)-2-phenylethenyl]-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
9fold selectivity for ALR2 over ALR1
[2-[(1,3-benzothiazol-2-yl)carbamoyl]-5-fluorophenoxy]acetic acid
an H-bond is formed between the backbone Leu300NH group and the nitrogen atom of the benzothiazolyl moiety
[2-[(2-carbamoylphenyl)methyl]-3-oxo-2,3-dihydro-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
-
424fold selectivity for ALR2 over ALR1
[2-[(2-cyanophenyl)methyl]-3-oxo-2,3-dihydro-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
-
1333fold selectivity for ALR2 over ALR1
[3,4-dioxo-10-[[4-(trifluoromethyl)phenyl]methyl]-3,4-dihydro[1,2,4]triazino[4,3-a]benzimidazol-2(10H)-yl]acetic acid
-
[3-(2,2-dimethylpropanoyl)-1H-indol-1-yl]acetic acid
-
[3-(2,4-dihydroxyphenyl)-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-(2,5-dihydroxyphenyl)-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
-
-
[3-[(4-chlorophenyl)methyl]-1,2,4-oxadiazol-5-yl]acetic acid
-
[3-[(diethylamino)methyl]-1H-indol-1-yl]acetic acid
-
[3-[(dimethylamino)methyl]-2-methyl-1H-indol-1-yl]acetic acid
-
[3-[(E)-2-(3,4-dihydroxyphenyl)ethenyl]-6-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[(E)-2-(3,4-dihydroxyphenyl)ethenyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
most potent activity
[3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-6-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[(E)-2-(4-hydroxyphenyl)ethenyl]-6-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[(E)-2-(4-hydroxyphenyl)ethenyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
most active inhibitor evaluated
[3-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[(morpholin-4-yl)methyl]-1H-indol-1-yl]acetic acid
-
[3-[(propan-2-yl)sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
-
[3-[(pyrrolidin-1-yl)methyl]-1H-indol-1-yl]acetic acid
-
[3-[2-(4-hydroxy-3-methoxyphenyl)ethyl]-6-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[2-(4-hydroxy-3-methoxyphenyl)ethyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[3-[2-(4-hydroxyphenyl)ethyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[5-(3-aminobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
-
IC50: 0.039 mM
[5-(3-carboxymethoxy-4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
i.e. CMD, a potent inhibitor of ALR2, but not for ALR1, structure molecular modelling, overview. The non-conserved C-terminal residue Leu300 in ALR2, which is Pro301 in ALR1, contributes to inhibitor selectivity
[5-(3-hydroxy-4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
i.e. HMD, modelling of inhibitor-enzyme active site complex
[5-(3-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.00066 mM
[5-(3-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
43% inhibition of ALR2 at 0.05 mM
[5-(3-methoxybenzyl)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 5.53
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.0030 mM
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
IC50: 0.0211 mM
[5-(3-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid
-
IC50: 0.00049 mM
[5-(3-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
-
22% inhibition of ALR2 at 0.05 mM
[5-(4-aminobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
-
25% inhibition of ALR2 at 0.05 mM
[5-(4-benzyloxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
24% inhibition of ALR2 at 0.05 mM
[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.00028 mM
[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
12% inhibition of ALR2 at 0.05 mM
[5-(4-bromophenyl)-3-methyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
-
[5-(4-chlorophenyl)-1-oxo-3-propylpyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
18fold selectivity for isoform AKR1B1 over AKR1B10
[5-(4-chlorophenyl)-3-ethyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
39fold selectivity for isoform AKR1B1 over AKR1B10
[5-(4-chlorophenyl)-3-ethyl-9-fluoro-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
9fold selectivity for isoform AKR1B1 over AKR1B10
[5-(4-chlorophenyl)-3-methyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
37fold selectivity for isoform AKR1B1 over AKR1B10
[5-(4-chlorophenyl)-9-fluoro-3-methyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
3fold selectivity for isoform AKR1B1 over AKR1B10
[5-(4-hydroxybenzyl)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 5.68
[5-(4-hydroxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.0021 mM
[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.00015 mM
[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
IC50: 0.0062 mM
[5-(4-methoxybenzyl)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 5.97
[5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.0011 mM
[5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
24% inhibition of ALR2 at 0.05 mM
[5-(4-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid
-
IC50: 0.0012 mM
[5-(4-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
-
8% inhibition of ALR2 at 0.05 mM
[5-(biphenyl-4-ylmethyl)-2,4-dioxo-1,3-thiazolidin-3-yl]acetic acid
-
pIC50 is 5.77
[5-fluoro-2-(phenylcarbamoyl)phenoxy]acetic acid
ligand is among the weakest of the known ALR2 binders that open the specificity pocket
[5-fluoro-2-[(3-nitrophenyl)carbamoyl]phenoxy]acetic acid
the ligand opens the specificity pocket with its terminal benzyl moiety and places the meta attached nitro group deeply in the transient pocket
[5-fluoro-2-[(4,5,7-trifluoro-1,3-benzothiazol-2-yl)carbamoyl]phenoxy]acetic acid
-
[5-fluoro-2-[[[(4,5,7-trifluoro-2-benzothiazolyl)methyl]amino]carbonyl]phenoxy]acetic acid
-
[5-methyl-7-oxo-4-(2-phenylethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl]acetic acid
-
[6-ethyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
-
-
[6-hydroxy-3-(4-hydroxyphenoxy)pyrazin-2-yl](4-hydroxyphenyl)methanone
-
isolated from red ascidian Botryllus leachi, pyrazine derivative, IC50: 0.0194 mM
[6-methoxy-2-oxo-3-(2,4,6-trihydroxyphenyl)quinoxalin-1(2H)-yl]acetic acid
-
[6-methyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
-
-
[7-fluoro-3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[7-fluoro-3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
[7-methoxy-2-oxo-3-(2,4,6-trihydroxyphenyl)quinoxalin-1(2H)-yl]acetic acid
-
[7-methoxy-2-oxo-3-[(E)-2-phenylethenyl]quinoxalin-1(2H)-yl]acetic acid
-
[8-(4-formylphenyl)-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
[8-(4-methoxyphenyl)-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
[8-[(E)-2-(4-fluorophenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
25.7fold selectivity for ALR2 over ALR1
[8-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
24fold selectivity for ALR2 over ALR1
[8-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
60fold selectivity for ALR2 over ALR1
[8-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
[8-[(E)-2-(4-methylphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
[8-[(E)-2-(4-nitrophenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
[8-[(E)-2-(4-tert-butylphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
4fold selectivity for ALR2 over ALR1
[8-[(E)-2-([1,1'-biphenyl]-4-yl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
[9-fluoro-5-(4-methoxyphenyl)-3-methyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
9fold selectivity for isoform AKR1B1 over AKR1B10
[[(4-methylphenyl)sulfonyl](2-thiophen-2-ylethyl)amino]acetic acid
S-12728
{(5Z)-2,4-dioxo-5-[3-(trifluoromethyl)benzylidene]-1,3-thiazolidin-3-yl}acetic acid
-
pIC50 is 6.33
{(5Z)-2,4-dioxo-5-[4-(trifluoromethyl)benzylidene]-1,3-thiazolidin-3-yl}acetic acid
-
pIC50 is 6.34
{(5Z)-5-[3-(carboxymethoxy)-4-ethoxybenzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl}acetic acid
-
pIC50 is 5.85
{(5Z)-5-[3-(carboxymethoxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl}acetic acid
-
pIC50 is 6.64
{(5Z)-5-[4-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl}acetic acid
-
pIC50 is 6.55
{(5Z)-5-[4-(carboxymethoxy)-3-methoxybenzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl}acetic acid
-
pIC50 is 6.59
{(5Z)-5-[4-(carboxymethoxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl}acetic acid
-
pIC50 is 6.22
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
-
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
-
(2S)-3beta,7,4'-trihydroxy-5-methoxy-8-(gamma,gamma-dimethylallyl)-flavanone
-
-
(2S)-3beta,7,4'-trihydroxy-5-methoxy-8-(gamma,gamma-dimethylallyl)-flavanone
-
-
(E,E)-5[2-methyl-3-phenyl-2-propenylidene-4-oxo-2-thioxo-3-thiazolidine]acetic acid
-
-
(E,E)-5[2-methyl-3-phenyl-2-propenylidene-4-oxo-2-thioxo-3-thiazolidine]acetic acid
-
recombinant from baculovirus system in Spodoptera frugiperda cells
(NH4)2SO4
-
0.05 mM: slight inhibition, 400 mM: activation
(NH4)2SO4
-
0.05 mM: slight inhibition, 400 mM: activation
(S)-6-fluorospiro[chroman-4,5'-imidazolidine]-2',4'-dione
-
-
(S)-6-fluorospiro[chroman-4,5'-imidazolidine]-2',4'-dione
-
wild type and recombinant from E. coli
(S)-6-fluorospiro[chroman-4,5'-imidazolidine]-2',4'-dione
-
recombinant from baculovirus system in Spodoptera frugiperda cells
(S)-6-fluorospiro[chroman-4,5'-imidazolidine]-2',4'-dione
-
-
(S)-6-fluorospiro[chroman-4,5'-imidazolidine]-2',4'-dione
-
-
(S)-6-fluorospiro[chroman-4,5'-imidazolidine]-2',4'-dione
-
wild type and recombinant from E. coli
1-O-Galloyl-beta-D-glucose
i.e. beta-glucogallin or BGG, a major component of the Emblica officinalis medicinal plant, and a stable, potent, and specific inhibitor of aldose reductase, noncompetitive inhibition through binding the active site of AKR1B1, occupying both the anionic and the specificity pockets
1-O-Galloyl-beta-D-glucose
i.e. beta-glucogallin or BGG, a major component of the Emblica officinalis medicinal plant, and a stable, potent, and specific inhibitor of aldose reductase, noncompetitive inhibition through binding the active site of AKR1B1, occupying both the anionic and the specificity pockets
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one
mixed-type inhibition
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one
-
650fold selectivity for isoform ALR2 over ALR1
2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one
mixed-type inhibition
2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one
-
858fold selectivity for isoform ALR2 over ALR1
3-(2,4-dihydroxyphenyl)-5-hydroxy-7-methoxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
-
a gamma,gamma-dimethylallyl type prenylated isoflavonoid
3-(2,4-dihydroxyphenyl)-5-hydroxy-7-methoxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
-
a gamma,gamma-dimethylallyl type prenylated isoflavonoid
3-hydroxybutyrate
-
-
3-[3,4-dihydroxy-5-(3-methylbut-2-en-1-yl)phenyl]-5,7-dihydroxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
-
a gamma,gamma-dimethylallyl type prenylated isoflavonoid
3-[3,4-dihydroxy-5-(3-methylbut-2-en-1-yl)phenyl]-5,7-dihydroxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
-
a gamma,gamma-dimethylallyl type prenylated isoflavonoid
4-hydroxy-trans-2-nonenal
-
-
4-hydroxy-trans-2-nonenal
-
i.e. HNE, a lipid peroxidation-derived aldehyde, triggers multiple signaling cascades that variably affect cell growth, differentiation, and apoptosis, the mitogenic effects of HNE, but not GS-HNE or GSDHN, are abolished by glutathione depletion
4-[5,7-dimethoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
-
a gamma,gamma-dimethylallyl type prenylated isoflavonoid
4-[5,7-dimethoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
-
a gamma,gamma-dimethylallyl type prenylated isoflavonoid
4-[7-hydroxy-5-methoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
-
a gamma,gamma-dimethylallyl type prenylated isoflavonoid
4-[7-hydroxy-5-methoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
-
a gamma,gamma-dimethylallyl type prenylated isoflavonoid
5,5-diphenylhydantoin
-
-
5,5-diphenylhydantoin
-
-
8-lavandulylkaempferol
-
potent inhibitor of recombinant human aldose reductase
8-lavandulylkaempferol
-
potent inhibitor of rat lens aldose reductase
Alrestatin
-
1,3-dioxo-1H-benz[de]isoquinoline-2-(3H)acetic acid
Alrestatin
-
inhibits aldose reductase, does not appear to affect RUNX2 activation in cells exposed to euglycemia
Alrestatin
-
1,3-dioxo-1H-benz[de]isoquinoline-2-(3H)acetic acid
Barbital
-
-
Barbital
-
26% inhibition
Barbital
-
less than 25% inhibition at 0.5 mM
Cl-
-
at high ionic strength
Cl-
-
0.2 M, wild type and recombinant from E. coli
Cl-
-
0.2 M, wild type and recombinant from E. coli
coptisine
-
53.85-61.54% inhibition at 0.075 mg/ml
coptisine
-
85.86-86.87% inhibition at 0.05 mg/ml
Cu2+
-
oxidative inactivation of ALR2, ratio Cu2+ to enzyme of 2:1, precipitation of the enzyme occurs at higher Cu2+ concentration, alpha-crystallin stabilizes the enzyme and protects against inactivation and precipitation by Cu2+ with higher efficiency at 37°C compared to 25°C, overview
CuCl2
-
addition of dithiothreitol or 2-mercaptoethanol recovers activity
CuCl2
-
0.007 mM, 20% residual activity, addition of dithiothreitol recovers activity
CuCl2
-
0.007 mM, 20% residual activity, addition of dithiothreitol recovers activity
curcumin
-
i.e. 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0068 mM
curcumin
inhibits ALR2 in a non-competitive manner, also inhibits AKR1B10, docking analysis and kinetics, overview. Curcumin is able to suppress sorbitol accumulation in human erythrocytes under high glucose conditions
davallialactone
-
-
desmethylanhydroicaritin
-
potent inhibitor of recombinant human aldose reductase
desmethylanhydroicaritin
-
potent inhibitor of rat lens aldose reductase
dithiothreitol
-
-
dithiothreitol
-
increased inhibitory effect of sorbinil
ellagic acid
-
-
epalrestat
-
-
epalrestat
-
orally active inhibitor
epalrestat
-
85.8% inhibition at 0.0025 mM
epalrestat
26.7fold selectivity for ALR2 over ALR1
epalrestat
55.7fold selectivity for isoform AKR1B1 over AKR1A1
epalrestat
-
full inhibition
epiberberine
-
69.23-76.92% inhibition at 0.075 mg/ml
epiberberine
-
complete inhibition at 0.05 mg/ml
fidarestat
-
-
fidarestat
-
i.e. inhibitor F, inhibition in vivo and in vitro
fidarestat
complex formation with the enzyme
fidarestat
thermodynamic binding data for isoform ALR2 and mutants
fidarestat
-
aldose reductase inhibitor, attenuates the increase in growth, but in the absence of angiogenic factors, such as VEGF- and FGF, fidarestat alone does not affect the HUVEC growth
fidarestat
an inhibitor highly selective for aldose reductase (AKR1B1, EC 1.1.1.21) versus aldehyde reductase (AKR1A1, EC 1.1.1.2). Inhibitor binding site and structure comparisons of enzymes AKR1B1 and AKR1B10, overview. Fidarestat is specific for aldose reductase AKR1B1 versus aldose reductae-like AKR1B10; an inhibitor highly selective for aldose reductase (AKR1B1, EC 1.1.1.21) versus aldehyde reductase (AKR1A1, EC 1.1.1.2). Inhibitor binding site and structure comparisons of enzymes AKR1B1 and AKR1B10, overview. Fidarestat is specific for aldose reductase AKR1B1 versus aldose reductae-like AKR1B10
fidarestat
significantly inhibits the enzyme activity as well as the enzyme expression
fidarestat
-
inhibition of enzyme in neural stem cells exposed to high glucose concentration results in decrease of oxidative stress, restoration of cell viability and proliferation, and reduction of apoptotic cell death. Inhibition attenuates the down-regulation of glucose transporter 1 expression
fidarestat
-
fidarestat decreases doxorubicin-induced upregulation of CD11b in THP-1 monocytes. Fidarestat attenuates doxorubicin-induced upregulation of IL-6, IL-1bta, and Nos2 in murine BMDM. Fidarestat also attenuates doxorubicin-induced activation and infiltration of multiple subsets of inflammatory immune cells identified by expression of markers CD11b+, CD11b+F4/80+, Ly6C+CCR2high, and Ly6C+CD11b+ in the mouse spleen and liver. Upregulation of markers of mitochondrial biogenesis PGC-1alpha, COX IV, TFAM, and phosphorylation of AMPKalpha1 (Ser485) is observed in THP-1 cells and livers of mice treated with doxorubicin in combination with fidarestat
fidarestat
-
i.e. inhibitor F, inhibition in vivo and in vitro
fidarestat
-
2S4S-eantiomer, i.e. (2S,4S)-6-fluoro-2',5'-dioxospiro-[chroman-4,4'-imidazoline]-2-carboxamide, IC50: 35 nM, binding site structure, binding to the enzyme does not induce conformational changes in the C-loop region, mechanism, active site binding modeling, the stereochemistry of the exocyclic amide group influences the affinity for the enzyme
groenlandicine
-
69.23-76.92% inhibition at 0.075 mg/ml
groenlandicine
-
52.38-60.32% inhibition at 0.05 mg/ml
HgCl2
-
-
hypholomine B
-
-
IDD 594
binding structure, inhibition mechanism, overview
IDD594
-
-
indomethacin
-
indomethacin
-
less than 25% inhibition at 0.1 mM
iodoacetate
-
-
isoliquiritigenin
-
-
kushenol E
-
potent inhibitor of recombinant human aldose reductase
kushenol E
-
potent inhibitor of rat lens aldose reductase
Li2SO4
-
200 mM: inhibition
Li2SO4
-
0.4 M: essential for full activity
lidorestat
-
-
lidorestat
binding mode, overview
liquiritigenin
-
-
minalrestat
complex formation with the enzyme
minalrestat
uncompetitive inhibition
minalrestat
-
cyclic imide inhibitor, mechanism, binds to ALR2 with its isoquinoline ring system located in a hydrophobic pocket formed mainly by the side chains of Trp20, Phe122, and Trp219
Myricitrin
-
-
N-ethylmaleimide
-
-
N-galloyl beta-D-glucopyranosylamine
-
N-galloyl beta-D-glucopyranosylamine
-
N-[[6-methoxy-5(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglycine
-
-
N-[[6-methoxy-5(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglycine
-
wild type and recombinant from E. coli
N-[[6-methoxy-5(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglycine
-
recombinant from baculovirus system in Spodoptera frugiperda cells
N-[[6-methoxy-5(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglycine
-
wild type and recombinant from E. coli
NaCl
-
-
NaCl
0.5 M, 73% residual activity, 1 M, 29% residual activity
NADP+
-
-
NADP+
-
competitve to NADPH
NADP+
-
competitve to NADPH
nitric oxide
-
from NO donors S-nitroso-N-acetylpenicillamine or S-nitrosoglutathione in vivo and in vitro, leads to increased S-glutathiolation of the enzyme
nitric oxide
-
from NO donors S-nitroso-N-acetylpenicillamine or S-nitrosoglutathione in vivo and in vitro, leads to increased S-glutathiolation of the enzyme
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
complete inhibition
p-hydroxymercuribenzoate
-
-
p-hydroxymercuribenzoate
-
-
p-hydroxymercuribenzoate
-
-
Phenobarbital
-
-
ponalrestat
-
IC50: 80 nM
ponalrestat
-
wild type and recombinant from E. coli
ponalrestat
-
wild type and recombinant from E. coli
ponalrestat
-
cytotoxic effect of methylglyoxal is enhanced in presence of ponalrestat
pyridoxal 5'-phosphate
-
inhibits cofactor binding
pyridoxal 5'-phosphate
-
-
quercetin
-
IC50: 0.0376 mM
quercetin
-
IC50: 0.027 mM
quercetin
-
39.1% inhibition at 0.002 mM
quercetin
uncompetitive inhibition
quercetin
-
potent inhibitor of recombinant human aldose reductase
quercetin
-
50% inhibition at 11.15 nM
quercetin
-
76.47-77.94% inhibition at 0.005 mg/ml
quercetin
-
potent inhibitor of rat lens aldose reductase
quercitrin
-
-
rutin
-
-
S-nitrosoglutathione
-
0.05 mM, up to 40% inhibition, possibly due to selctive formation of a single mixed disulfide between glutathione and Cys298
S-nitrosoglutathione
-
1 mM, 70% inhibition, reversed by incubation with fresh media
semilicoisoflavone B
-
contains a gamma,gamma-dimethylchromene ring on the aromatic ring
semilicoisoflavone B
-
contains a gamma,gamma-dimethylchromene ring on the aromatic ring
sorbinil
-
IC50: 0.0011 mM
sorbinil
-
IC50: 0.0034 mM
sorbinil
-
inhibition of enzyme, preventing apotosis and activation of caspase-3, attenuation of TNF-alpha and hyperglykemia-induced activation of protein kinase C
sorbinil
-
competitive, IC50: 0.0021 mM, recombinant enzyme
sorbinil
-
enzyme inhibition abolishes fibroblast growth factorinduced and platelet-derived growth factorinduced up-regulation of PGE2 synthesis and lipid-adehyde signaling, e.g. by 4-hydroxy-trans-2-nonenal, in Caco-2 cells, overview
sorbinil
-
in vivo inhibition potentiates apoptosis due to lipid aldehydes, overview
sorbinil
complex formation with the enzyme
sorbinil
-
orally active inhibitor, IC50: 0.0036 mM
sorbinil
-
inhibition significantly prevents the tumor necrosis factor alpha-induced prostaglandin E2 production in Caco-2 cells
sorbinil
thermodynamic binding data for isoform ALR2 and mutants
sorbinil
-
inhibition of aldose reductase suppresses lipopolysaccharide-stimulated production of nitric oxide and over-expression of inducible nitric oxide synthase. Inhibition also prevents the lipopolysaccaride-induced apoptosis, cell cycle arrest, activation of caspase-3, downregulation of Bcl-xl and up-regulation of Bax and Bak in macrophages
sorbinil
-
50% inhibition at 29 nM
sorbinil
-
AR inhibitor, prevents hyperproliferation of aortic smooth muscle cells
sorbinil
-
aldose reductase inhibitor, IC50: 900 nM
Tolrestat
-
-
Tolrestat
-
inhibition of enzyme, preventing apotosis and activation of caspase-3, attenuation of TNF-alpha and hyperglykemia-induced activation of protein kinase C
Tolrestat
-
0.001 mM, about 50% inhibition
Tolrestat
-
orally active inhibitor
Tolrestat
-
inhibition significantly prevents the tumor necrosis factor alpha-induced prostaglandin E2 production in Caco-2 cells
Tolrestat
thermodynamic binding data for isoform ALR2 and mutants
Tolrestat
uncompetitive inhibition with respect to NADP+, competitive inhibition with respect to geraniol
Tolrestat
uncompetitive inhibition
Tolrestat
-
inhibition of aldose reductase suppresses lipopolysaccharide-stimulated production of nitric oxide and over-expression of inducible nitric oxide synthase. Inhibition also prevents the lipopolysaccaride-induced apoptosis, cell cycle arrest, activation of caspase-3, downregulation of Bcl-xl and up-regulation of Bax and Bak in macrophages
Tolrestat
-
AR inhibitor, prevents hyperproliferation of aortic smooth muscle cells, cell cycle progression in the presence of high glucose was blocked by tolrestat
Tolrestat
-
potent inhibition, mechanism involves residues Arg312, Leu300, and Phe122
Valproic acid
-
vanillic acid
-
-
vanillic acid
able to prevent the formation of the tubulin/aldose reductase complex and the activation of aldose reductase by tubulin
Zenarestat
-
Zenarestat
-
orally active inhibitor
Zn2+
-
-
zopolrestat
-
-
zopolrestat
-
0.001 mM, about 30% inhibition
zopolrestat
-
competitive, IC50: 0.00006 mM, recombinant enzyme
zopolrestat
thermodynamic binding data for isoform ALR2 and mutants
zopolrestat
-
inhibition of aldose reductase suppresses lipopolysaccharide-stimulated production of nitric oxide and over-expression of inducible nitric oxide synthase. Inhibition also prevents the lipopolysaccaride-induced apoptosis, cell cycle arrest, activation of caspase-3, downregulation of Bcl-xl and up-regulation of Bax and Bak in macrophages
zopolrestat
-
inhibition of enzyme, increase in rates of glycolysis and glucose oxidation
zopolrestat
-
treatment with the aldose reductase inhibitor zopolrestat significantly improves endothelial-dependent relaxation in response to acetylcholine in aged rats
additional information
-
high ionic strength inhibits the enzyme to a higher extent when NADPH instead of NADH is used as a cofactor
-
additional information
-
scarcely inhibitory: sorbinil
-
additional information
-
no inhibition by 3,5-bis(3,4-dimethoxybenzylidene)-4-piperidone, 1,5-bis(3,4-dimethoxyphenyl)-1,4-pentadiene-3-one, 2,5-bis(3,4-dimethoxybenzylidene)cyclopentanone, and 2,6-bis(3,4-dimethoxybenzylidene)cyclohexanone, at 0.1 mM
-
additional information
-
molecular modelling, enzyme docking at the active site of the enzyme, structure-activity relationships of 5-arylidene-2,4-thiazolidinediones, an additional aromatic ring or an H-bond donor group on the 5-benzylidene ring enhance ALR2 inhibitory potency, the presence of a carboxylic anionic chain on N-3 is important, and the length of the carboxylic chain is critical, overview, no inhibition by 5b 4-[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]-2-butenoic acid methyl ester
-
additional information
-
poor inhibition by [2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid methyl ester
-
additional information
-
synthesis and evaluation of 2,4-thiazolidinedione inhibitors, structure-activity relationships, overview. No inhibition by (Z)-5-[(4-benzyloxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
additional information
partial nonclassical competitive inhibition is exerted by the aldose hemiacetal on the reduction of the free aldehyde, aldose reductase modulation by hemiacetals, negative cooperative behavior of AR acting on L-idose, mechanism of inhibition, kinetic modelling, nonclassical competitive model, detailed overview
-
additional information
-
partial nonclassical competitive inhibition is exerted by the aldose hemiacetal on the reduction of the free aldehyde, aldose reductase modulation by hemiacetals, negative cooperative behavior of AR acting on L-idose, mechanism of inhibition, kinetic modelling, nonclassical competitive model, detailed overview
-
additional information
synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5-imidazolidine]-2,4-diones, analysis of the Kador-Sharpless model for minimal pharmacophoric requirements for an aldose reductase inhibitor, and superposition of target molecules on a hypoglycemic pharmacophoric model and a aldose reductase pharmacophoric model, overview. Molecular dynamics simulations and inhibitor binding model. Effects of the compounds on diabetic BALB/c mice
-
additional information
-
enzyme-inhibitor complex structures, the hydrophobic nature of the enzyme active site makes significant contributions to inhibitor binding rather than a reliance on pi-pi orbital interactions with Trp 20, overview
-
additional information
-
inhibition of AR protects the ischemic myocardium and is associated with improved energy metabolism
-
additional information
-
enzyme inhibition counteracts nitrosative stress and poly(ADP-ribose) polymerase activation in high-glucose exposed mesengial cells
-
additional information
-
aldose reductase inhibitors have considerable potential for the treatment of diabetes, without increased risk of hypoglycemia, structure-activity relationship study, the applicable side alkyl chain length and the presence of a OCH3 group at C3 in the aromatic ring are essential features for enzyme recognition and binding, no or poor inhibition by gingerol, shogaol, 2-(4-hydroxy-3-nitrophenyl)ethanoic acid, 2-(3,4-dihydroxyphenyl)ethanoic acid, and 2-(4-hydroxyphenyl)ethanoic acid
-
additional information
not inhibited by (Z)-2-[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]acetamide, (Z)-2-[5-(4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide, and (Z)-2-[5-(3-hydroxy-4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
-
additional information
Arg312 in ALR1 contributes favourably to the binding of 3,5-dichlorosalicylic acid through an electrostatic interaction with the inhibitor's electronegative halide atom and undergoes a conformational change upon tolrestat binding. Tyr116 in ALR1 forms electrostatic interactions with the fluorobenzyl moiety of minalrestat and the 3- and 4-hydroxy groups on the phenyl ring of quercetin.
-
additional information
-
identification of inhibitory compounds from Glycyrrhiza uralensis, overview
-
additional information
-
development of series of highly potent and selective [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid aldose reductase inhibitors. The compounds inhibit aldose reductase, but are inactive against aldehyde reductase
-
additional information
enzyme active site interactions with the 3-carboxymethoxy-4-methoxy-phenyl moiety of the inhibitor, binding structure, overview
-
additional information
-
structure analysis of a series of 2,4-thiazolidinediones derivative ALR2 inhibitors, 3D-QSAR molcular modeling, detailed overview. A large volume group next to the R-substituent will increase the ALR2 inhibitory activity, and adding a -CH2COOH substituent at the R-position can generate a compound with higher predicted activity
-
additional information
-
inhibition of the enzyme activity also inhibits the expression of the enzyme protein in xenograft tissue
-
additional information
-
inhibitor molecular docking study with ALR2, overview
-
additional information
partial nonclassical competitive inhibition is exerted by the aldose hemiacetal on the reduction of the free aldehyde, aldose reductase modulation by hemiacetals, negative cooperative behavior of AR acting on L-idose, mechanism of inhibition, kinetic modelling, nonclassical competitive model, detailed overview
-
additional information
-
partial nonclassical competitive inhibition is exerted by the aldose hemiacetal on the reduction of the free aldehyde, aldose reductase modulation by hemiacetals, negative cooperative behavior of AR acting on L-idose, mechanism of inhibition, kinetic modelling, nonclassical competitive model, detailed overview
-
additional information
analysis of pterin-7-carboxamides as aldose reductase inhibitors, evaluation of the inhibitory activity of the compounds
-
additional information
-
analysis of pterin-7-carboxamides as aldose reductase inhibitors, evaluation of the inhibitory activity of the compounds
-
additional information
design and synthesis of chiral 2H-chromene-N-imidazolo-imino acid conjugates as aldose reductase inhibitors, identification by NMR and mass spectrometry, in vitro inhibition screening, molecular docking study, overview
-
additional information
no inhibition by the triazole 1-(beta-D-glucopyranosyl)-4-(3,4,5-trihydroxyphenyl)-1,2,3-triazole, the amide N-phenylacetyl beta-D-glucopyranosylamine, and the glycosides of beta-glucogallin, 2-(3,4,5-trihydroxyphenyl)ethyl beta-D-glucopyranoside, [1-(3,4,5-trihydroxybenzyl)-1,2,3-triazole-4-yl]methyl beta-D-glucopyranoside, and 3-(3,4,5-trihydroxyphenyl)propyl beta-D-glucopyranoside, synthesis and evaluation, overview
-
additional information
identification of aldose reductase inhibitors based on carboxymethylated mercaptotriazinoindole scaffold, structure-activity relationships, overview
-
additional information
synthesis of spiroimidazolidine-2,4-dione derivatives which preserve the minimum requirements of the proposed pharmacophoric models to enhance both activities. All compounds (except 1-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione) reduce the blood glucose level and all inhibit aldose reductase activity
-
additional information
use of dihydrobenzoxazinone derivatives as aldose reductase inhibitors. Most of the derivatives with styryl side chains exhibit good inhibitory activities and most of the compounds reveal powerful antioxidant activity
-
additional information
phenolic hydroxyl groups are important both in C3 side chain and the core structure of quinoxalinone cores for constructing potent ALR2 inhibitors with antioxidant activity
-
additional information
contruction of two explicit models to correlate the binding energies with the inhibitory activities. Flavonoids tend to bind aldose reductase in E and EC states, while sulfonyl-pyridazinones prefer ES and ECS states. Van der Waals and electrostatic interactions always have positive contributions for stabilizing flavonoids and sulfonyl-pyridazinones. The conserved feature for the aldose reductase binding pocket and the aldose reductase inhibitors is the aromatic stacking and hydrogen bonding
-
additional information
synthesis of a series of 1-oxo-pyrimido[4,5-c]quinoline-2-acetic acid derivatives as inhibitors. The 2-amino compounds are unable to inhibit AKR1B1 while the 2-acetic acid derivatives are not cytotoxic against fibrosarcoma HT-1080 cells
-
additional information
-
synthesis of a series of 1-oxo-pyrimido[4,5-c]quinoline-2-acetic acid derivatives as inhibitors. The 2-amino compounds are unable to inhibit AKR1B1 while the 2-acetic acid derivatives are not cytotoxic against fibrosarcoma HT-1080 cells
-
additional information
synthesis of 2-phenoxypyrido[3,2-b]pyrazin-3(4H)-one derivatives.The combination of phenolic 3,5-dihydroxyl in the C2-phenoxy group and C7-halogen (Cl or Br) in the core structure largely increases the AKR1B1 inhibitory activity, and the 3,5-dihydroxyl substituent contributes greatly to the activity enhancement of antioxidation when comparing all the phenolic hydroxyl derivatives
-
additional information
-
inhibition of the aldehyde-metabolizing enzyme modulates NF-kappaB-dependent activation of inflammatory cytokines and chemokines in mouse serum, liver, heart, and spleen, overview
-
additional information
no inhibition by the triazole 1-(beta-D-glucopyranosyl)-4-(3,4,5-trihydroxyphenyl)-1,2,3-triazole, the amide N-phenylacetyl beta-D-glucopyranosylamine, and the glycosides of beta-glucogallin, 2-(3,4,5-trihydroxyphenyl)ethyl beta-D-glucopyranoside, [1-(3,4,5-trihydroxybenzyl)-1,2,3-triazole-4-yl]methyl beta-D-glucopyranoside, and 3-(3,4,5-trihydroxyphenyl)propyl beta-D-glucopyranoside, synthesis and evaluation, overview
-
additional information
-
model of inhibitor binding interactions
-
additional information
-
scarcely inhibitory: sorbinil
-
additional information
-
inhibition of AR protects the ischemic myocardium and is associated with improved energy metabolism
-
additional information
-
enzyme inhibition counteracts nitrosative stress and poly(ADP-ribose) polymerase activation in diabetic kidney cortex
-
additional information
-
synthesis and structure-activity relationship study of inhibitors, overview
-
additional information
inhibitor synthesis, overview, enzyme docking study, modeling, no inhibition by (1,3,3-trioxo-2,3-dihydronaphtho[2,3-d]isothiazol-2-yl)acetic acid and 2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
-
additional information
-
berberine and palmatine exhibit no RLAR inhibitory activities within the test concentration of 0.012.5-0.05 mg/ml; extract and fractions of the rhizome of Coptis chinensis exhibit broad and moderate RLAR inhibitory activities of approximately 0.038.9-0.067.5 mg/ml
-
additional information
-
the enzyme activity is not affected by 0.1 mM Wy14643
-
additional information
-
methanolic and ethanolic extracts of Litchi chinensis fruits are potent inhibitors of rat lens aldose reductase
-
additional information
-
identification of inhibitory compounds from Glycyrrhiza uralensis, overview. Inhibitory effect of the compounds on the sorbitol accumulation in rat lenses incubated with high glucose
-
additional information
-
structure-activity relationship of a series of coumarins as ALR1 inhibitors, overview. The C6 OH group interferes with ALR1 inhibition activity; structure-activity relationship of a series of coumarins as ALR2 inhibitors and their suppressive effect on the accumulation of galactitol in the rat lens, overview. Substitutions in the C7 OH group enhanced the potency toward ALR2
-
additional information
-
design and synthesis of pyrrole based inhibitors and evaluation as selective aldose reductase inhibitors, bioisosterism between a carboxylic acid moiety and that of a tetrazole, overview
-
additional information
-
inhibitory effect of total lignan from fructus Arctii on aldose reductase, ethanolic extract from dry ripe fruits of Arctium lappa
-
additional information
-
synthesis of quinoxalinone derivatives as potent inhibitors of aldose reductase, Structure-activity relationship and molecular docking studies, overview
-
additional information
-
inhibitor development, synthesis and molecular docking, overview
-
additional information
-
inhibitors isolated from Prunus mume flower buds, cultivated in Zhejiang province, China, structure analysis, overview
-
additional information
structure-activity relationships study of quinoxalinone derivatives as aldose reductase inhibitors. Among them, N1-acetate derivatives have significant activity, molecular modeling and docking, overview. Both C3-phenethyl and C6-NO2 groups play an important role in enhancing the activity and selectivity of the quinoxalinone based inhibitors
-
additional information
design and synthesis of potent and multifunctional aldose reductase inhibitors based on quinoxalinones, overview. Phenolic structure is installed in the compounds for the combination of antioxidant activity and strengthening the ability to fight against diabetic complications, radical scavenging activity using the model reaction with the stable free radicals of 2,2-diphenyl-1-picrylhydrazyl. Molecular docking study using the lidorestat-bound conformation of ALR2, PDB ID 1Z3N
-
additional information
flavonoids from Litsea japonica inhibit advanced glycation end products formation and rat lense aldose reductase in vitro with IC50 values of 0.0074-0.072 mM, flavonoid structure determinations by NMR spectroscopy, overview. No significant inhibition by 1, 2, afzelin, quercitrin, rutin, and lyoniside
-
additional information
-
synthesis of derivatives of rhodanine-3-hippuric acid-pyrazole hybrid. All the compounds exhibit a well-defined binding mode within the aldose reductase active site, with the anion head group bound to the catalytic center, blocking thus its activity
-
additional information
-
synthesis of oxotriazinoindole inhibitors
-
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0.01
(1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
Rattus norvegicus
IC50: 0.010 mM
0.02
(1-(2H-tetrazole-5-yl)-1H-pyrrol-2-yl)(phenyl)-methanone
Rattus norvegicus
-
pH 7.2, temperature not specified in the publication
0.018
(1-(2H-tetrazole-5-yl)-1H-pyrrol-3-yl)(phenyl)-methanone
Rattus norvegicus
-
pH 7.2, temperature not specified in the publication
0.0033
(17alpha)-17-hydroxyandrost-4-en-3-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
7.3
(1H-indol-1-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
2.87
(2,3-dihydrocyclopenta[b]indol-4(1H)-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.000678
(2,4-dioxo-5-[(6,8-dimethyl-4-oxo-4H-chromen-3-yl)methylene]-1,3-thiazolidine-3-yl) acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.000522
(2,4-dioxo-5-[(6-isopropyl-4-oxo-4H-chromen-3-yl)methylene]-1,3-thiazolidine-3-yl) acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.000805
(2,4-dioxo-5-[(6-methyl-4-oxo-4H-chromen-3-yl)methylene]-1,3-thiazolidine-3-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.000261
(2,4-dioxo-5-[(6-nitro-4-oxo-4H-chromen-3-yl)methylene]-1,3-thiazolidine-3-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.0182
(2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-8-yl)-acetic acid
Rattus norvegicus
-
pH and temperature not specified in the publication
0.001932
(2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid
Homo sapiens
30°C, pH 6.2
0.00334
(2-oxo-8-phenyl-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid
Homo sapiens
30°C, pH 6.2
0.000138
(2-oxo-8-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid
Homo sapiens
30°C, pH 6.2
0.000241
(2-[[2-(hydroxymethyl)phenyl]methyl]-3-oxo-2,3-dihydro-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.0963 - 0.2572
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
0.04141
(2R)-1-[(benzyloxy)carbonyl]-2,3-dihydro-1H-indole-2-carboxylic acid
Homo sapiens
-
0.00057
(2R,4S)-6-fluoro-2',5'-dioxospiro-[chroman-4,4'-imidazoline]-2-carboxamide
Sus scrofa
-
IC50: 570 nM, mechanism, active site binding modeling, the stereochemistry of the exocyclic amide group influences the affinity for the enzyme
0.00377
(2S)-2'-methoxykurarinone
Rattus norvegicus
-
-
0.00363
(2S)-3beta,7,4'-trihydroxy-5-methoxy-8-(gamma,gamma-dimethylallyl)-flavanone
Rattus norvegicus
-
-
0.00037
(2S)-7,4'-dihydroxy-5-methoxy-8-(gamma,gamma-dimethylallyl)-flavanone
Homo sapiens
-
-
0.00049
(2Z)-3-(3,4-dihydroxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
Rattus norvegicus
-
37°C, pH 7.0
0.00795
(2Z)-3-(3-methoxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
Rattus norvegicus
-
37°C, pH 7.0
0.00111
(3-benzyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00043
(3-methyl-1-oxo-5-phenylpyrimido[4,5-c]quinolin-2(1H)-yl)acetic acid
Homo sapiens
pH 7.5, 25°C
0.097
(3-sulfanyl-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
2.24
(3-[[(2-fluorophenyl)methyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
4.06
(3-[[2-oxo-2-(2,4,6-trimethylanilino)ethyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.0244
(4-hydroxy-3-methoxyphenyl)acetonitrile
Homo sapiens
-
IC50: 0.0244 mM
0.0634
(4-hydroxy-3-methoxyphenyl)methamine
Homo sapiens
-
IC50: 0.0634 mM
0.0414
(4-hydroxyphenyl)(6-hydroxypyrazin-2-yl)methanone
Homo sapiens
-
isolated from red ascidian Botryllus leachi, pyrazine derivative, IC50: 0.0414 mM
0.0214
(4-hydroxyphenyl)[4-(4-hydroxyphenyl)-1H-imidazol-2-yl]methanone
Homo sapiens
-
isolated from red ascidian Botryllus leachi, imidazole derivative, IC50: 0.0214 mM
11.46
(4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indol-5-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.00003
(4-oxo-3-{[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]methyl}-3,4-dihydrophthalazin-1-yl)acetic acid
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.0017
(5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid
Bos taurus
-
IC50: 0.0017 mM
0.00026
(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-acetic acid
Bos taurus
-
IC50: 0.00026 mM
0.00017
(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetic acid
Bos taurus
-
IC50: 0.00017 mM
0.000432
(5E)-5-[4-(4-oxo-4H-chromen-2-yl)benzylidene]-1,3-thiazolidine-2,4-dione
Rattus norvegicus
-
pH 6.2, 37°C
0.019
(5Z)-3-chloro-4-(3,5-dibromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
Homo sapiens
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.019 mM
0.0008
(5Z)-3-chloro-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-4-(4-hydroxyphenyl)furan-2(5H)-one
Homo sapiens
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.0008 mM
0.02
(5Z)-4-(3,5-dibromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
Homo sapiens
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.020 mM
0.013
(5Z)-4-(3-bromo-4-hydroxyphenyl)-3-chloro-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
Homo sapiens
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.013 mM
0.048
(5Z)-4-(3-bromo-4-hydroxyphenyl)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]furan-2(5H)-one
Homo sapiens
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.048 mM
0.017
(5Z)-4-(3-bromo-4-hydroxyphenyl)-5-[(3-bromo-4-hydroxyphenyl)methylidene]-3-chlorofuran-2(5H)-one
Homo sapiens
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.017 mM
0.057
(5Z)-5-[(3,5-dibromo-4-hydroxyphenyl)methylidene]-4-(4-hydroxyphenyl)furan-2(5H)-one
Homo sapiens
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.057 mM
0.046
(5Z)-5-[(3-bromo-4-hydroxyphenyl)methylidene]-3-chloro-4-(4-hydroxyphenyl)furan-2(5H)-one
Homo sapiens
-
isolated from ascidians Ritterella rubra and Synoicum blochmanni, IC50: 0.046 mM
0.000683
(5Z)-5-[(4-oxo-2-phenyl-4H-chromen-6-yl)methylidene]-1,3-thiazolidine-2,4-dione
Rattus norvegicus
-
pH 6.2, 37°C
0.1
(6-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
Rattus norvegicus
IC50: 0.10 mM
0.18
(6-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
Rattus norvegicus
IC50: 0.180 mM
2.75
(6H-indolo[2,3-b]quinoxalin-6-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
9.95
(7H-indolo[2',3':5,6][1,2,4]triazino[2,3-a]benzimidazol-7-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.33
(8-methyl-3-[[2-oxo-2-(propylamino)ethyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.1
(9-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
Rattus norvegicus
IC50: 0.10 mM
0.19
(9-nitro-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
Rattus norvegicus
IC50: 0.190 mM
0.019
(E)-3-(5-(3-nitrophenyl)furan-2-yl)acrylic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0203
(Z)-2-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-N-hydroxyacetamide
Homo sapiens
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C
0.00734
(Z)-2-[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]-N-hydroxyacetamide
Homo sapiens
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C
0.00652
(Z)-2-[5-(4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
Homo sapiens
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C
0.0123
(Z)-5-[(3-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.0233
(Z)-5-[(3-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.003
(Z)-5-[(4-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.0174
(Z)-5-[(4-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.0083
(Z)-5-[(4-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.0042
(Z)-N-hydroxy-2-(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide
Homo sapiens
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C
0.0127
(Z)-N-hydroxy-2-[2,4-dioxo-5-(3-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
Homo sapiens
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C
0.00367
(Z)-N-hydroxy-2-[2,4-dioxo-5-(4-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
Homo sapiens
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C
0.00179
(Z)-N-hydroxy-2-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
Homo sapiens
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C
0.07764
([2-[(4-methoxy-1-methyl-1H-indazol-3-yl)amino]-2-oxoethyl]sulfanyl)acetic acid
Homo sapiens
-
0.0111
1'-(4-fluorobenzene-1-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
Homo sapiens
pH 6.2, 33°C
0.00375
1'-(5-chlorothiophene-2-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
Homo sapiens
pH 6.2, 33°C
0.0034
1,5-bis(3,4-dihydroxyphenyl)-1,4-pentadiene-3-one
Bos taurus
-
IC50: 0.0034 mM
0.0253
1,5-bis(4-hydroxy-3,5-dimethoxyphenyl)-1,4-pentadiene-3-one
Bos taurus
-
IC50: 0.0253 mM
0.0359
1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one
Bos taurus
-
IC50: 0.0359 mM
0.0331
1,5-bis(4-hydroxyphenyl)-1,4-pentadiene-3-one
Bos taurus
-
IC50: 0.0331 mM
0.00776
1-(4-fluorophenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
Homo sapiens
pH 6.2, 33°C
0.00253
1-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
Homo sapiens
pH 6.2, 33°C
0.00872
1-(4-methylphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
Homo sapiens
pH 6.2, 33°C
0.00478
1-(5-chlorothiophen-2-yl)-1,3-diazaspiro[4.5]decane-2,4-dione
Homo sapiens
pH 6.2, 33°C
0.00029
1-butyl-2-[[(4-oxo-3,4-dihydroquinazolin-2-yl)methyl]sulfanyl]-1H-benzimidazole-5-sulfonamide
Homo sapiens
pH 6.6, temperature not specified in the publication
0.008
1-O-Galloyl-beta-D-glucose
Homo sapiens
pH and temperature not specified in the publication
0.000242
1-[4-benzoyl-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]-2,2,2-trifluoroethan-1-one
Rattus norvegicus
-
pH 7.4, 37°C
0.012
17alpha-estradiol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.003
17beta-estradiol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.03561
2,1,3-benzoxadiazol-5-yl 5-chlorothiophene-2-sulfonate
Homo sapiens
-
0.5271
2,2'-[sulfonylbis(benzene-4,1-diyliminomethylylidene)]dipropanedinitrile
Homo sapiens
-
0.000064
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(3-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one
Rattus norvegicus
-
pH 7.4, 37°C
0.000073
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one
Rattus norvegicus
-
pH 7.4, 37°C
0.00074
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-phenoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one
Rattus norvegicus
-
pH 7.4, 37°C
0.000094
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methanesulfonyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one
Rattus norvegicus
-
pH 7.4, 37°C
0.000043
2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one
Rattus norvegicus
-
pH 7.4, 37°C
0.00014
2,2,2-trifluoro-1-[4-(3-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one
Rattus norvegicus
-
pH 7.4, 37°C
0.000078
2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one
Rattus norvegicus
-
pH 7.4, 37°C
0.0026
2,5-bis(3,4-dihydroxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0026 mM
0.0208
2,5-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0208 mM
0.0234
2,5-bis(4-hydroxy-3,5-dimethoxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0234 mM
0.0258
2,5-bis(4-hydroxy-3-methoxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0258 mM
0.0274
2,5-bis(4-hydroxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0274 mM
4.41
2,5-dihydro-3H-[1,2,4]triazino[5,6-b]indole-3-thione
Homo sapiens
pH and temperature not specified in the publication
0.0029
2,6-bis(3,4-dihydroxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.0029 mM
0.021
2,6-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.021 mM
0.0249
2,6-bis(4-hydroxy-3,5-dimethoxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.0249 mM
0.0264
2,6-bis(4-hydroxy-3-methoxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.0264 mM
0.0275
2,6-bis(4-hydroxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.0275 mM
0.000987
2-(2-oxo-3-((3,4,5-trifluorophenyl)amino)quinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0303
2-(3,4-dimethoxyphenyl)-ethanoic acid
Homo sapiens
-
IC50: 0.0303 mM
0.00213
2-(3,7-bis(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.001204
2-(3-((2,4-difluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.000124
2-(3-((4-bromo-2-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.00015
2-(3-((4-bromophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.000494
2-(3-((4-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0004
2-(3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000639
2-(3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000045
2-(3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0000463
2-(3-(4-bromo-2-fluorophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0000748
2-(3-(4-bromo-2-fluorophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0000356
2-(3-(4-bromo-2-fluorophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0000226
2-(3-(4-bromo-2-fluorophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0000273
2-(3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.00000243
2-(3-(4-bromophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0000493
2-(3-(4-bromophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.000033
2-(3-(4-bromophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0000114
2-(3-(4-bromophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.000296
2-(3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00027
2-(3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.0000328
2-(3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.00338
2-(3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
259
2-(3-(4-hydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.002
2-(3-benzoyl-1H-pyrrol-1-yl)acetic acid
Rattus norvegicus
-
pH 7.2, temperature not specified in the publication
0.000468
2-(3-phenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00598
2-(3-phenyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00042
2-(3-thiophenoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00116
2-(4-((E)-4-oxo-5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00006
2-(4-((E)-4-oxo-5-((1-phenyl-3-m-tolyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00064
2-(4-((E)-4-oxo-5-((1-phenyl-3-p-tolyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.0009
2-(4-((E)-5-((3-(3-bromophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00087
2-(4-((E)-5-((3-(3-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00004
2-(4-((E)-5-((3-(3-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00098
2-(4-((E)-5-((3-(3-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00008
2-(4-((E)-5-((3-(3-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00112
2-(4-((E)-5-((3-(4-bromophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido) acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00136
2-(4-((E)-5-((3-(4-chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00036
2-(4-((E)-5-((3-(4-fluorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.0011
2-(4-((E)-5-((3-(4-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00076
2-(4-((E)-5-((3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
37°C, pH not specified in the publication
0.00127
2-(4-((Z)-5-(2,3-dichlorobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido) acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.002
2-(4-((Z)-5-(2-bromobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.002
2-(4-((Z)-5-(2-chlorobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)aceticacid
Rattus norvegicus
-
pH 6.2, 37°C
0.00212
2-(4-((Z)-5-(2-fluorobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00148
2-(4-((Z)-5-(2-methoxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00236
2-(4-((Z)-5-(2-methylbenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00169
2-(4-((Z)-5-(2-nitrobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.0006
2-(4-((Z)-5-(3,4,5-trimethoxybenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido) acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00146
2-(4-((Z)-5-(3-bromobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00164
2-(4-((Z)-5-(3-chlorobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.0002
2-(4-((Z)-5-(3-fluorobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00118
2-(4-((Z)-5-(3-methoxybenzylidene)-4-oxo-2-thioxothiazolidin-3yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00162
2-(4-((Z)-5-(3-methylbenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00161
2-(4-((Z)-5-(3-nitrobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.0015
2-(4-((Z)-5-(4-bromobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.0018
2-(4-((Z)-5-(4-chlorobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00187
2-(4-((Z)-5-(4-fluorobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00234
2-(4-((Z)-5-(4-formylbenzylidene) 4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.0013
2-(4-((Z)-5-(4-methoxybenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00215
2-(4-((Z)-5-(4-methylbenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.0012
2-(4-((Z)-5-(4-nitrobenzylidene)4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.0016
2-(4-((Z)-5-benzylidene-4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.00152
2-(4-(4-oxo-2-thioxothiazolidin-3-yl)benzamido)acetic acid
Rattus norvegicus
-
pH 6.2, 37°C
0.0185
2-(4-hydroxy-3-methoxyphenyl)ethanoic acid
Homo sapiens
-
derived from ginger rhizom, Zingiber officinale, IC50: 0.0185 mM, suppresses nt only sorbitol accumulation in human erythrocytes
0.0192
2-(4-hydroxy-3-methoxyphenyl)ethanol
Homo sapiens
-
derived from ginger rhizom, Zingiber officinale, IC50: 0.0192 mM, suppresses sorbitol accumulation in human erythrocytes
0.000139
2-(6-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.0000382
2-(6-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.00000163
2-(6-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.000319
2-(6-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00000431
2-(6-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.000095
2-(6-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00000504
2-(6-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.00006
2-(6-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00007
2-(6-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.00334
2-(7-(4-fluorobenzyl)-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000091
2-(7-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000368
2-(7-bromo-3-(3-indolyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.0000047
2-(7-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0000435
2-(7-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.000467
2-(7-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000395
2-(7-bromo-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.0000063
2-(7-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.000069
2-(7-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000238
2-(7-chloro-3-(2-benzothiophene)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000326
2-(7-chloro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000158
2-(7-chloro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.0000423
2-(7-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.00152
2-(7-chloro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000032
2-(7-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00019
2-(7-fluoro-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000056
2-(7-fluoro-3-(4-chlorothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.0000191
2-(7-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.00087
2-(7-fluoro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.0265
2-amino-4-oxo-3,4-dihydropteridine-7-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.068 - 0.1
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
0.00014
2-carboxymethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
Rattus norvegicus
IC50: 140 nM, binding structure analysis
0.00055
2-carboxymethyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid carboxymethyl ester
Rattus norvegicus
IC50: 550 nM, binding structure analysis
0.088
2-methyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
Rattus norvegicus
IC50: 0.088 mM
0.00086
2-oxo-3-(3,4,5-trihydroxyphenoxy)-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00757
2-oxo-3-(3,4,5-trimethoxyphenoxy)-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00857
2-oxo-3-phenoxy-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0251
2-[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino]-4-phenylbutanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.0012
2-[(4-fluorobenzyl)[(2-fluorophenyl)sulfonyl]amino]-N-[2-(3-fluorophenyl)ethyl]acetamide
Homo sapiens
pH 6.6, temperature not specified in the publication
0.000139
2-[[5-(carboxymethyl)-3-oxo-3,5-dihydro-2H-[1,2,4]triazino[5,6-b]indol-2-yl]methyl]benzoic acid
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.00162
3'-(4-fluorobenzene-1-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
Homo sapiens
pH 6.2, 33°C
0.00491
3'-(5-chlorothiophene-2-sulfonyl)spiro[fluorene-9,4'-imidazolidine]-2',5'-dione
Homo sapiens
pH 6.2, 33°C
0.0318
3,3-Tetramethyleneglutaric acid
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.4812
3,4-dinitro-2,5-bis(phenylsulfanyl)thiophene
Homo sapiens
-
0.0049
3,5-bis(3,4-dihydroxybenzylidene)-4-piperidone
Bos taurus
-
IC50: 0.0049 mM
0.0208
3,5-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)-4-piperidone
Bos taurus
-
IC50: 0.0208 mM
0.0223
3,5-bis(4-hydroxy-3,5-dimethoxybenzylidene)-4-piperidone
Bos taurus
-
IC50: 0.0223 mM
0.0299
3,5-bis(4-hydroxy-3-methoxybenzylidene)-4-piperidone
Bos taurus
-
IC50: 0.0299 mM
0.0311
3,5-bis(4-hydroxyphenyl)-4-piperidone
Bos taurus
-
IC50: 0.0311 mM
0.127
3,5-dichlorosalicylic acid
Homo sapiens
ALR2 in 50 mM potassium phosphate (pH 6.2)
53.54
3-(1H-indol-1-yl)propanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.0285 - 0.0765
3-(2,4-dihydroxyphenyl)-5-hydroxy-7-methoxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
0.022
3-(2-phenylthiazole-4-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.00031
3-(3,4-dihydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00568
3-(3,4-dimethoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00236
3-(3,5-dihydroxy-4-methoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000087
3-(3,5-dihydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0043
3-(3,5-dimethoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0097
3-(3-benzoyl-1H-pyrrol-1-yl)propanoic acid
Rattus norvegicus
-
pH 7.2, temperature not specified in the publication
0.00453
3-(3-hydroxy-4,5-dimethoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0025
3-(3-hydroxy-4-methoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00285
3-(3-hydroxy-5-methoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00768
3-(4-fluorophenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
Homo sapiens
pH 6.2, 33°C
0.283
3-(4-hydroxy-3-methoxyphenyl)propanol
Homo sapiens
-
IC50: 0.283 mM
0.00012
3-(4-hydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00268
3-(4-methoxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00831
3-(4-methoxyphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
Homo sapiens
pH 6.2, 33°C
0.00353
3-(4-methylphenyl)-1,3-diazaspiro[4.5]decane-2,4-dione
Homo sapiens
pH 6.2, 33°C
0.1073
3-(4-nitrophenyl)-2-[(phenylsulfonyl)amino]propanoic acid
Homo sapiens
-
0.0019 - 0.014
3-(5-(3-(trifluormethyl)phenyl)thiophene-2-yl)propanoic acid
0.003
3-(5-(3-acetylphenyl)furan-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.016
3-(5-(3-aminophenyl)furan-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0068
3-(5-(3-methoxyphenyl)furan-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0054
3-(5-(3-methoxyphenyl)thiophene-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0057
3-(5-(3-methylphenyl)furan-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0049
3-(5-(3-methylphenyl)thiophene-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.004
3-(5-(3-methylsulfonyl)phenylfuran-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.00026
3-(5-(3-nitrophenyl)furan-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.00017
3-(5-(3-nitrophenyl)thiophene-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.002
3-(5-(3-trifluormethyl)phenylfuran-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.00047
3-(5-chlorothiophen-2-yl)-1,3-diazaspiro[4.5]decane-2,4-dione
Homo sapiens
pH 6.2, 33°C
0.016
3-(5-phenylfuran-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0053
3-(5-phenylthiophene-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.031
3-(5-pyridine-2-yl-furan-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.019
3-(5-pyridine-3-yl-furan-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.03108
3-benzyl-1-methyl-2-oxo-1,2-dihydroquinolin-4-yl 4-methylbenzenesulfonate
Homo sapiens
-
0.062 - 0.172
3-hydroxycoumarin
0.0006
3-O-caffeoylquinic acid
Rattus norvegicus
-
pH 7.0, 25°C
0.0995 - 0.2808
3-[3,4-dihydroxy-5-(3-methylbut-2-en-1-yl)phenyl]-5,7-dihydroxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
19.85
3-[3-[(diethylamino)methyl]-1H-indol-1-yl]propanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.0288
30-norhederagenin
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.006
4-(3-benzoyl-1H-pyrrol-1-yl)butanoic acid
Rattus norvegicus
-
pH 7.2, temperature not specified in the publication
0.197
4-(4-hydroxy-3-methoxyphenyl)-2-butanone
Homo sapiens
-
IC50: 0.197 mM
0.642
4-(4-hydroxy-3-methoxyphenyl)butanol
Homo sapiens
-
IC50: 0.642 mM
0.0031
4-(5-(3-methylphenyl)thiophene-2-yl)butanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0064
4-(5-phenylthiophene-2-yl)butanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0016
4-androsten-17beta-ol-3-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0005
4-androstene-3,17-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.273
4-hydroxy-3-methoxyphenol
Homo sapiens
-
IC50: 0.273 mM
0.0244
4-hydroxy-3-methoxyphenyl methanol
Homo sapiens
-
IC50: 0.0244 mM
0.045 - 0.4
4-Hydroxycoumarin
0.0362
4-O-butylpaeoniflorin
Rattus norvegicus
-
in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.0041
4-oxo-4-(5-(3-methylphenyl)thiophene-2-yl)butanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0065
4-oxo-4-(5-phenylthiophen-2-yl)butanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.0025
4-pregenene-21-ol-3,20-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.017
4-pregnene-11beta,17alpha,21-triol-3,20-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.005
4-pregnene-11beta,21-diol-3,20-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0022
4-pregnene-17alpha,21-diol-3,11,20-trione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.022
4-pregnene-18-al-11beta,21-diol-3,20-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0255
4-[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino]butanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.00119 - 0.00392
4-[3-(5-oxo-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-6-yl)-1,2,4-oxadiazol-5-yl]butanoic acid
0.0624 - 0.1762
4-[5,7-dimethoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
0.0042
4-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]-2-butenoic acid
Bos taurus
-
IC50: 0.0042 mM
0.0427 - 0.1306
4-[7-hydroxy-5-methoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
0.0202
5-(3-aminobenzylidene)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0202 mM
0.0107
5-(3-hydroxybenzylidene)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0107 mM
0.0789
5-(3-phenoxybenzyl)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0789 mM
0.0314
5-(4-benzyloxybenzyl)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0314 mM
0.009
5-(4-hydroxybenzylidene)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.009 mM
0.0404
5-(4-phenoxybenzyl)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0404 mM
0.0011
5-androsten-3beta-ol-17-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0658
5-biphenyl-4-ylmethyl-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0658 mM
0.00023
5-cholenic acid-3beta-ol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.05
5-hydroxy-3S-hydroxymethyl-6-methyl-2,3-dihydrobenzofuran
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.0107
5-naphthalen-1-ylmethylene-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0107 mM
0.0853
5-oxo-3-phenyl-5-(quinolin-2-ylamino)pentanoic acid
Homo sapiens
-
0.0117
5-[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino]pentanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000643
5-[(4-oxo-2-phenyl-4H-chromen-6-yl)methyl]-1,3-thiazolidine-2,4-dione
Rattus norvegicus
-
pH 6.2, 37°C
0.000955
5-[(6-isopropyl-4-oxo-4H-chromen-3-yl)methylene]thiazolidine-2,4-dione
Rattus norvegicus
-
pH 6.2, 37°C
0.000944
5-[(6-methyl-4-oxo-4H-chromen-3-yl)methylene]thiazolidine-2,4-dione
Rattus norvegicus
-
pH 6.2, 37°C
0.000687
5-[3-(4-oxo-4H-chromen-2-yl)benzyl]-1,3-thiazolidine-2,4-dione
Rattus norvegicus
-
pH 6.2, 37°C
0.000432
5-[4-(4-oxo-4H-chromen-2-yl)benzyl]-1,3-thiazolidine-2,4-dione
Rattus norvegicus
-
pH 6.2, 37°C
0.0057
5alpha-Androstan-17alpha-ol-3-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00051
5alpha-androstan-17beta-ol-3-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0027
5alpha-Androstan-3alpha-ol-17-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00032
5alpha-Androstan-3beta-ol-17-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00039
5alpha-androstane-3,17-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0046
5alpha-androstane-3alpha,17beta-diol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00052
5alpha-Androstane-3beta,17beta-diol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.000064
5alpha-cholanic acid-3beta-ol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0005
5alpha-pregnan-3beta-ol-20-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00037
5alpha-pregnane-21-ol-3,20-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00044
5alpha-pregnane-3,20-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0042
5beta-androstan-17beta-ol-3-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0048
5beta-Androstan-3alpha-ol-17-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00033
5beta-androstan-3beta-ol-17-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0021
5beta-androstane-3,17-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0016
5beta-androstane-3beta,17beta-diol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.04
5beta-cholan-24-ol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.000052
5beta-cholanic acid
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.018
5beta-cholanic acid methyl ester
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00011
5beta-cholanic acid-3-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00021
5beta-cholanic acid-3alpha,12alpha-diol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00026
5beta-cholanic acid-3alpha,6alpha-diol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0022
5beta-cholanic acid-3alpha,7alpha,12alpha-triol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0011
5beta-cholanic acid-3alpha,7alpha-diol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00078
5beta-cholanic acid-3alpha,7beta-diol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00012
5beta-cholanic acid-3alpha-ol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.000027
5beta-cholanic acid-3beta-ol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00055
5beta-Pregnan-3alpha-ol-20-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00044
5beta-Pregnan-3beta-ol-20-one
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00078
5beta-pregnane-3,20-dione
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.038 - 0.064
6,7-dihydroxy-4-methylcoumarin
0.0096 - 0.066
6,7-dihydroxy-4-phenylcoumarin
0.0365 - 0.067
6,7-dihydroxycoumarin
0.000055
6-(2,3-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 55 nM
0.000035
6-(2,3-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 35 nM
0.00039
6-(2,3-difluorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 390 nM
0.000257
6-(2,3-difluorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 257 nM
0.00019
6-(2,4-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 190 nM
0.00087
6-(2,4-difluorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 870 nM
0.000073
6-(2,5-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 73 nM
0.00005
6-(2,6-dichlorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 50 nM
0.000052
6-(2,6-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 52 nM
0.00021
6-(2-bromobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 210 nM
0.00028
6-(2-chloro-4-fluorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 280 nM
0.000026
6-(2-chloro-6-fluorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 26 nM
0.00017
6-(2-chlorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 170 nM
0.000118
6-(2-chlorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 118 nM
0.000054
6-(2-fluoro-3-chlorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 54 nM
0.000044
6-(2-fluoro-3-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 44 nM
0.000667
6-(2-fluoro-4-bromophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 667 nM
0.00054
6-(2-fluorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 540 nM
0.000422
6-(2-fluorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 422 nM
0.0005
6-(2-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 500 nM
0.000013
6-(3,5-dimethylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 13 nM
0.00024
6-(3-chlorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 240 nM
0.00014
6-(3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 140 nM
0.000023
6-(3-phenylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 23 nM
0.000175
6-(3-trifluoromethylbenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 175 nM
0.000072
6-(3-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 72 nM
0.000049
6-(3-[4-fluorophenyl]benzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 49 nM
0.00014
6-(4-bromo-2-fluorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 140 nM
0.00035
6-(4-bromobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 350 nM
0.00038
6-(4-chlorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 380 nM
0.000474
6-(4-fluorobenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 474 nM
0.002
6-(4-methoxybenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 0.002 mM
0.00036
6-(4-trifluoromethylbenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 360 nM
0.0038
6-(5,6-methylenedioxyindole-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 0.0038 mM
0.000087
6-(5,7-dichlorobenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 87 nM
0.0002
6-(5,7-dichloroindole-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 200 nM
0.000006
6-(5-chloro-3-ethylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 6 nM
0.000092
6-(5-chloro-3-isopropylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 92 nM
0.001
6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 0.001 mM
0.000055
6-(5-chloro-3-methylbenzothiophene-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 55 nM
0.000034
6-(5-chloro-3-phenylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 34 nM
0.000025
6-(5-chlorobenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 25 nM
0.0011
6-(5-chloroindole-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 0.0011 mM
0.000003
6-(5-fluoro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 3 nM
0.00023
6-(5-methoxybenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 230 nM
0.00016
6-(5-methylbenzothiophene-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 160 nM
0.000005
6-(5-trifluoromethyl-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 5 nM
0.00019
6-(6-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 190 nM
0.000645
6-(6-chloroindole-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 645 nM
0.0014
6-(6-fluoroindole-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 0.0014 mM
0.00045
6-(7-chloroindole-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 450 nM
0.00015
6-(alpha-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 150 nM
0.00015
6-(benzofuran-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 150 nM
0.00045
6-(benzothiazole-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 450 nM
0.00018
6-(benzothiophene-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 180 nM
0.00036
6-(beta-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 360 nM
0.0022
6-(biphenyl-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 0.0022 mM
0.00059
6-(indole-2-sulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 590 nM
0.000056
6-bromo-3-(3,5-dihydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000023
6-chloro-3-(3,5-dihydroxyphenoxy)-2-oxo-1,8-naphthyridine-1(2H)-carboxylic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.056 - 0.101
6-hydroxy-7-methoxycoumarin
0.156 - 0.171
6-hydroxycoumarin
0.05
6-methoxypaeoniflorigenone
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.00402
6-[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino]hexanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.0245 - 0.09
7-hydroxy-4-methylcoumarin
0.0024 - 0.037
7-hydroxy-4-phenylcoumarin
0.046 - 0.074
7-hydroxy-6-methoxycoumarin
0.023 - 0.086
7-hydroxycoumarin
0.053 - 0.063
7-hydroxylcoumarin-4-acetic acid
0.021 - 0.142
7-hydroxylcoumarinyl-4-acetic acid
0.0675 - 0.131
7-methoxycoumarin
0.00079 - 0.0038
8-lavandulylkaempferol
0.001
8-methoxy-N-[(1S)-2-methyl-1-(5-phenyl-1H-imidazol-2-yl)propyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000731
8-methoxy-N-[(5-phenyl-1H-imidazol-2-yl)methyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000899
8-methoxy-N-[[5-(4-methoxyphenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.05
8-O-benzoylpaeonidanin
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.000055
8-phenylsulfonylphthalazin-2H-3-one
Rattus norvegicus
-
IC50: 55 nM
0.05
alpha-benzoyloxypaeoniflorin
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.05
apiopaeonoside
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.0008
benzbromarone
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.05
benzoylpaeoniflorin
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.05
beta-benzoyloxypaeoniflorin
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.003
bezafibrate
Homo sapiens
-
noncompetitive, IC50: 0.003 mM, recombinant enzyme
0.0137
bisdemethoxycurcumin
Bos taurus
-
i.e. 1,7-bis(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0137 mM
0.0007
butein
Homo sapiens
-
in 0.1 M sodium phosphate buffer (pH 6.2)
0.00086
ciprofibrate
Homo sapiens
-
competitive, IC50: 0.00086 mM, recombinant enzyme
0.0012
Clofibric acid
Homo sapiens
-
noncompetitive, IC50: 0.0012 mM, recombinant enzyme
0.1184 - 0.1873
coptisine
0.01
daidzein
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.0159
demethoxycurcumin
Bos taurus
-
i.e. 1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0159 mM
0.00045 - 0.00095
desmethylanhydroicaritin
0.022
diadzin
Capra hircus
-
pH 6.4, 24°C
0.00000143 - 0.094
epalrestat
0.1 - 0.1681
epiberberine
0.025
estriol
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.0016
estrone
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00056
fenofibrate
Homo sapiens
-
competitive, IC50: 0.00056 mM, recombinant enzyme
0.000026 - 0.033
fidarestat
0.0525
folic acid
Homo sapiens
pH and temperature not specified in the publication
0.038
formononetin
Capra hircus
-
pH 6.4, 24°C
0.0446
galloylpaeoniflorin
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.0065
gemfibrozil
Homo sapiens
-
noncompetitive, IC50: 0.0065 mM, recombinant enzyme
0.0071
glycochenodeoxycholic acid
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.00071
glycolithocholic acid
Homo sapiens
in 0.1 M potassium phosphate, pH 7.4, at 25°C
0.1401 - 0.1542
groenlandicine
0.0032
Hexestrol
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.00928
indomethacin
Homo sapiens
pH 6.2, temperature not specified in the publication, ALR2
0.0034 - 0.0275
isoliquiritigenin
0.00027
kuraridin
Homo sapiens
-
-
0.00213
kurarinol
Rattus norvegicus
-
-
0.00299
kurarinone
Rattus norvegicus
-
-
0.00085 - 0.00774
kushenol E
0.000005 - 0.027
lidorestat
0.002 - 0.0219
liquiritigenin
0.0006
lukianol B
Homo sapiens
-
IC50: 0.0006 mM
0.00126
methyl 3-methyl-2-([2-nitro-4-(trifluoromethyl)phenyl]amino)butanoate
Homo sapiens
pH 6.6, temperature not specified in the publication
0.00028 - 0.0006
minalrestat
0.0068
myricetin
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.0175
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-beta-alanine
Homo sapiens
pH and temperature not specified in the publication
0.0124
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-alanine
Homo sapiens
pH and temperature not specified in the publication
0.069
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-isoleucine
Homo sapiens
pH and temperature not specified in the publication
0.0617
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-leucine
Homo sapiens
pH and temperature not specified in the publication
0.046
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-phenylalanine
Homo sapiens
pH and temperature not specified in the publication
0.0292
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-serine
Homo sapiens
pH and temperature not specified in the publication
0.216
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-tyrosine
Homo sapiens
pH and temperature not specified in the publication
0.0834
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)-L-valine
Homo sapiens
pH and temperature not specified in the publication
0.00197
N-(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)glycine
Homo sapiens
pH and temperature not specified in the publication
0.0055 - 0.0659
N-(2-phenylethyl)-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
0.0011 - 0.0104
N-(2-phenylethyl)-N-[(3-nitrophenyl)sulfonyl]glycine
0.0036
N-(2-phenylethyl)-N-[(4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0454
N-(2-phenylethyl)-N-[(4-chlorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0471 - 0.0745
N-(2-phenylethyl)-N-[(4-fluorophenyl)sulfonyl]glycine
0.0847
N-(2-phenylethyl)-N-[(4-methylphenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.021
N-(2-phenylethyl)-N-[(4-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0683
N-(2-phenylethyl)-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.018 - 0.0804
N-benzyl-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
0.0065 - 0.0083
N-benzyl-N-[(2-naphthalenyl)sulfonyl]glycine
0.0055 - 0.0881
N-benzyl-N-[(3-nitrophenyl)sulfonyl]glycine
0.0704
N-benzyl-N-[(4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0234
N-benzyl-N-[(4-chlorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.029 - 0.0339
N-benzyl-N-[(4-fluorophenyl)sulfonyl]glycine
0.0248
N-benzyl-N-[(4-methylphenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0173
N-benzyl-N-[(4-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0747
N-benzyl-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.00367
N-cyclopropyl-N-[cyclopropyl(5-phenyl-1H-imidazol-2-yl)methyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.003072
N-cyclopropyl-N-[cyclopropyl(5-phenyl-1H-imidazol-2-yl)methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000222
N-cyclopropyl-N-[cyclopropyl[5-(pyridin-3-yl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000146
N-cyclopropyl-N-[cyclopropyl[5-(pyridin-3-yl)-1H-imidazol-2-yl]methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.009
N-galloyl beta-D-glucopyranosylamine
Homo sapiens
pH and temperature not specified in the publication
0.001
N-tert-butyl-2-(2-chloro-6-methoxy-4-([(3-methyl-5-sulfanyl-4H-1,2,4-triazol-4-yl)amino]methyl)phenoxy)acetamide
Homo sapiens
pH 6.6, temperature not specified in the publication
0.00022
N-[(1S)-1-[5-(4-bromophenyl)-1H-imidazol-2-yl]-2-methylpropyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000771
N-[(1S)-1-[5-(4-bromophenyl)-1H-imidazol-2-yl]-2-methylpropyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.00429
N-[(1S)-2-methyl-1-(5-phenyl-1H-imidazol-2-yl)propyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.002122
N-[(5-phenyl-1H-imidazol-2-yl)methyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.0012 - 0.0265
N-[2-(2-thienyl)ethyl]-N-[(1,10-biphenyl)-4-sulfonyl]glycine
0.0124 - 0.0147
N-[2-(2-thienyl)ethyl]-N-[(1-naphthalenyl)sulfonyl]glycine
0.0022 - 0.0576
N-[2-(2-thienyl)ethyl]-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
0.00427 - 0.0059
N-[2-(2-thienyl)ethyl]-N-[(2-naphthalenyl)sulfonyl]glycine
0.000431 - 0.0076
N-[2-(2-thienyl)ethyl]-N-[(3-nitrophenyl)sulfonyl]glycine
0.0046 - 0.0578
N-[2-(2-thienyl)ethyl]-N-[(4-bromophenyl)sulfonyl]glycine
0.0224
N-[2-(2-thienyl)ethyl]-N-[(4-chlorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0108 - 0.0612
N-[2-(2-thienyl)ethyl]-N-[(4-fluorophenyl)sulfonyl]glycine
0.0119 - 0.0847
N-[2-(2-thienyl)ethyl]-N-[(4-nitrophenyl)sulfonyl]glycine
0.0525 - 0.0732
N-[2-(2-thienyl)ethyl]-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
0.0133
N-[2-(2-thienyl)ethyl]-N-[(5-dimethylamino-1 naphthalenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.016
N-[2-(2-thienyl)ethyl]-N-[(5-dimethylamino-1-naphthalenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.000732
N-[[5-(4-bromophenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000091
N-[[5-(4-bromophenyl)-1H-imidazol-2-yl]methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000337
N-[[5-(4-chlorophenyl)-1H-imidazol-2-yl](cyclopropyl)methyl]-N-cyclopropyl-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000031
N-[[5-(4-chlorophenyl)-1H-imidazol-2-yl](cyclopropyl)methyl]-N-cyclopropyl-8-methoxy-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000114
N-[[5-(4-chlorophenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000065
N-[[5-(4-chlorophenyl)-1H-imidazol-2-yl]methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.00042
N-[[5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000071
N-[[5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl]-8-methoxy-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.000275
N-[[5-(4-methoxyphenyl)-1H-imidazol-2-yl]methyl]-2H-1-benzopyran-3-carboxamide
Homo sapiens
pH 6.2, 30°C
0.0241
N2-(2-methylaminobenzoyl)tetrahydro-1H-pyrido[3,4-b]indol-1-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0026
naringenin
Homo sapiens
pH 6.2, 25°C
0.00822
nitazoxanide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.05
nudanpinoside H
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.05
oxypaeoniflorin
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.05
paeoniflorigenone
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.05
paeoniflorin
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.05
paeonol
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.05
paeonolide
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.05
paeonoside
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.0114
palbinone
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.16
piplartine
Homo sapiens
-
pH 7.4, 37°C
0.00008
ponalrestat
Bos taurus
-
IC50: 80 nM
0.0223
puerariafuran
Rattus norvegicus
-
pH 7.0, 37°C
0.0387
pyrazolo[5,1-c][1,2,4]benzotriazin-8-yl dimethylcarbamate
Homo sapiens
-
0.0025 - 0.0376
quercetin
0.00056
quercitrin
Rattus norvegicus
-
pH 7.0, 25°C
0.01
rutin
Capra hircus
-
pH 6.4, 24°C
0.0188
S12728
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0018 - 0.0106
semilicoisoflavone B
0.012
silibinin
Capra hircus
-
pH 6.4, 24°C
0.016
silymarin
Capra hircus
-
pH 6.4, 24°C
0.0013
sulfuretin
Homo sapiens
-
in 0.1 M sodium phosphate buffer (pH 6.2)
0.000374
sulindac
Homo sapiens
pH 6.2, temperature not specified in the publication, ALR2
0.000279
sulindac sulfide
Homo sapiens
pH 6.2, temperature not specified in the publication, ALR2
0.000367
sulindac sulfone
Homo sapiens
pH 6.2, temperature not specified in the publication, ALR2
0.0314
thienocinnolinone alkanoic acid derivatives
Bos taurus
-
i.e. 8-halogen-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid derivatives, synthesis and inhibitory potency, IC50 as low as 0.0314 mM, the length of the N2 alkanoic chain strongly influences the inhibitory activity, overview
-
0.00535
tizoxanide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00239
Tolmetin
Homo sapiens
pH 6.2, temperature not specified in the publication, ALR2
0.00026 - 0.0008
Tolrestat
0.0501 - 0.056
Valproic acid
0.025
zearalenone
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.000004 - 0.00006
zopolrestat
0.0426
[(2-amino-4-oxo-3,4-dihydropteridine-7-carbonyl)amino](phenyl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
3.46
[(5H-[1,2,4]triazino[5,6-b]indol-3-yl)sulfanyl]acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.001
[2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0010 mM
0.0028
[2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0028 mM
0.00082
[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.00082 mM
0.00014
[2-oxo-3-(2-phenylethyl)quinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00082
[2-oxo-3-[(Z)-2-phenylethenyl]quinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.000308
[2-oxo-8-[(E)-2-phenylethenyl]-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.000234
[2-[(2-carbamoylphenyl)methyl]-3-oxo-2,3-dihydro-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000076
[2-[(2-cyanophenyl)methyl]-3-oxo-2,3-dihydro-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
13.76
[3-(2,2-dimethylpropanoyl)-1H-indol-1-yl]acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.00018
[3-(2,4-dihydroxyphenyl)-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00087
[3-(2,5-dihydroxyphenyl)-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000007 - 0.1
[3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
30.14
[3-[(diethylamino)methyl]-1H-indol-1-yl]acetic acid
Homo sapiens
pH and temperature not specified in the publication
42.16
[3-[(dimethylamino)methyl]-2-methyl-1H-indol-1-yl]acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.00016
[3-[(E)-2-(3,4-dihydroxyphenyl)ethenyl]-6-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0001
[3-[(E)-2-(3,4-dihydroxyphenyl)ethenyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000419
[3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00019
[3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-6-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00021
[3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00018
[3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.0001
[3-[(E)-2-(4-hydroxyphenyl)ethenyl]-6-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00006
[3-[(E)-2-(4-hydroxyphenyl)ethenyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00418
[3-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus
pH 6.2, 30°C
34.52
[3-[(morpholin-4-yl)methyl]-1H-indol-1-yl]acetic acid
Homo sapiens
pH and temperature not specified in the publication
2.05
[3-[(propan-2-yl)sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
Homo sapiens
pH and temperature not specified in the publication
46.48
[3-[(pyrrolidin-1-yl)methyl]-1H-indol-1-yl]acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.00098
[3-[2-(4-hydroxy-3-methoxyphenyl)ethyl]-6-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00085
[3-[2-(4-hydroxy-3-methoxyphenyl)ethyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0008
[3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00051
[3-[2-(4-hydroxyphenyl)ethyl]-7-methoxy-2-oxoquinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.039
[5-(3-aminobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
Bos taurus
-
IC50: 0.039 mM
0.0002
[5-(3-carboxymethoxy-4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
Homo sapiens
ALR2, pH 6.7, temperature not specified in the publication
0.00066
[5-(3-hydroxy-4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
Homo sapiens
ALR2, pH 6.7, temperature not specified in the publication
0.00066
[5-(3-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.00066 mM
0.003
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0030 mM
0.0211
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
Bos taurus
-
IC50: 0.0211 mM
0.00049
[5-(3-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid
Bos taurus
-
IC50: 0.00049 mM
0.00028
[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.00028 mM
0.0002
[5-(4-bromophenyl)-3-methyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
Homo sapiens
pH 7.5, 25°C
0.00019
[5-(4-chlorophenyl)-1-oxo-3-propylpyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
Homo sapiens
pH 7.5, 25°C
0.00012
[5-(4-chlorophenyl)-3-ethyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
Homo sapiens
pH 7.5, 25°C
0.00041
[5-(4-chlorophenyl)-3-ethyl-9-fluoro-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
Homo sapiens
pH 7.5, 25°C
0.00021
[5-(4-chlorophenyl)-3-methyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
Homo sapiens
pH 7.5, 25°C
0.00035
[5-(4-chlorophenyl)-9-fluoro-3-methyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
Homo sapiens
pH 7.5, 25°C
0.0021
[5-(4-hydroxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0021 mM
0.00015
[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.00015 mM
0.0062
[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
Bos taurus
-
IC50: 0.0062 mM
0.0011
[5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0011 mM
0.0012
[5-(4-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid
Bos taurus
-
IC50: 0.0012 mM
0.000012 - 0.1012
[6-ethyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
0.0194
[6-hydroxy-3-(4-hydroxyphenoxy)pyrazin-2-yl](4-hydroxyphenyl)methanone
Homo sapiens
-
isolated from red ascidian Botryllus leachi, pyrazine derivative, IC50: 0.0194 mM
0.00027
[6-methoxy-2-oxo-3-(2,4,6-trihydroxyphenyl)quinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000008 - 0.1
[6-methyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
0.000153
[7-fluoro-3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00065
[7-fluoro-3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus
pH 6.2, 30°C
0.00017
[7-methoxy-2-oxo-3-(2,4,6-trihydroxyphenyl)quinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00092
[7-methoxy-2-oxo-3-[(E)-2-phenylethenyl]quinoxalin-1(2H)-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00105
[8-(4-formylphenyl)-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.000774
[8-(4-methoxyphenyl)-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.000167
[8-[(E)-2-(4-fluorophenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.000188
[8-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.000082
[8-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.000208
[8-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.00022
[8-[(E)-2-(4-methylphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.000262
[8-[(E)-2-(4-nitrophenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.00017
[8-[(E)-2-(4-tert-butylphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.000281
[8-[(E)-2-([1,1'-biphenyl]-4-yl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
Homo sapiens
30°C, pH 6.2
0.00026
[9-fluoro-5-(4-methoxyphenyl)-3-methyl-1-oxopyrimido[4,5-c]quinolin-2(1H)-yl]acetic acid
Homo sapiens
pH 7.5, 25°C
0.05887
[[(4-methylphenyl)sulfonyl](2-thiophen-2-ylethyl)amino]acetic acid
Homo sapiens
-
additional information
Euphorbia regis-jubae aqueous extract
-
0.0963
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
Rattus norvegicus
-
pH 7.0, 37°C
0.2572
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
Homo sapiens
-
pH 7.0, 37°C
0.068
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
Rattus norvegicus
IC50: 0.068 mM
0.1
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
Rattus norvegicus
IC50: 0.10 mM
0.0285
3-(2,4-dihydroxyphenyl)-5-hydroxy-7-methoxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
Rattus norvegicus
-
pH 7.0, 37°C
0.0765
3-(2,4-dihydroxyphenyl)-5-hydroxy-7-methoxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
Homo sapiens
-
pH 7.0, 37°C
0.0019
3-(5-(3-(trifluormethyl)phenyl)thiophene-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.014
3-(5-(3-(trifluormethyl)phenyl)thiophene-2-yl)propanoic acid
Homo sapiens
in sodium phosphate buffer (100 mM, pH 6.2)
0.062
3-hydroxycoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.172
3-hydroxycoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.0995
3-[3,4-dihydroxy-5-(3-methylbut-2-en-1-yl)phenyl]-5,7-dihydroxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
Rattus norvegicus
-
pH 7.0, 37°C
0.2808
3-[3,4-dihydroxy-5-(3-methylbut-2-en-1-yl)phenyl]-5,7-dihydroxy-6-(3-methylbut-2-en-1-yl)-4H-chromen-4-one
Homo sapiens
-
pH 7.0, 37°C
0.045
4-Hydroxycoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.4
4-Hydroxycoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.00119
4-[3-(5-oxo-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-6-yl)-1,2,4-oxadiazol-5-yl]butanoic acid
Homo sapiens
-
0.00392
4-[3-(5-oxo-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-6-yl)-1,2,4-oxadiazol-5-yl]butanoic acid
Homo sapiens
-
0.0624
4-[5,7-dimethoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
Rattus norvegicus
-
pH 7.0, 37°C
0.1762
4-[5,7-dimethoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
Homo sapiens
-
pH 7.0, 37°C
0.0427
4-[7-hydroxy-5-methoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
Rattus norvegicus
-
pH 7.0, 37°C
0.1306
4-[7-hydroxy-5-methoxy-6-(3-methylbut-2-en-1-yl)-2H-chromen-3-yl]benzene-1,3-diol
Homo sapiens
-
pH 7.0, 37°C
0.038
6,7-dihydroxy-4-methylcoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.064
6,7-dihydroxy-4-methylcoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.0096
6,7-dihydroxy-4-phenylcoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.066
6,7-dihydroxy-4-phenylcoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.0365
6,7-dihydroxycoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.067
6,7-dihydroxycoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.056
6-hydroxy-7-methoxycoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.101
6-hydroxy-7-methoxycoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.156
6-hydroxycoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.171
6-hydroxycoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.0245
7-hydroxy-4-methylcoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.09
7-hydroxy-4-methylcoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.0024
7-hydroxy-4-phenylcoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.037
7-hydroxy-4-phenylcoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.046
7-hydroxy-6-methoxycoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.074
7-hydroxy-6-methoxycoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.023
7-hydroxycoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.086
7-hydroxycoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.053
7-hydroxylcoumarin-4-acetic acid
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.063
7-hydroxylcoumarin-4-acetic acid
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.021
7-hydroxylcoumarinyl-4-acetic acid
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.142
7-hydroxylcoumarinyl-4-acetic acid
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.0675
7-methoxycoumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.131
7-methoxycoumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.00079
8-lavandulylkaempferol
Homo sapiens
-
-
0.0038
8-lavandulylkaempferol
Rattus norvegicus
-
-
0.0075
capsaicin
Rattus norvegicus
-
enzyme isolated from heart, pH 6.2, temperature not specified in the publication
0.367
capsaicin
Rattus norvegicus
-
enzyme isolated from kidney, pH 6.2, temperature not specified in the publication
0.734
capsaicin
Rattus norvegicus
-
enzyme isolated from liver, pH 6.2, temperature not specified in the publication
0.904
capsaicin
Rattus norvegicus
-
enzyme isolated from brain, pH 6.2, temperature not specified in the publication
0.1184
coptisine
Rattus norvegicus
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.1873
coptisine
Homo sapiens
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.4
coumarin
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.5
coumarin
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.0068
curcumin
Bos taurus
-
i.e. 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0068 mM
0.01
curcumin
Homo sapiens
pH 6.0, 30°C, ALR2
0.03
curcumin
Homo sapiens
pH 7.0, 37°C, AKR1B10
0.00045
desmethylanhydroicaritin
Homo sapiens
-
-
0.00095
desmethylanhydroicaritin
Rattus norvegicus
-
-
0.00000143
epalrestat
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.000045
epalrestat
Homo sapiens
pH 6.2, 30°C
0.0000665
epalrestat
Homo sapiens
pH and temperature not specified in the publication
0.000075
epalrestat
Rattus norvegicus
-
37°C, pH 7.0
0.000084
epalrestat
Rattus norvegicus
pH 6.2, 30°C
0.000089
epalrestat
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00009
epalrestat
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00011
epalrestat
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00011
epalrestat
Homo sapiens
pH 6.2, temperature not specified in the publication, ALR2
0.00028
epalrestat
Homo sapiens
-
-
0.0013
epalrestat
Homo sapiens
-
in 0.1 M sodium phosphate buffer (pH 6.2)
0.0014
epalrestat
Rattus norvegicus
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.0125
epalrestat
Rattus norvegicus
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.017
epalrestat
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.094
epalrestat
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.1
epiberberine
Rattus norvegicus
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.1681
epiberberine
Homo sapiens
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.000026
fidarestat
Homo sapiens
pH 7.0, 25°C, recombinant detagged enzyme
0.000035
fidarestat
Sus scrofa
-
2S4S-eantiomer, i.e. (2S,4S)-6-fluoro-2',5'-dioxospiro-[chroman-4,4'-imidazoline]-2-carboxamide, IC50: 35 nM, binding site structure, binding to the enzyme does not induce conformational changes in the C-loop region, mechanism, active site binding modelin
0.0018
fidarestat
Homo sapiens
pH 7.0, 25°C, recombinant detagged enzyme
0.0085
fidarestat
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.033
fidarestat
Homo sapiens
pH 7.0, 25°C, recombinant detagged wild-type enzyme
0.1401
groenlandicine
Rattus norvegicus
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.1542
groenlandicine
Homo sapiens
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.0034
isoliquiritigenin
Rattus norvegicus
-
pH 7.0, 37°C
0.0275
isoliquiritigenin
Homo sapiens
-
pH 7.0, 37°C
0.00085
kushenol E
Homo sapiens
-
-
0.00774
kushenol E
Rattus norvegicus
-
-
0.000005
lidorestat
Homo sapiens
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.027
lidorestat
Homo sapiens
-
ALR1, pH not specified in the publication, temperature not specified in the publication
0.002
liquiritigenin
Rattus norvegicus
-
pH 7.0, 37°C
0.0219
liquiritigenin
Homo sapiens
-
pH 7.0, 37°C
0.00028
minalrestat
Homo sapiens
ALR2 in 50 mM potassium phosphate (pH 6.2)
0.0006
minalrestat
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.0055
N-(2-phenylethyl)-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0659
N-(2-phenylethyl)-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0011
N-(2-phenylethyl)-N-[(3-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0104
N-(2-phenylethyl)-N-[(3-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0471
N-(2-phenylethyl)-N-[(4-fluorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0745
N-(2-phenylethyl)-N-[(4-fluorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.018
N-benzyl-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0804
N-benzyl-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0065
N-benzyl-N-[(2-naphthalenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0083
N-benzyl-N-[(2-naphthalenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0055
N-benzyl-N-[(3-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0881
N-benzyl-N-[(3-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.029
N-benzyl-N-[(4-fluorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0339
N-benzyl-N-[(4-fluorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0012
N-[2-(2-thienyl)ethyl]-N-[(1,10-biphenyl)-4-sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0265
N-[2-(2-thienyl)ethyl]-N-[(1,10-biphenyl)-4-sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0124
N-[2-(2-thienyl)ethyl]-N-[(1-naphthalenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0147
N-[2-(2-thienyl)ethyl]-N-[(1-naphthalenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0022
N-[2-(2-thienyl)ethyl]-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0576
N-[2-(2-thienyl)ethyl]-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.00427
N-[2-(2-thienyl)ethyl]-N-[(2-naphthalenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0059
N-[2-(2-thienyl)ethyl]-N-[(2-naphthalenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.000431
N-[2-(2-thienyl)ethyl]-N-[(3-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0076
N-[2-(2-thienyl)ethyl]-N-[(3-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0046
N-[2-(2-thienyl)ethyl]-N-[(4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0578
N-[2-(2-thienyl)ethyl]-N-[(4-bromophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0108
N-[2-(2-thienyl)ethyl]-N-[(4-fluorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0612
N-[2-(2-thienyl)ethyl]-N-[(4-fluorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0119
N-[2-(2-thienyl)ethyl]-N-[(4-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0847
N-[2-(2-thienyl)ethyl]-N-[(4-nitrophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0525
N-[2-(2-thienyl)ethyl]-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 7.2, 37°C, ALR1
0.0732
N-[2-(2-thienyl)ethyl]-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0025
quercetin
Rattus norvegicus
-
pH 7.0, 37°C
0.00254
quercetin
Homo sapiens
-
-
0.00592
quercetin
Homo sapiens
ALR2 in 50 mM potassium phosphate (pH 6.2)
0.00773
quercetin
Rattus norvegicus
-
-
0.0127
quercetin
Homo sapiens
-
pH 7.0, 37°C
0.0188
quercetin
Rattus norvegicus
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.027
quercetin
Homo sapiens
-
IC50: 0.027 mM
0.0376
quercetin
Bos taurus
-
IC50: 0.0376 mM
0.0018
semilicoisoflavone B
Rattus norvegicus
-
pH 7.0, 37°C
0.0106
semilicoisoflavone B
Homo sapiens
-
pH 6.2, 37°C
0.00014
sorbinil
Rattus norvegicus
-
IC50: 140 nM
0.00025
sorbinil
Rattus norvegicus
-
pH 7.2, temperature not specified in the publication
0.00025
sorbinil
Rattus norvegicus
-
isoform ALR2, pH 7.4, 37°C
0.0009
sorbinil
Sus scrofa
-
aldose reductase inhibitor, IC50: 900 nM
0.0011
sorbinil
Bos taurus
-
IC50: 0.0011 mM
0.00141
sorbinil
Homo sapiens
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C
0.002
sorbinil
Bos taurus
-
pH 6.8, 37°C
0.0021
sorbinil
Homo sapiens
-
competitive, IC50: 0.0021 mM, recombinant enzyme
0.0034
sorbinil
Bos taurus
-
IC50: 0.0034 mM
0.0036
sorbinil
Homo sapiens
-
orally active inhibitor, IC50: 0.0036 mM
0.03
sorbinil
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.00026
Tolrestat
Homo sapiens
ALR2 in 50 mM potassium phosphate (pH 6.2)
0.0008
Tolrestat
Rattus norvegicus
-
in 0.1 M potassium phosphate, pH 7.4
0.0501
Valproic acid
Rattus norvegicus
-
pH 7.2, temperature not specified in the publication
0.056
Valproic acid
Rattus norvegicus
-
isoform ALR1, pH 7.4, 37°C
0.000004
zopolrestat
Rattus norvegicus
-
IC50: 4 nM
0.00006
zopolrestat
Homo sapiens
-
competitive, IC50: 0.00006 mM, recombinant enzyme
0.000007
[3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
Homo sapiens
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.1
[3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
Homo sapiens
-
above, ALR1, pH not specified in the publication, temperature not specified in the publication
0.000012
[6-ethyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
Homo sapiens
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.1012
[6-ethyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
Homo sapiens
-
above, ALR1, pH not specified in the publication, temperature not specified in the publication
0.000008
[6-methyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
Homo sapiens
-
ALR2, pH not specified in the publication, temperature not specified in the publication
0.1
[6-methyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid
Homo sapiens
-
above, ALR1, pH not specified in the publication, temperature not specified in the publication
additional information
Euphorbia regis-jubae aqueous extract
Jaculus orientalis
-
IC50 value is 140 microg/ml
-
additional information
Euphorbia regis-jubae hydroethanolic extract
Jaculus orientalis
-
IC50 value is 96 microg/ml
-
additional information
additional information
Rattus norvegicus
-
D-mannitol IC50: above 0.1 mg/ml, 2,5-dihydrobenzoic acid IC50: 0.0359 mg/ml, delphinidin 3-O-beta-galactopyranoside-3',5'-di-O-beta-glucopyranoside IC50: 0.00123 mg/ml, delphinidin 3-O-beta-galactopyranoside IC50: 0.00023 mg/ml, methanolic and ethanolic extracts of Litchi chinensis fruits are potent inhibitors with IC50 values of 0.0036 and 0.0003 mg/ml, respectively
-
additional information
additional information
Homo sapiens
-
gallic acid IC50: 0.0973 mg/ml, p-coumaric acid IC50: 0.1623 mg/ml, syringic acid IC50: 0.1721 mg/ml, trans-cinnamic acid IC50: 0.0681 mg/ml, p-catechuic acid IC50: 0.0427 mg/ml, quercetin IC50: 0.02523 mg/ml (in 50 mM sodium potassium phosphate buffer (pH 6.0) containing 5 mM beta-mercaptoethanol, 0.7 M NADPH, 0.4 M Li2SO4, and 2.5 mM of DL-glyceraldehyde)
-
additional information
additional information
Rattus norvegicus
IC50 values and 95% confidence intervals of flavonoids from Litsea japonica on advanced glycation end products formation, IC50 values of 0.0074-0.072 mM, overview
-
additional information
additional information
Bos taurus
inhibition kinetics and thermodynamics, overview
-
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