Information on EC 1.1.1.21 - aldehyde reductase and Organism(s) Rattus norvegicus and UniProt Accession P07943

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Rattus norvegicus
UNIPROT: P07943
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The expected taxonomic range for this enzyme is: Eukaryota, Bacteria


The taxonomic range for the selected organisms is: Rattus norvegicus

EC NUMBER
COMMENTARY hide
1.1.1.21
-
RECOMMENDED NAME
GeneOntology No.
aldehyde reductase
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
oxidation
-
-
-
-
reduction
-
-
-
-
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
D-galactose degradation IV
-
-
D-xylose degradation II
-
-
L-arabinose degradation II
-
-
lipid A biosynthesis
-
-
Pentose and glucuronate interconversions
-
-
Fructose and mannose metabolism
-
-
Galactose metabolism
-
-
Glycerolipid metabolism
-
-
Folate biosynthesis
-
-
Metabolic pathways
-
-
SYSTEMATIC NAME
IUBMB Comments
alditol:NAD(P)+ 1-oxidoreductase
Has wide specificity.
CAS REGISTRY NUMBER
COMMENTARY hide
9028-31-3
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
-
aldose reductase (ALR2) is a member of aldo-keto reductase superfamily
malfunction
-
inhibition of the enzyme causes advanced glycation end products formation
metabolism
-
ALR2 is the first rate-determining enzyme in the polyol pathway and catalyzes the reduction of glucose to sorbitol in the presence of NADPH as a cofactor. Sorbitol is in turn converted into fructose with accompanied reduction of NAD+ by sorbitol dehydrogenase. Under normal circumstances, glucose is predominantly converted to glucose-6-phosphate by hexokinase and then enters the glycolytic pathway, whereas only a small amount of glucose is metabolized through the polyol pathway due to a relatively low affinity of ALR2 for this substrate. During hyperglycemia, the polyol metabolic pathway is activated and the increased flux of glucose through the polyol pathway triggers the accumulation of sorbitol, which mainly happens in tissues demonstrating insulin-independent uptake of glucose, such as lens, kidney, retina, and peripheral nerves
metabolism
physiological function
additional information
-
inhibition of the enzyme prevents 4-hydroxy-trans-2-nonenal-and glutathione-4-hydroxy-trans-2-nonenal-induced E2F-1 expression
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
D-glucose + NADPH + H+
sorbitol + NADP+
show the reaction diagram
-
-
-
-
?
D-glyceraldehyde + NADPH + H+
glycerol + NADP+
show the reaction diagram
-
-
-
r
DL-glyceraldehyde + NADPH + H+
glycerol + NADP+
show the reaction diagram
-
-
-
-
?
(1S)-camphorquinone + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
(S)-1-indanol + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
(S)-1-tetralol + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
1-butanal + NADPH + H+
1-butanol + NADP+
show the reaction diagram
-
-
-
-
?
1-decanal + NADPH + H+
1-decanol + NADP+
show the reaction diagram
-
-
-
-
?
1-hexanal + NADPH + H+
1-hexanol + NADP+
show the reaction diagram
-
-
-
-
?
1-nonanal + NADPH + H+
1-nonanol + NADP+
show the reaction diagram
-
-
-
-
?
1-propanal + NADPH + H+
1-propanol + NADP+
show the reaction diagram
-
-
-
-
?
16-ketoestrone + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2,3-butanedione + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2,3-heptanedione + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2,3-hexanedione + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2,3-pentanedione + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2,4-decadienal + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2,4-nonadienal + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2-decenal + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2-hexenal + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2-nonenal + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
2-phenyl-2-propenal + NADPH + H+
2-phenyl-1-propanol + NADP+
show the reaction diagram
-
-
-
-
?
21-dehydrocortisol + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
3,4-hexanedione + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
3-deoxyglucosone + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
4-hydroxy-trans-2-nonenal + NADPH + H+
1,4-dihydroxynonane + NADP+
show the reaction diagram
-
-
-
-
?
4-hydroxynonenal + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
4-nitrobenzaldehyde + NADPH + H+
4-nitrobenzyl alcohol + NADP+
show the reaction diagram
-
-
-
-
?
acrolein + NADPH + H+
2-propen-1-ol + NADP+
show the reaction diagram
-
-
-
-
?
alditol + NAD(P)+
aldose + NAD(P)H
show the reaction diagram
-
-
-
-
r
aldose + NAD(P)H
alditol + NAD(P)+
show the reaction diagram
-
-
-
-
r
aldose + NADPH + H+
alditol + NADP+
show the reaction diagram
benzaldehyde + NADPH + H+
benzyl alcohol + NADP+
show the reaction diagram
-
-
-
-
?
D-galactose + NAD(P)H
dulcitol + NAD(P)+
show the reaction diagram
-
-
-
-
r
D-glucose + NAD(P)H
sorbitol + NAD(P)+
show the reaction diagram
-
-
-
-
r
D-glucose + NADPH + H+
D-sorbitol + NADP+
show the reaction diagram
-
-
-
-
?
D-glucose + NADPH + H+
sorbitol + NADP+
show the reaction diagram
D-glucuronate + NAD(P)H
?
show the reaction diagram
-
-
-
-
r
D-glucuronate + NADPH
?
show the reaction diagram
-
-
-
-
?
D-glucuronate + NADPH
? + NADP+
show the reaction diagram
-
substrate of aldehyde reductase ALR1
-
-
?
D-glyceraldehyde + NAD(P)H
glycerol + NAD(P)+
show the reaction diagram
-
-
-
-
?
D-lactoaldehyde + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
D-xylose + NAD(P)H
xylitol + NAD(P)+
show the reaction diagram
-
-
-
-
r
D-xylose + NADPH
?
show the reaction diagram
-
-
-
-
?
DL-glyceraldehyde + NAD(P)H
glycerol + NAD(P)+
show the reaction diagram
-
-
-
-
r
DL-glyceraldehyde + NADPH
glycerol + NADP+
show the reaction diagram
DL-glyceraldehyde + NADPH + H+
DL-glycerol + NADP+
show the reaction diagram
-
-
-
-
?
DL-glyceraldehyde + NADPH + H+
glycerol + NADP+
show the reaction diagram
glucose + NADPH
sorbitol + NADP+
show the reaction diagram
-
-
-
-
?
glutathione-4-hydroxy-trans-2-nonenal + NADPH + H+
glutathione-1,4-dihydroxynonane + NADP+
show the reaction diagram
-
-
-
-
?
glyceraldehyde + NADPH + H+
glycerol + NADP+
show the reaction diagram
-
-
-
-
?
glycoaldehyde + NADPH + H+
ethylene glycol + NADP+
show the reaction diagram
-
-
-
-
?
glyoxal + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
isatin + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
methylglyoxal + NADPH
?
show the reaction diagram
-
-
-
-
?
methylglyoxal + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
octanal + NADPH + H+
1-octanol + NADP+
show the reaction diagram
-
-
-
-
?
phenyl-1,2-propanedione + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
phenylglyoxal + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
pyridine-3-aldehyde + NAD(P)H
3-hydroxypyridine + NAD(P)+
show the reaction diagram
-
-
-
-
r
pyridine-3-aldehyde + NADPH + H+
3-hydroxypyridine + NADP+
show the reaction diagram
-
-
-
-
?
pyridine-3-methanol + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
pyridine-4-aldehyde + NAD(P)H
4-hydroxypyridine + NAD(P)+
show the reaction diagram
-
-
-
-
r
pyridine-4-aldehyde + NADPH + H+
4-hydroxypyridine + NADP+
show the reaction diagram
-
-
-
-
?
sorbitol + NAD+
D-fructose + NADH + H+
show the reaction diagram
-
aldehyde reductase, ALR1
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
D-glucose + NADPH + H+
sorbitol + NADP+
show the reaction diagram
-
-
-
-
?
4-hydroxy-trans-2-nonenal + NADPH + H+
1,4-dihydroxynonane + NADP+
show the reaction diagram
-
-
-
-
?
aldose + NAD(P)H
alditol + NAD(P)+
show the reaction diagram
-
-
-
-
r
aldose + NADPH + H+
alditol + NADP+
show the reaction diagram
D-glucose + NADPH + H+
D-sorbitol + NADP+
show the reaction diagram
-
-
-
-
?
D-glucose + NADPH + H+
sorbitol + NADP+
show the reaction diagram
DL-glyceraldehyde + NADPH + H+
DL-glycerol + NADP+
show the reaction diagram
-
-
-
-
?
glutathione-4-hydroxy-trans-2-nonenal + NADPH + H+
glutathione-1,4-dihydroxynonane + NADP+
show the reaction diagram
-
-
-
-
?
sorbitol + NAD+
D-fructose + NADH + H+
show the reaction diagram
-
aldehyde reductase, ALR1
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
NADPH
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(3-benzyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
1,2-benzothiazin-1,1-dioxide
-
-
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
-
-
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-(3,7-bis(4-fluorophenyl)-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-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-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-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-(6-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
-
2-(6-bromo-3-(4-bromothiophenoxy)-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-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic 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-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
-
2-(7-bromo-3-(4-chlorothiophenoxy)-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-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-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
3-(4-fluorostyryl)-1-(4-nitrobenzyl)quinoxalin-2(1H)-one
-
-
3-(benzo[b] thiophen-3-yl)-1-(4-nitrobenzylquinoxalin-2(1H)-one
-
-
6-(5-chloro,3-methylbenzofuran-2-sulfonyl)2H-pyridazin-3-one
-
-
epalrestat
-
-
epicatechin
-
-
fidarestat
-
-
kaempferol
-
-
kaempferol 3-O-rutinoside
-
-
lidorestat
-
-
Myricitrin
-
-
N-(tert-butyl)-3-(4-(4-nitrobenzyl)-3-oxo-3,4-dihydroquinoxalin-2-ylacryl amide
-
-
ponalrestat
-
-
quercetin 3-O-beta-D-apiofuranosyl-(1->2)-beta-D-glucopyranoside
-
-
rhamnocitrin-3-O-rhamnoside
-
-
sorbinil
-
-
tiliroside
-
-
zenorestat
-
-
[2-oxo-3-(2-phenylethyl)quinoxalin-1(2H)-yl]acetic acid
-
-
[2-oxo-3-[(Z)-2-phenylethenyl]quinoxalin-1(2H)-yl]acetic acid
-
-
-
[3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
-
[3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
-
[3-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
-
-
[3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-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
-
-
((1-(2H-tetrazol-5-yl)methyl)-1H-pyrrol-3-yl)(phenyl)-methanone
-
40% inhibition
(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
(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-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid
-
; uncompetitive with both D,L-glyceraldehyde and NADPH
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
-
(2S)-2'-methoxykurarinone
-
potent inhibitor of rat lens aldose reductase
(2S)-3beta,7,4'-trihydroxy-5-methoxy-8-(gamma,gamma-dimethylallyl)-flavanone
-
-
(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
(5E)-5-[4-(4-oxo-4H-chromen-2-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
-
(5Z)-5-[(4-oxo-2-phenyl-4H-chromen-6-yl)methylidene]-1,3-thiazolidine-2,4-dione
-
-
(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
-
(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
-
(S)-6-fluorospiro[chroman-4,5'-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
-
-
1,3,3-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
-
-
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-dihydrobenzoic acid
-
-
2-(2-oxo-3-((3,4,5-trifluorophenyl)amino)quinoxalin-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-(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-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-benzoyl-1H-pyrrol-1-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-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(6-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(6-fluoro-3-(4-fluorophenoxy)-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-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(7-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(7-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic 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-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-ethoxycarbonyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid ethoxycarbonylmethyl ester
-
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-tert-butylsulfonylnaphthalene-1,3-dicarboxylic acid
-
2-tert-butylsulfonylnaphthalene-1-carboxylic acid
-
3',3'',5',5''-tetrabromophenolphthalein
-
less than 25% inhibition at 0.1 mM
3,3-dioxidenaphtho[1,2-d]isothiazole-1(2H)-one
-
3,3-Tetramethyleneglutaric acid
-
-
3,6,7-trichloroquinoxalin-2(1H)-one
-
-
3,6-dichloroquinoxalin-2(1H)-one
-
-
3,7-dichloroquinoxalin-2(1H)-one
-
-
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-(3-benzoyl-1H-pyrrol-1-yl)propanoic acid
-
-
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-hydroxycoumarin
-
-
3-morpholino syndnonimine
-
1 mM, 76% inhibition, reversed by incubation with fresh media
3-tert-butylsulfonylnaphthalene-2-carboxylic acid
-
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
30-norhederagenin
-
-
4-(3-benzoyl-1H-pyrrol-1-yl)butanoic acid
-
-
4-amino-N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamide
-
-
4-hydroxy-trans-2-nonenal
4-Hydroxycoumarin
-
-
4-O-butylpaeoniflorin
-
-
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
5-hydroxy-3S-hydroxymethyl-6-methyl-2,3-dihydrobenzofuran
-
-
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
-
-
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-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-chloroquinoxalin-2(1H)-one
-
-
6-hydroxy-7-methoxycoumarin
-
-
6-hydroxycoumarin
-
-
6-methoxypaeoniflorigenone
-
-
7-bromo-3-chloroquinoxalin-2(1H)-one
-
-
7-hydroxy-4-methylcoumarin
-
-
7-hydroxy-4-phenylcoumarin
-
-
7-hydroxy-6-methoxycoumarin
-
-
7-hydroxycoumarin
-
-
7-hydroxylcoumarin-4-acetic acid
-
-
7-hydroxylcoumarinyl-4-acetic acid
-
-
7-methoxycoumarin
-
-
7-methyl-2,3-dihydrospiro[4H-thiopyrano[2,3-b]pyridin-4,4'imidazolidine]-2',5'-dione
-
50% inhibition at 0.0011 mM
8-lavandulylkaempferol
-
potent inhibitor of rat lens aldose reductase
8-O-benzoylpaeonidanin
-
-
8-phenylsulfonylphthalazin-2H-3-one
-
IC50: 55 nM
alpha-benzoyloxypaeoniflorin
-
-
apiopaeonoside
-
-
Barbital
benzbromarone
-
-
benzoylpaeoniflorin
-
-
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
-
-
chlorogenic acid
-
-
Cl-
-
0.2 M, wild type and recombinant from E. coli
coptisine
-
85.86-86.87% inhibition at 0.05 mg/ml
coumarin
-
-
CuCl2
-
0.007 mM, 20% residual activity, addition of dithiothreitol recovers activity
D-mannitol
-
-
daidzein
-
-
davallialactone
-
-
delphinidin 3-O-beta-galactopyranoside
-
most potent inhibitor
delphinidin 3-O-beta-galactopyranoside-3',5'-di-O-beta-glucopyranoside
-
-
desmethylanhydroicaritin
-
potent inhibitor of rat lens aldose reductase
Diphenic acid
-
less than 25% inhibition at 0.5 mM
DTT
-
activates the enzyme in healthy heart slightly, but slightly inhibits the ischemic heart enzyme
ellagic acid
-
-
epalrestat
epiberberine
-
complete inhibition at 0.05 mg/ml
fidarestat
galloylpaeoniflorin
-
-
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
groenlandicine
-
52.38-60.32% inhibition at 0.05 mg/ml
Hexestrol
-
-
hypholomine B
-
-
indomethacin
-
less than 25% inhibition at 0.1 mM
isoliquiritigenin
-
-
isorhamnetin 3-O-beta-D-galactopyranoside
-
-
isorhamnetin 3-O-beta-D-glucopyranoside
-
-
jateorrhizine
-
12.68-14.08% inhibition at 0.05 mg/ml
kurarinol
-
potent inhibitor of rat lens aldose reductase
kurarinone
-
potent inhibitor of rat lens aldose reductase
kushenol E
-
potent inhibitor of rat lens aldose reductase
liquiritigenin
-
-
Ly-294002
-
0.05 mM, little decrease in sorbitol-induced activity
magnoflorine
-
18.33-29.85% inhibition at 0.05 mg/ml
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
-
-
minalrestat
-
-
mumeflavonoside A
-
-
mumeose K
-
-
mumeose L
-
-
mumeose M
-
-
mumeose N
-
-
myricetin
-
-
Myricitrin
-
-
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-(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-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-napthalenyl)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-[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-[[6-methoxy-5(trifluoromethyl)-1-naphthalenyl]thioxomethyl]-N-methylglycine
-
wild type and recombinant from E. coli
naphtho[1,2-d]isothiazole acetic acid derivatives
-
-
nitazoxanide
-
partial inhibition
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
nudanpinoside H
-
-
oxypaeoniflorin
-
-
p-chloromercuribenzoate
paeoniflorigenone
-
-
paeoniflorin
-
-
paeonolide
-
-
paeonoside
-
-
palbinone
-
-
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
Phenobarbital
-
-
ponalrestat
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
quercetin
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
-
-
ranirestat
-
-
rubrolide L
-
-
S-nitroso-N-acetylpenicillamine
-
1 mM, 86% inhibition, reversed by incubation with fresh media
S-nitrosoglutathione
-
1 mM, 70% 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 inhbition of ALR1
SB-203580
-
0 0.01 mM, decrease of sorbitol-induced activity below control level
semilicoisoflavone B
-
contains a gamma,gamma-dimethylchromene ring on the aromatic ring
sorbinil
stobadine
-
i.e. (-)-cis-2,8-dimethyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3,-b]indole
tetramethylene glutaric acid
-
-
tizoxanide
-
partial inhibition
TNF-alpha
-
-
-
Tolrestat
Valproate
-
less than 25% inhibition at 0.5 mM
Valproic acid
-
-
zearalenone
-
-
zopolrestat
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(NH4)2SO4
DTT
-
activates the enzyme in healthy heart slightly, but slightly inhibits the ischemic heart enzyme
methylglyoxal
-
up to 4.5fold induction of mRNA, activity and protein level, abolished in presence of cycloheximide or actinomycin D
Na2SO4
-
0.1 M, wild type and recombinant from E.coli
sorbitol
-
600 mosmol per kg H2O, up to 2fold increase in activity
SP-600125
-
0.01 mM, about 50% increase of sorbitol-induced activity
sulfate
-
activates the enzyme in ischemic heart
additional information
-
gene expression in YPEN-1 and NRK cells is up-regulated by treatments with submicromolar concentrations of hydrogen peroxide and 1,4-naphthoquinone, but not with fibroblast growth factor-1, fibroblast growth factor-2, 5alpha-dihydrotestosterone and 17beta-estradiol
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.2
(1S)-Camphorquinone
-
in 0.1 M potassium phosphate, pH 7.4
0.015
1-butanal
-
in 0.1 M potassium phosphate, pH 7.4
63
1-butanol
-
in 0.1 M potassium phosphate, pH 7.4
0.0055
1-decanal
-
in 0.1 M potassium phosphate, pH 7.4
0.082
1-Decanol
-
in 0.1 M potassium phosphate, pH 7.4
0.023
1-hexanal
-
in 0.1 M potassium phosphate, pH 7.4
0.97
1-Hexanol
-
in 0.1 M potassium phosphate, pH 7.4
0.005
1-nonanal
-
in 0.1 M potassium phosphate, pH 7.4
0.74
1-nonanol
-
in 0.1 M potassium phosphate, pH 7.4
0.014
1-octanal
-
in 0.1 M potassium phosphate, pH 7.4
0.3
1-propanal
-
in 0.1 M potassium phosphate, pH 7.4
0.0057
16-ketoestrone
-
in 0.1 M potassium phosphate, pH 7.4
0.68
2,3-Butanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.0065
2,3-heptanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.014
2,3-Hexanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.2
2,3-Pentanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.048
2,4-decadienal
-
in 0.1 M potassium phosphate, pH 7.4
0.064
2,4-nonadienal
-
in 0.1 M potassium phosphate, pH 7.4
0.01
2-decenal
-
in 0.1 M potassium phosphate, pH 7.4
0.075
2-hexenal
-
in 0.1 M potassium phosphate, pH 7.4
0.017
2-nonenal
-
in 0.1 M potassium phosphate, pH 7.4
0.78
2-phenyl-1-propanol
-
in 0.1 M potassium phosphate, pH 7.4
0.052
2-phenyl-2-propenal
-
in 0.1 M potassium phosphate, pH 7.4
0.0095
21-Dehydrocortisol
-
in 0.1 M potassium phosphate, pH 7.4
0.31
3,4-hexanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.07
3-deoxyglucosone
-
in 0.1 M potassium phosphate, pH 7.4
0.03
4-hydroxynonenal
-
in 0.1 M potassium phosphate, pH 7.4
0.0035
4-nitrobenzaldehyde
-
in 0.1 M potassium phosphate, pH 7.4
0.12
acrolein
-
in 0.1 M potassium phosphate, pH 7.4
0.063
benzaldehyde
-
in 0.1 M potassium phosphate, pH 7.4
2.1
benzyl alcohol
-
in 0.1 M potassium phosphate, pH 7.4
78 - 83
D-galactose
204 - 281
D-glucose
13.9 - 19.2
D-glucuronate
0.073
D-lactoaldehyde
-
in 0.1 M potassium phosphate, pH 7.4
13.5 - 29
D-xylose
0.071 - 2
DL-glyceraldehyde
1.5
glycoaldehyde
-
in 0.1 M potassium phosphate, pH 7.4
1.28
Glyoxal
-
in 0.1 M potassium phosphate, pH 7.4
0.069
isatin
-
in 0.1 M potassium phosphate, pH 7.4
0.26
methylglyoxal
-
in 0.1 M potassium phosphate, pH 7.4
0.054
NADPH
-
isoform ALR2, pH 6.2, 30°C
0.056
phenyl-1,2-propanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.016
Phenylglyoxal
-
in 0.1 M potassium phosphate, pH 7.4
0.012
Pyridine-3-aldehyde
-
in 0.1 M potassium phosphate, pH 7.4
0.02
Pyridine-4-aldehyde
-
in 0.1 M potassium phosphate, pH 7.4
additional information
additional information
-
steady-state kinetics
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.333
(1S)-Camphorquinone
-
in 0.1 M potassium phosphate, pH 7.4
0.007
(S)-1-indanol
-
in 0.1 M potassium phosphate, pH 7.4
0.003
(S)-1-tetralol
-
in 0.1 M potassium phosphate, pH 7.4
0.67
1-butanal
-
in 0.1 M potassium phosphate, pH 7.4
0.137
1-butanol
-
in 0.1 M potassium phosphate, pH 7.4
0.35
1-decanal
-
in 0.1 M potassium phosphate, pH 7.4
0.023
1-Decanol
-
in 0.1 M potassium phosphate, pH 7.4
0.75
1-hexanal
-
in 0.1 M potassium phosphate, pH 7.4
0.068
1-Hexanol
-
in 0.1 M potassium phosphate, pH 7.4
0.57
1-nonanal
-
in 0.1 M potassium phosphate, pH 7.4
0.062
1-nonanol
-
in 0.1 M potassium phosphate, pH 7.4
0.7
1-octanal
-
in 0.1 M potassium phosphate, pH 7.4
0.13
1-propanal
-
in 0.1 M potassium phosphate, pH 7.4
0.183
16-ketoestrone
-
in 0.1 M potassium phosphate, pH 7.4
0.333
2,3-Butanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.6
2,3-heptanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.25
2,3-Hexanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.383
2,3-Pentanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.2
2,4-decadienal
-
in 0.1 M potassium phosphate, pH 7.4
0.2
2,4-nonadienal
-
in 0.1 M potassium phosphate, pH 7.4
0.145
2-decenal
-
in 0.1 M potassium phosphate, pH 7.4
0.67
2-hexenal
-
in 0.1 M potassium phosphate, pH 7.4
0.155
2-nonenal
-
in 0.1 M potassium phosphate, pH 7.4
0.012
2-phenyl-1-propanol
-
in 0.1 M potassium phosphate, pH 7.4
0.43
2-phenyl-2-propenal
-
in 0.1 M potassium phosphate, pH 7.4
0.2
21-Dehydrocortisol
-
in 0.1 M potassium phosphate, pH 7.4
0.233
3,4-hexanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.2
3-deoxyglucosone
-
in 0.1 M potassium phosphate, pH 7.4
0.183
4-hydroxynonenal
-
in 0.1 M potassium phosphate, pH 7.4
0.57
4-nitrobenzaldehyde
-
in 0.1 M potassium phosphate, pH 7.4
0.27
acrolein
-
in 0.1 M potassium phosphate, pH 7.4
0.42
benzaldehyde
-
in 0.1 M potassium phosphate, pH 7.4
0.0383
benzyl alcohol
-
in 0.1 M potassium phosphate, pH 7.4
0.283
D-lactoaldehyde
-
in 0.1 M potassium phosphate, pH 7.4
0.583
DL-glyceraldehyde
-
in 0.1 M potassium phosphate, pH 7.4
0.2
glycoaldehyde
-
in 0.1 M potassium phosphate, pH 7.4
0.2
Glyoxal
-
in 0.1 M potassium phosphate, pH 7.4
0.283
isatin
-
in 0.1 M potassium phosphate, pH 7.4
0.43
methylglyoxal
-
in 0.1 M potassium phosphate, pH 7.4
0.383
phenyl-1,2-propanedione
-
in 0.1 M potassium phosphate, pH 7.4
0.42
Phenylglyoxal
-
in 0.1 M potassium phosphate, pH 7.4
0.52
Pyridine-3-aldehyde
-
in 0.1 M potassium phosphate, pH 7.4
0.002
Pyridine-3-methanol
-
in 0.1 M potassium phosphate, pH 7.4
0.63
Pyridine-4-aldehyde
-
in 0.1 M potassium phosphate, pH 7.4
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0182 - 3.081
(2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid
0.0167 - 0.328
(2-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid
0.0088
1,2,7-trihydroxy-3,8-dimethoxy-6-methylanthracene-9,10-dione 2-O-beta-D-glucoside
-
pH 7.0, 37°C
0.0136
1,3,7-trihydroxy-2,8-dimethoxy-6-methylanthracene-9,10-dione
-
pH 7.0, 37°C
0.0159
1,3,8-trihydroxy-6-methylanthracene-9,10-dione
-
pH 7.0, 37°C
0.0241
3,3-Tetramethyleneglutaric acid
-
pH 7.0, 37°C
0.0141
4-amino-N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamide
-
-
0.00033
davallialactone
-
pH 6.2, 37°C
0.00063
ellagic acid
-
pH 6.2, 37°C
0.00082
hypholomine B
-
pH 6.2, 37°C
0.0155
N-(3,5-difluoro-4-hydroxyphenyl)-4-methoxybenzenesulfonamide
-
-
0.0444
N-(3,5-difluoro-4-hydroxyphenyl)-4-nitrobenzenesulfonamide
-
-
0.0329
N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamide
-
-
0.01355
nitazoxanide
-
pH and temperature not specified in the publication
0.00935
tizoxanide
-
pH and temperature not specified in the publication
0.000005
zopolrestat
-
pH 6.2, 30°C, isoform ALR2
additional information
additional information
-
inhibition kinetics, overview
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00111
(3-benzyl-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
0.00213
2-(3,7-bis(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
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
0.000296
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
0.00338
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
0.000468
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
0.000139
2-(6-bromo-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
0.000319
2-(6-bromo-3-(4-bromothiophenoxy)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
0.000095
2-(6-chloro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
0.00006
2-(6-fluoro-3-(2,4-dihydroxyphenyl)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
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
0.000467
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
0.000069
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
0.00152
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
0.00087
2-(7-fluoro-3-(4-fluorophenyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
0.000084
epalrestat
Rattus norvegicus;
-
pH 6.2, 30°C
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
-
0.000419
[3-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
0.00018
[3-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
0.00418
[3-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
0.0008
[3-[2-(4-hydroxyphenyl)ethyl]-2-oxoquinoxalin-1(2H)-yl]acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C
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
0.01
(1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
Rattus norvegicus;
P07943
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
0.000678
(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
0.0963
(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
0.00377
(2S)-2'-methoxykurarinone
Rattus norvegicus;
-
-
0.00363
(2S)-3beta,7,4'-trihydroxy-5-methoxy-8-(gamma,gamma-dimethylallyl)-flavanone
Rattus norvegicus;
-
-
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
0.00003
(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
0.000432
(5E)-5-[4-(4-oxo-4H-chromen-2-yl)benzylidene]-1,3-thiazolidine-2,4-dione
Rattus norvegicus;
-
pH 6.2, 37°C
0.000683
(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;
P07943
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;
P07943
IC50: 0.180 mM
0.1
(9-amino-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
Rattus norvegicus;
P07943
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;
P07943
IC50: 0.190 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
0.001204
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
0.000045
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
0.0000328
2-(3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C, ALR2
0.002
2-(3-benzoyl-1H-pyrrol-1-yl)acetic acid
Rattus norvegicus;
-
pH 7.2, temperature not specified in the publication
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
0.00000431
2-(6-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C, ALR2
0.00000504
2-(6-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C, ALR2
0.00007
2-(6-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C, ALR2
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
0.0000063
2-(7-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C, ALR2
0.0000423
2-(7-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C, ALR2
0.0000191
2-(7-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
Rattus norvegicus;
-
pH 6.2, 30°C, ALR2
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;
P07943
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;
P07943
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;
P07943
IC50: 0.088 mM
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
0.0285
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
0.0097
3-(3-benzoyl-1H-pyrrol-1-yl)propanoic acid
Rattus norvegicus;
-
pH 7.2, temperature not specified in the publication
0.062 - 0.172
3-hydroxycoumarin
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
0.0288
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
0.045 - 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
0.0624
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
0.0427
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
0.05
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
0.000643
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
0.038 - 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
0.056 - 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
0.0245 - 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
0.0038
8-lavandulylkaempferol
Rattus norvegicus;
-
-
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
0.1184
coptisine
Rattus norvegicus;
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.4 - 0.5
coumarin
0.01
daidzein
Rattus norvegicus;
-
in 0.1 M potassium phosphate, pH 7.4
0.00095
desmethylanhydroicaritin
Rattus norvegicus;
-
-
0.00000143 - 0.094
epalrestat
0.1
epiberberine
Rattus norvegicus;
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.0085
fidarestat
Rattus norvegicus;
-
in 0.1 M potassium phosphate, pH 7.4
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
0.1401
groenlandicine
Rattus norvegicus;
-
in 100 mM sodium phosphate buffer (pH 6.2)
0.0032
Hexestrol
Rattus norvegicus;
-
in 0.1 M potassium phosphate, pH 7.4
0.0034
isoliquiritigenin
Rattus norvegicus;
-
pH 7.0, 37°C
0.00213
kurarinol
Rattus norvegicus;
-
-
0.00299
kurarinone
Rattus norvegicus;
-
-
0.00774
kushenol E
Rattus norvegicus;
-
-
0.002
liquiritigenin
Rattus norvegicus;
-
pH 7.0, 37°C
0.0006
minalrestat
Rattus norvegicus;
-
in 0.1 M potassium phosphate, pH 7.4
0.0068
myricetin
Rattus norvegicus;
-
in 0.1 M potassium phosphate, pH 7.4
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-napthalenyl)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
0.0012 - 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
0.00822
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
0.0223
puerariafuran
Rattus norvegicus;
-
pH 7.0, 37°C
0.0025 - 0.0188
quercetin
0.0188
S12728
Rattus norvegicus;
-
pH 6.2, 30°C, ALR2
0.0018
semilicoisoflavone B
Rattus norvegicus;
-
pH 7.0, 37°C
0.00014 - 0.03
sorbinil
0.00535
tizoxanide
Rattus norvegicus;
-
pH and temperature not specified in the publication
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
0.025
zearalenone
Rattus norvegicus;
-
in 0.1 M potassium phosphate, pH 7.4
0.000004
zopolrestat
Rattus norvegicus;
-
IC50: 4 nM
additional information
additional information
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
1.2
-
healthy lens
19.2
-
diabetic lens
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6
-
assay at
7.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
24
-
assay at
25
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
aortic, higher activity in aged compared to young rats
Manually annotated by BRENDA team
-
of diabetic rats
Manually annotated by BRENDA team
additional information
-
the mRNA is detected in all rat tissues besides the brain, but contents in rat tissues other than the lung, stomach and adrenal gland are low
Manually annotated by BRENDA team
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
35000
-
gel filtration
36000
-
SDS-PAGE
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
no glycoprotein
-
-
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
hanging drop vapour diffusion method, using 0.1 M HEPES pH 7.5, 20% (w/v) polyethylene glycol 4000 and 10% (v/v) 2-propanol
-
purified recombinant enzyme in ternary/binary complex with inhibitor nitazoxanide and/or NADP+, or with NADP+ and glyceraldehyde, for enzyme-NADP+-nitazoxanide complex, enzyme-NADP+ crystals are soaked in a saturated solution of nitazoxanide containing 50% N,N-dimethylformamide, 50 mM ammonium citrate, pH 5.0, and 12.5% PEG 6000, for enzyme-NADP+-D-glyceraldehyde complex, enzyme-NADP+ crystals are soaked in a solution containing 20% pyridine, 0.3 M D,L-glyceraldehyde, 50 mM ammonium citrate, pH 5.0, and 12.5% m/v PEG 6000, X-ray diffraction structure determination and analysis, modeling
-
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6 - 8
-
the NADPH-linked pyridine-3-aldehyde reductase activity is gradually increased by decreasing pH from 8.0 to 6.0
697266
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
enzyme is not stable unless dithiothreitol in micromolar range is present
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
ALR2 partially from lenses
-
native enzyme partially from left ventricular tissue, by ultracentrifugation and gel filtration
-
native enzyme partially from lens by ammonium sulfate fractionation and dialysis
Q-Sepharose column chromatography and Sephadex G-100 gel filtration
-
Q-Sepharose column chromatography, Sephadex G-100 gel filtration, and Red-Sepharose column chromatography
-
wild type and expressed in Escherichia coli
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expressed in Escherichia coli and in YPEN-1 and NRK cells
-
expressed in Escherichia coli BL21 (DE3) pLysS cells
-
expression in Escherichia coli
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
upregulation of the aldose reductase pathway with aging
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C298S
-
similar sensitivity against Cu2+ as wild-type
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine