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Information on EC 1.1.1.21 - aldose reductase and Organism(s) Rattus norvegicus and UniProt Accession P07943
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EC Tree
1.1.1.21 aldose reductaseIUBMB Comments
Has wide specificity.
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Word Map
- 1.1.1.21
- lens
- nerve
- neuropathy
- sorbinil
- cataract
- mellitus
- retinopathy
- hyperglycemia
-
glycation
- streptozotocin
- galactose
-
sciatic
- fructose
- retinal
- endothelial
-
streptozotocin-induced
- myo-inositol
- erythrocyte
- reductases
-
nadph-dependent
-
streptozotocin-diabetic
-
microvascular
-
galactosemic
- galactitol
-
hypertonic
-
diabetes-induced
-
stz-induced
- opacity
-
antidiabetic
-
glucose-induced
-
osmolytes
- pericytes
-
nondiabetic
-
cataractogenesis
-
galactose-induced
- microangiopathy
-
endoneurial
- xylitol
-
sural
- hne
-
hyperglycemia-induced
- polyneuropathy
-
lenticular
-
glycaemic
-
mesangial
- synthesis
-
opacification
-
stz-diabetic
- alr
- akr1c3
- microaneurysms
- nutrition
- medicine
- drug development
- diagnostics
- biotechnology
The taxonomic range for the selected organisms is: Rattus norvegicus
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea
Synonyms
aldose reductase, akr1b10, akr1b3, akr1b, aldose reductase-like, aldose reductase-like protein, aldo-keto reductase family 1 member b1, akr1b14, aldose reductase 2, aldrxv4, 
more
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
20-alpha-HSD
-
-
-
-
20-alpha-hydroxysteroid dehydrogenase
-
-
-
-
aldehyde reductase
alditol:NADP 1-oxidoreductase
-
-
-
-
alditol:NADP oxidoreductase
-
-
-
-
aldo-keto reductase family 1 member B7
-
-
-
-
aldose reductase
-
-
aldose xylose reductase
-
-
-
-
ALR2
Fibroblast growth factor regulated protein
-
-
-
-
FR-1 protein
-
-
-
-
MVDP
-
-
-
-
NADPH-aldopentose reductase
-
-
-
-
NADPH-aldose reductase
-
-
-
-
polyol dehydrogenase (NADP2)
-
-
-
-
TPN-polyol dehydrogenase
-
-
-
-
VAS deferens androgen-dependent protein
-
-
-
-
aldehyde reductase
-
-
-
-
ALR2
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
oxidation
-
-
-
-
reduction
-
-
-
-
PATHWAY SOURCE
PATHWAYS
BRENDA
KEGG
-
-, -, -, -, -
SYSTEMATIC NAME
IUBMB Comments
alditol:NAD(P)+ 1-oxidoreductase
Has wide specificity.
CAS REGISTRY NUMBER
COMMENTARY
9028-31-3
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
4-hydroxy-trans-2-nonenal + NADPH + H+
1,4-dihydroxynonane + NADP+
-
-
-
-
?
D-glucuronate + NADPH
? + NADP+
-
substrate of aldehyde reductase ALR1
-
-
?
DL-glyceraldehyde + NADPH + H+
DL-glycerol + NADP+
-
-
-
-
?
DL-glyceraldehyde + NADPH + H+
glycerol + NADP+
-
-
-
-
?
glutathione-4-hydroxy-trans-2-nonenal + NADPH + H+
glutathione-1,4-dihydroxynonane + NADP+
-
-
-
-
?
aldose + NADPH + H+
alditol + NADP+
-
first and rate-limiting step in the polyol pathway, in which reduction of glucose to sorbitol is coupled with NADPH oxidation, the enzyme activity is negatively regulated by nitric oxide in the eye lens, the activity in diabetic rat lens is increased due to reduced NO concentration, overview
-
-
?
aldose + NADPH + H+
alditol + NADP+
-
first and rate-limiting step in the polyol pathway, pathway network overview
-
-
?
aldose + NADPH + H+
alditol + NADP+
-
increased enzyme activity and oxidative or nitrosative stress are involved in pathogenesis of diabetic nephropathy, overview
-
-
?
D-glucose + NADPH + H+
sorbitol + NADP+
-
the aldose reductase pathway has been demonstrated to be a key component of myocardial ischemia reperfusion injury, inhibition of AR protects the ischemic myocardium and is associated with improved energy metabolism, overview, pharmacological inhibition of the enzyme or sorbitol dehydrogenase blocks JAK2 and STAT5 activation and is associated with lower lactate/pyruvate ratio and lower protein kinase C activity, mechanism, overview
-
-
?
DL-glyceraldehyde + NADPH
glycerol + NADP+
-
-
-
-
?
DL-glyceraldehyde + NADPH
glycerol + NADP+
-
substrate of aldose reductase ALR2
-
-
?
additional information
?
-
-
protective role of enzyme against methylglyoxal induced cell damage
-
-
?
additional information
?
-
-
protective role of enzyme against methylglyoxal induced cell damage, cytotoxic effect of methylglyoxal is enhanced in presence of ponalrestat
-
-
?
additional information
?
-
-
the enzyme regulates high-glucose-induced growth and contributes to diabetic hyperproliferation of vascular smooth muscle cells, inhibition of the enzyme also increases vascular oxidative stress, overview
-
-
?
additional information
?
-
-
the enzyme shows increased activity and is redox activated in ischemic heart
-
-
?
additional information
?
-
-
aldose reductase regulates high glucose-induced ectodomain shedding of tumor necrosis factor-alpha via protein kinase C-delta and tumor necrosis factor-alpha converting enzyme in vascular smooth muscle cells
-
-
?
additional information
?
-
-
exhibits low NADP+-linked dehydrogenase activity towards aliphatic and aromatic alcohols
-
-
?
additional information
?
-
-
no NADH-linked reductase activity is observed
-
-
?
additional information
?
-
-
the enzyme catalyzes the reduction of a wide range of substances, including prostaglandin H2, phospholipid aldehydes, lipid peroxidation products, environmental pollutants and their glutathione conjugates
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
4-hydroxy-trans-2-nonenal + NADPH + H+
1,4-dihydroxynonane + NADP+
-
-
-
-
?
DL-glyceraldehyde + NADPH + H+
DL-glycerol + NADP+
-
-
-
-
?
glutathione-4-hydroxy-trans-2-nonenal + NADPH + H+
glutathione-1,4-dihydroxynonane + NADP+
-
-
-
-
?
aldose + NADPH + H+
alditol + NADP+
-
first and rate-limiting step in the polyol pathway, in which reduction of glucose to sorbitol is coupled with NADPH oxidation, the enzyme activity is negatively regulated by nitric oxide in the eye lens, the activity in diabetic rat lens is increased due to reduced NO concentration, overview
-
-
?
aldose + NADPH + H+
alditol + NADP+
-
first and rate-limiting step in the polyol pathway, pathway network overview
-
-
?
aldose + NADPH + H+
alditol + NADP+
-
increased enzyme activity and oxidative or nitrosative stress are involved in pathogenesis of diabetic nephropathy, overview
-
-
?
D-glucose + NADPH + H+
sorbitol + NADP+
-
the aldose reductase pathway has been demonstrated to be a key component of myocardial ischemia reperfusion injury, inhibition of AR protects the ischemic myocardium and is associated with improved energy metabolism, overview, pharmacological inhibition of the enzyme or sorbitol dehydrogenase blocks JAK2 and STAT5 activation and is associated with lower lactate/pyruvate ratio and lower protein kinase C activity, mechanism, overview
-
-
?
additional information
?
-
-
protective role of enzyme against methylglyoxal induced cell damage
-
-
?
additional information
?
-
-
protective role of enzyme against methylglyoxal induced cell damage, cytotoxic effect of methylglyoxal is enhanced in presence of ponalrestat
-
-
?
additional information
?
-
-
the enzyme regulates high-glucose-induced growth and contributes to diabetic hyperproliferation of vascular smooth muscle cells, inhibition of the enzyme also increases vascular oxidative stress, overview
-
-
?
additional information
?
-
-
the enzyme shows increased activity and is redox activated in ischemic heart
-
-
?
additional information
?
-
-
aldose reductase regulates high glucose-induced ectodomain shedding of tumor necrosis factor-alpha via protein kinase C-delta and tumor necrosis factor-alpha converting enzyme in vascular smooth muscle cells
-
-
?
additional information
?
-
-
the enzyme catalyzes the reduction of a wide range of substances, including prostaglandin H2, phospholipid aldehydes, lipid peroxidation products, environmental pollutants and their glutathione conjugates
-
-
?
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(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
-
(3,3-dihydroxy-1-oxo-1,3-dihydro-2H-3lambda4-naphtho[1,2-d]isothiazol-2-yl)acetic acid
i.e. NiT
(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
-
1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
-
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}
-
2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid}
41% inhibition
2-(3-(3-(tert-butylamino)-3-oxoprop-1-en-1-yl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
25% inhibition
2-(3-(4-(4-methoxyphenyl) piperazin-1-yl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
48% inhibition
2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
40% inhibition
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-(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-(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
-
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
-
N-(tert-butyl)-3-(4-(4-nitrobenzyl)-3-oxo-3,4-dihydroquinoxalin-2-ylacryl amide
-
[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-(2-(2H-tetrazol-5-yl)ethyl)-1H-pyrrol-3-yl)(phenyl)-methanone
-
6% inhibition
(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-[[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
-
-
(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
-
-
(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
-
-
1,2,7-trihydroxy-3,8-dimethoxy-6-methylanthracene-9,10-dione 2-O-beta-D-glucoside
-
-
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
2,2,2-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
-
650fold selectivity for isoform ALR2 over ALR1
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
-
858fold selectivity for isoform ALR2 over ALR1
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-(2-oxo-3-((3,4,5-trifluorophenyl)amino)quinoxalin-1(2H)-yl)acetic acid
-
-
2-(3-((4-bromo-2-fluorophenyl)amino)-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-(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-(6-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
2-(7-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
-
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-(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-morpholino syndnonimine
-
1 mM, 76% inhibition, reversed by incubation with fresh media
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-[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
6,7-dihydroxy-4-phenylcoumarin
-
binds to ALR2 in a different manner from epalrestat, molecular docking, overview. Suppresses galactitol accumulation
6-(2-chloro-6-fluorophenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 26 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-trifluoromethylphenylmethanesulfonyl)-2H-pyridazin-3-one
-
IC50: 500 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-(5,6-methylenedioxyindole-2-sulfonyl)-2H-pyridazin-3-one
-
IC50: 0.0038 mM
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-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
7-methyl-2,3-dihydrospiro[4H-thiopyrano[2,3-b]pyridin-4,4'imidazolidine]-2',5'-dione
-
50% inhibition at 0.0011 mM
CuCl2
-
0.007 mM, 20% residual activity, addition of dithiothreitol recovers activity
DTT
-
activates the enzyme in healthy heart slightly, but slightly inhibits the ischemic heart 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
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-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-(6-bromo-3-(4-bromo-2-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-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
methyl 2-(7-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
-
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-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)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-[(4-trifluoromethylphenyl)sulfonyl]glycine
-
no inhibition of ALR1
N-[2-(2-thienyl)ethyl]-N-[(4-chlorophenyl)sulfonyl]glycine
-
no inhibition of ALR1
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
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
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
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
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
stobadine
-
i.e. (-)-cis-2,8-dimethyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3,-b]indole
[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
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
-
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
IC50: 0.068 mM
2-benzyl-1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazole-4-carboxylic acid
IC50: 0.10 mM
(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
-
-
(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
(S)-6-fluorospiro[chroman-4,5'-imidazolidine]-2',4'-dione
-
wild type and recombinant from E. coli
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
ponalrestat
-
cytotoxic effect of methylglyoxal is enhanced in presence of ponalrestat
sorbinil
-
AR inhibitor, prevents hyperproliferation of aortic smooth muscle cells
Tolrestat
-
AR inhibitor, prevents hyperproliferation of aortic smooth muscle cells, cell cycle progression in the presence of high glucose was blocked by tolrestat
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
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
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
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
-
enzyme inhibition counteracts nitrosative stress and poly(ADP-ribose) polymerase activation in diabetic kidney cortex
-
additional information
-
inhibition of AR protects the ischemic myocardium and is associated with improved energy metabolism
-
additional information
-
synthesis and structure-activity relationship study of inhibitors, overview
-
additional information
-
berberine and palmatine exhibit no RLAR inhibitory activities within the test concentration of 0.012.5-0.05 mg/ml
-
additional information
-
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
-
methanolic and ethanolic extracts of Litchi chinensis fruits are potent inhibitors of rat lens aldose reductase
-
additional information
-
the enzyme activity is not affected by 0.1 mM Wy14643
-
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
-
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
-
inhibitory effect of total lignan from fructus Arctii on aldose reductase, ethanolic extract from dry ripe fruits of Arctium lappa
-
additional information
-
structure-activity relationship of a series of coumarins as ALR1 inhibitors, overview. The C6 OH group interferes with ALR1 inhibition activity
-
additional information
-
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
-
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
-
synthesis of quinoxalinone derivatives as potent inhibitors of aldose reductase, Structure-activity relationship and molecular docking studies, overview
-
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
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
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
LITERATURE
IMAGE
0.0934
DL-glyceraldehyde
-
pH 6.0, 25°C, ischemic heart, in presence of DTT
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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
additional information
additional information
-
inhibition kinetics, overview
-
0.0182
(2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid
-
pH 6.2, 30°C, isoform ALR2
3.081
(2-benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid
-
pH 7.2, 37°C, isoform ALR1
0.0167
(2-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid
-
pH 6.2, 30°C, isoform ALR2
0.328
(2-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole-8-yl)-acetic acid
-
pH 7.2, 37°C, isoform ALR1
0.0089
capsaicin
-
enzyme isolated from heart, pH 6.2, temperature not specified in the publication
0.267
capsaicin
-
enzyme isolated from kidney, pH 6.2, temperature not specified in the publication
0.535
capsaicin
-
enzyme isolated from liver, pH 6.2, temperature not specified in the publication
0.597
capsaicin
-
enzyme isolated from brain, pH 6.2, temperature not specified in the publication
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.01
(1,3,3-trioxo-1,2-dihydronaphtho[1,2-d]isothiazol-2-yl)acetic acid
Rattus norvegicus
IC50: 0.010 mM
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
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
0.00213
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
0.00014
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
0.00014
[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
0.02
(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
0.000241
(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
(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
0.00363
(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
0.000242
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
0.000064
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
0.000987
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
0.00116
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
0.0000382
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
0.000139
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
0.0318
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
0.0995
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
0.0362
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
0.000035
6-(2,3-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 35 nM
0.000257
6-(2,3-difluorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 257 nM
0.000052
6-(2,6-dichlorophenylmethanesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 52 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
0.000118
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
0.000422
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
0.00014
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
0.00036
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
0.000006
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
0.000003
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
0.00015
6-(alpha-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 150 nM
0.00036
6-(beta-naphthylmethylbenzenesulfonyl)-2H-pyridazin-3-one
Rattus norvegicus
-
IC50: 360 nM
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
0.05
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
0.05
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
0.05
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
0.0446
galloylpaeoniflorin
Rattus norvegicus
-
IC50 above 0.05 mM, in 135 mM Na/K phosphate buffer (pH 7.0), 100 mM Li2SO4, at 37°C
0.0036
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
0.0847
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
0.0747
N-benzyl-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
0.0224
N-[2-(2-thienyl)ethyl]-N-[(4-chlorophenyl)sulfonyl]glycine
Rattus norvegicus
-
pH 6.2, 30°C, ALR2
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
0.05
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
0.000234
[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
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
0.062
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
0.045
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
0.038
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
0.0075
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
0.4
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
0.0014
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
0.0055
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
0.0012
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
0.0501
Valproic acid
Rattus norvegicus
-
pH 7.2, temperature not specified in the publication
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
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
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
enzyme activity, and sorbitol, glucose, and fructose contents in renal cortex of control and streptozotocin-diabetic rats, determination of nitrotyrosine in control and diabetic kidney, overview
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
6.2
6.2
7.2
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
30
30
37
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
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
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
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
metabolism
-
aldose reductase is the first enzyme in the polyol pathway and reduces glucose to sorbitol utilizing NADPH as a cofactor. Sorbitol is then metabolized to fructose by sorbitol dehydrogenase
metabolism
-
the enzyme catalyzes the first step in the polyol pathway of glucose metabolism
metabolism
-
the enzyme is the first and rate-limiting enzyme in the polyol pathway where it catalyzes the reduction of glucose to sorbitol
physiological function
-
aldose reductase inhibition reduces sorbitol accumulation and cell death in ischemia-reperfusion injury in the retina, phenotype, overview
physiological function
-
aldose reductase is involved in the polyol pathway, and regulates vascular smooth muscle cell proliferation by modulating G1/S phase transition of cell cycle. It prevents high glucose- or TNFalpha-induced vascular smooth muscle cell proliferation by accumulating the cells in the G1 phase
physiological function
-
high sugar levels found in diabetic cataract cause the opacification of lenses by osmotic changes induced via the aldose reductase-mediated polyol pathway
physiological function
-
the enzyme and AGE-RAGE pathways, involving advanced glycation endproducts and their a soluble form of the chief signal transduction receptors, play central roles in the pathogenesis of vascular dysfunction in aging rats. Significant increases in aldose reductase expression and activity in aged rat vasculature linked to endothelial dysfunction may be mitigated, at least in part, via aldose reductase inhibitors and that aging-linked increased flux via aldose reductase generates advanced glycation endproducts, species which transduce endothelial injury consequent to their interaction with RAGE, the soluble form of the chief signal transduction receptors of advanced glycation products
physiological function
-
the enzyme is involved in sorbitol accumulation in red blood cells after peroxide, e.g. 2,2'-azobis(2-amidinopropane) hydrochloride and tert-butyl hydroperoxide, induced hemolysis, overview
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). ALDR_RAT
316
0
35797
Swiss-Prot
other Location (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
monomer
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
docking studies of rhodanine-3-hippuric acid and its benzylidene derivatives
-
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
-
molecular docking predicts the binding sites between aldose reductase and gigantol to be residues Trp111, His110, Tyr48 and Trp20
-
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
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
mutation of residues Trp111, His110, Tyr48 or Trp20 leads to a significant reduction in aldose reductase activity
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
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
native enzyme partially from lens by ammonium sulfate fractionation and dialysis
native enzyme partially from left ventricular tissue, by ultracentrifugation and gel filtration
-
Q-Sepharose column chromatography, Sephadex G-100 gel filtration, and Red-Sepharose column chromatography
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
medicine
medicine
-
inhibition of enzyme by zolrestat attenuates apoptosis in sorbitol-treated cells. Hyperosmolarity-induced cell death requires induction of enzyme as well as a decrease in intracellular glutathione levels
medicine
-
inhibition of enzyme inhibits vascular smooth muscle cell growth upon injuries via a decrease in activity of transcription factor NF-kappaB
medicine
-
myocardial enzyme activity is increased during ischemia, partially due to activation by nitric oxide, enzyme inhibition increases glycolysis and glucose oxidation
medicine
-
treatment with the nitric oxide synthase inhibitor, N-nitro-L-arginine methyl ester prevented ischemia-induced aldose reductase activation and myocardial sorbitol accumulation in rat hearts subjected to global ischemia ex vivo or coronary ligation in situ, whereas inhibition of inducible nitric oxide synthase and neuronal nitric oxide synthase have no effect. Activation of aldose reductase in the ischemic heart is abolished by pretreatment with peroxynitrite scavengers hesperetin or 5,10,15,20-tetrakis-[4-sulfonatophenyl]-porphyrinato-iron [III]
medicine
-
inhibition of aldose reductase may represent a useful strategy for treating vascular inflammation associated with diabetes
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Cromlish, J.A.; Flynn, T.G.
Purification and characterization of two aldose reductase isoenzymes from rabbit muscle
J. Biol. Chem.
258
3416-3424
1983
Bos taurus, Oryctolagus cuniculus, Rattus norvegicus, Sus scrofa
Sato, S.; Old, S.; Carper, D.; Kador, P.F.
Purification and characterization of recombinant human placental and rat lens aldose reductases expressed in Escherichia coli
Adv. Exp. Med. Biol.
5
259-268
1995
Homo sapiens, Rattus norvegicus
Inazu, N.; Nagashima, Y.; Satoh, T.; Fujii, T.
Purification and properties of six aldo-keto reductases from rat adrenal gland
J. Biochem.
115
991-999
1994
Rattus norvegicus
Da Settimo, F.; Primofiore, G.; La Motta, C.; Salerno, S.; Novellino, E.; Greco, G.; Lavecchia, A.; Laneri, S.; Boldrini, E.
Spirohydantoin derivatives of thiopyrano[2,3-b]pyridin-4(4H)-one as potent in vitro and in vivo aldose reductase inhibitors
Bioorg. Med. Chem.
13
491-499
2005
Rattus norvegicus
Yabe-Nishimura, C.; Nishinaka, T.; Iwata, K.; Seo, H.G.
Up-regulation of aldose reductase by the substrate, methylglyoxal
Chem. Biol. Interact.
143-144
317-323
2003
Rattus norvegicus
Srivastava, S.K.; Ramana, K.V.; Chandra, D.; Srivastava, S.; Bhatnagar, A.
Regulation of aldose reductase and the polyol pathway activity by nitric oxide
Chem. Biol. Interact.
143-144
333-340
2003
Homo sapiens, Rattus norvegicus
Hwang, Y.C.; Sato, S.; Tsai, J.Y.; Yan, S.; Bakr, S.; Zhang, H.; Oates, P.J.; Ramasamy, R.
Aldose reductase activation is a key component of myocardial response to ischemia
FASEB J.
16
243-245
2002
Rattus norvegicus
Lee, H.S.
Rat lens aldose reductase inhibitory activities of Coptis japonica root-derived isoquinoline alkaloids
J. Agric. Food Chem.
50
7013-7016
2002
Rattus norvegicus
Ramana, K.V.; Chandra, D.; Srivastava, S.; Bhatnagar, A.; Aggarwal, B.B.; Srivastava, S.K.
Aldose reductase mediates mitogenic signaling in vascular smooth muscle cells
J. Biol. Chem.
277
32063-32070
2002
Rattus norvegicus
Cecconi, I.; Scaloni, A.; Rastelli, G.; Moroni, M.; Vilardo, P.G.; Costantino, L.; Cappiello, M.; Garland, D.; Carper, D.; Petrash, J.M.; Del Corso, A.; Mura, U.
Oxidative modification of aldose reductase induced by copper ion. Definition of the metal-protein interaction mechanism
J. Biol. Chem.
277
42017-42027
2002
Bos taurus, Homo sapiens, Rattus norvegicus
Galvez, A.S.; Ulloa, J.A.; Chiong, M.; Criollo, A.; Eisner, V.; Barros, L.F.; Lavandero, S.
Aldose reductase induced by hyperosmotic stress mediates cardiomyocyte apoptosis: differential effects of sorbitol and mannitol
J. Biol. Chem.
278
38484-38494
2003
Rattus norvegicus
Chang, K.C.; Paek, K.S.; Kim, H.J.; Lee, Y.S.; Yabe-Nishimura, C.; Seo, H.G.
Substrate-induced up-regulation of aldose reductase by methylglyoxal, a reactive oxoaldehyde elevated in diabetes
Mol. Pharmacol.
61
1184-1191
2002
Rattus norvegicus
Srivastava, S.; Ramana, K.V.; Tammali, R.; Srivastava, S.K.; Bhatnagar, A.
Contribution of aldose reductase to diabetic hyperproliferation of vascular smooth muscle cells
Diabetes
55
901-910
2006
Rattus norvegicus
Srivastava, S.; Tammali, R.; Chandra, D.; Greer, D.A.; Ramana, K.V.; Bhatnagar, A.; Srivastava, S.K.
Regulation of lens aldose reductase activity by nitric oxide
Exp. Eye Res.
81
664-672
2005
Homo sapiens, Rattus norvegicus
Hwang, Y.C.; Shaw, S.; Kaneko, M.; Redd, H.; Marrero, M.B.; Ramasamy, R.
Aldose reductase pathway mediates JAK-STAT signaling: a novel axis in myocardial ischemic injury
FASEB J.
19
795-797
2005
Homo sapiens, Rattus norvegicus
Drel, V.R.; Pacher, P.; Stevens, M.J.; Obrosova, I.G.
Aldose reductase inhibition counteracts nitrosative stress and poly(ADP-ribose) polymerase activation in diabetic rat kidney and high-glucose-exposed human mesangial cells
Free Radic. Biol. Med.
40
1454-1465
2006
Homo sapiens, Rattus norvegicus
Kaiserova, K.; Srivastava, S.; Hoetker, J.D.; Awe, S.O.; Tang, X.L.; Cai, J.; Bhatnagar, A.
Redox activation of aldose reductase in the ischemic heart
J. Biol. Chem.
281
15110-15120
2006
Homo sapiens, Rattus norvegicus
Ramana, K.V.; Bhatnagar, A.; Srivastava, S.; Yadav, U.C.; Awasthi, S.; Awasthi, Y.C.; Srivastava, S.K.
Mitogenic responses of vascular smooth muscle cells to lipid peroxidation-derived aldehyde 4-hydroxy-trans-2-nonenal (HNE): role of aldose reductase-catalyzed reduction of the HNE-glutathione conjugates in regulating cell growth
J. Biol. Chem.
281
17652-17660
2006
Rattus norvegicus
Mylari, B.L.; Armento, S.J.; Beebe, D.A.; Conn, E.L.; Coutcher, J.B.; Dina, M.S.; OGorman, M.T.; Linhares, M.C.; Martin, W.H.; Oates, P.J.; Tess, D.A.; Withbroe, G.J.; Zembrowski, W.J.
A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners
J. Med. Chem.
48
6326-6339
2005
Rattus norvegicus
Da Settimo, F.; Primofiore, G.; La Motta, C.; Sartini, S.; Taliani, S.; Simorini, F.; Marini, A.M.; Lavecchia, A.; Novellino, E.; Boldrini, E.
Naphtho[1,2-d]isothiazole acetic acid derivatives as a novel class of selective aldose reductase inhibitors
J. Med. Chem.
48
6897-6907
2005
Rattus norvegicus (P07943)
Jang, D.S.; Lee, G.Y.; Kim, Y.S.; Lee, Y.M.; Kim, C.S.; Yoo, J.L.; Kim, J.S.
Anthraquinones from the seeds of Cassia tora with inhibitory activity on protein glycation and aldose reductase
Biol. Pharm. Bull.
30
2207-2210
2007
Rattus norvegicus
Lee, Y.S.; Kang, Y.H.; Jung, J.Y.; Kang, I.J.; Han, S.N.; Chung, J.S.; Shin, H.K.; Lim, S.S.
Inhibitory constituents of aldose reductase in the fruiting body of Phellinus linteus
Biol. Pharm. Bull.
31
765-768
2008
Homo sapiens, Rattus norvegicus
Alexiou, P.; Nicolaou, I.; Stefek, M.; Kristl, A.; Demopoulos, V.J.
Design and synthesis of N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamides as aldose reductase inhibitors
Bioorg. Med. Chem.
16
3926-3932
2008
Rattus norvegicus
Stefek, M.; Snirc, V.; Djoubissie, P.O.; Majekova, M.; Demopoulos, V.; Rackova, L.; Bezakova, Z.; Karasu, C.; Carbone, V.; El-Kabbani, O.
Carboxymethylated pyridoindole antioxidants as aldose reductase inhibitors: Synthesis, activity, partitioning, and molecular modeling
Bioorg. Med. Chem.
16
4908-4920
2008
Rattus norvegicus
Bozdag-Duendar, O.; Evranos, B.; Das-Evcimen, N.; Sarikaya, M.; Ertan, R.
Synthesis and aldose reductase inhibitory activity of some new chromonyl-2,4-thiazolidinediones
Eur. J. Med. Chem.
43
2412-2417
2008
Rattus norvegicus
Das-Evcimen, N.; Bozdag-Dundar, O.; Sarikaya, M.; Ertan, R.
In vitro aldose reductase inhibitory activity of some flavonyl-2,4-thiazolidinediones
J. Enzyme Inhib. Med. Chem.
23
297-301
2008
Rattus norvegicus
Wang, S.; Yan, J.; Hao, D.; Niu, X.; Cheng, M.
Synthesis and activity of a new series of (Z)-3-phenyl-2-benzoylpropenoic acid derivatives as aldose reductase inhibitors
Molecules
12
885-895
2007
Rattus norvegicus, Homo sapiens (P15121), Homo sapiens
Chung, R.; Endo, S.; Hara, A.; El-Kabbani, O.
Crystallization and preliminary X-ray analysis of a rat aldose reductase-like protein (AKR1B14)
Acta Crystallogr. Sect. F
65
395-397
2009
Rattus norvegicus
Jung, H.A.; Yoon, N.Y.; Bae, H.J.; Min, B.S.; Choi, J.S.
Inhibitory activities of the alkaloids from Coptidis Rhizoma against aldose reductase
Arch. Pharm. Res.
31
1405-1412
2008
Homo sapiens, Rattus norvegicus
Endo, S.; Matsunaga, T.; Mamiya, H.; Hara, A.; Kitade, Y.; Tajima, K.; El-Kabbani, O.
Characterization of a rat NADPH-dependent aldo-keto reductase (AKR1B13) induced by oxidative stress
Chem. Biol. Interact.
178
151-157
2009
Rattus norvegicus
Reddy, A.B.; Ramana, K.V.; Srivastava, S.; Bhatnagar, A.; Srivastava, S.K.
Aldose reductase regulates high glucose-induced ectodomain shedding of tumor necrosis factor (TNF)-alpha via protein kinase C-delta and TNF-alpha converting enzyme in vascular smooth muscle cells
Endocrinology
150
63-74
2009
Rattus norvegicus
Lee, S.J.; Park, W.H.; Park, S.D.; Moon, H.I.
Aldose reductase inhibitors from Litchi chinensis Sonn
J. Enzyme Inhib. Med. Chem.
24
957-959
2009
Rattus norvegicus
Ha, D.T.; Ngoc, T.M.; Lee, I.; Lee, Y.M.; Kim, J.S.; Jung, H.; Lee, S.; Na, M.; Bae, K.
Inhibitors of aldose reductase and formation of advanced glycation end-products in moutan cortex (Paeonia suffruticosa)
J. Nat. Prod.
72
1465-1470
2009
Rattus norvegicus
Jung, H.A.; Yoon, N.Y.; Kang, S.S.; Kim, Y.S.; Choi, J.S.
Inhibitory activities of prenylated flavonoids from Sophora flavescens against aldose reductase and generation of advanced glycation endproducts
J. Pharm. Pharmacol.
60
1227-1236
2008
Homo sapiens, Rattus norvegicus
Hallam, K.M.; Li, Q.; Ananthakrishnan, R.; Kalea, A.; Zou, Y.S.; Vedantham, S.; Schmidt, A.M.; Yan, S.F.; Ramasamy, R.
Aldose reductase and AGE-RAGE pathways: central roles in the pathogenesis of vascular dysfunction in aging rats
Aging Cell
9
776-784
2010
Rattus norvegicus
Kim, N.H.; Kim, Y.S.; Lee, Y.M.; Jang, D.S.; Kim, J.S.
Inhibition of aldose reductase and xylose-induced lens opacity by puerariafuran from the roots of Pueraria lobata
Biol. Pharm. Bull.
33
1605-1609
2010
Rattus norvegicus
Lee, Y.S.; Kim, S.H.; Jung, S.H.; Kim, J.K.; Pan, C.H.; Lim, S.S.
Aldose reductase inhibitory compounds from Glycyrrhiza uralensis
Biol. Pharm. Bull.
33
917-921
2010
Homo sapiens, Rattus norvegicus
Kato, A.; Kobayashi, K.; Narukawa, K.; Minoshima, Y.; Adachi, I.; Hirono, S.; Nash, R.J.
6,7-Dihydroxy-4-phenylcoumarin as inhibitor of aldose reductase 2
Bioorg. Med. Chem. Lett.
20
5630-5633
2010
Rattus norvegicus
Pegklidou, K.; Koukoulitsa, C.; Nicolaou, I.; Demopoulos, V.J.
Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole
Bioorg. Med. Chem.
18
2107-2114
2010
Rattus norvegicus
Tammali, R.; Saxena, A.; Srivastava, S.K.; Ramana, K.V.
Aldose reductase regulates vascular smooth muscle cell proliferation by modulating G1/S phase transition of cell cycle
Endocrinology
151
2140-2150
2010
Rattus norvegicus
Obrosova, I.G.; Maksimchyk, Y.; Pacher, P.; Agardh, E.; Smith, M.L.; El-Remessy, A.B.; Agardh, C.D.
Evaluation of the aldose reductase inhibitor fidarestat on ischemia-reperfusion injury in rat retina
Int. J. Mol. Med.
26
135-142
2010
Rattus norvegicus
Xu, Z.; Yang, H.; Zhou, M.; Feng, Y.; Jia, W.
Inhibitory effect of total lignan from fructus Arctii on aldose reductase
Phytother. Res.
24
472-473
2010
Rattus norvegicus
Stefek, M.; Tsantili-Kakoulidou, A.; Milackova, I.; Juskova, M.; Snirc, V.; Triantos, N.
(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
Bioorg. Med. Chem.
19
7181-7185
2011
Rattus norvegicus, Rattus norvegicus Wistar
Yang, Y.; Zhang, S.; Wu, B.; Ma, M.; Chen, X.; Qin, X.; He, M.; Hussain, S.; Jing, C.; Ma, B.; Zhu, C.
An efficient synthesis of quinoxalinone derivatives as potent inhibitors of aldose reductase
ChemMedChem
7
823-835
2012
Rattus norvegicus, Rattus norvegicus Wistar
Zheng, X.; Zhang, L.; Chen, W.; Chen, Y.; Xie, W.; Hu, X.
Partial inhibition of aldose reductase by nitazoxanide and its molecular basis
ChemMedChem
7
1921-1923
2012
Rattus norvegicus
Ramunno, A.; Cosconati, S.; Sartini, S.; Maglio, V.; Angiuoli, S.; La Pietra, V.; Di Maro, S.; Giustiniano, M.; La Motta, C.; Da Settimo, F.; Marinelli, L.; Novellino, E.
Progresses in the pursuit of aldose reductase inhibitors: the structure-based lead optimization step
Eur. J. Med. Chem.
51
216-226
2012
Rattus norvegicus, Rattus norvegicus Sprague-Dawley
Nakamura, S.; Fujimoto, K.; Matsumoto, T.; Ohta, T.; Ogawa, K.; Tamura, H.; Matsuda, H.; Yoshikawa, M.
Structures of acylated sucroses and an acylated flavonol glycoside and inhibitory effects of constituents on aldose reductase from the flower buds of Prunus mume
J. Nat. Med.
67
799-806
2013
Rattus norvegicus
Hussain, S.; Parveen, S.; Hao, X.; Zhang, S.; Wang, W.; Qin, X.; Yang, Y.; Chen, X.; Zhu, S.; Zhu, C.; Ma, B.
Structure-activity relationships studies of quinoxalinone derivatives as aldose reductase inhibitors
Eur. J. Med. Chem.
80
383-392
2014
Rattus norvegicus (P07943), Rattus norvegicus Wistar (P07943)
Qin, X.; Hao, X.; Han, H.; Zhu, S.; Yang, Y.; Wu, B.; Hussain, S.; Parveen, S.; Jing, C.; Ma, B.; Zhu, C.
Design and synthesis of potent and multifunctional aldose reductase inhibitors based on quinoxalinones
J. Med. Chem.
58
1254-1267
2015
Rattus norvegicus (P07943), Rattus norvegicus Wistar (P07943)
Lee, I.S.; Kim, Y.J.; Jung, S.H.; Kim, J.H.; Kim, J.S.
Flavonoids from Litsea japonica inhibit AGEs formation and rat lense aldose reductase in vitro and vessel dilation in zebrafish
Planta Med.
83
318-325
2016
Rattus norvegicus (P07943)
Celestina, S.; Sundaram, K.; Ravi, S.
In vitro studies of potent aldose reductase inhibitors Synthesis, characterization, biological evaluation and docking analysis of rhodanine-3-hippuric acid derivatives
Bioorg. Chem.
97
103640
2020
Rattus norvegicus
Hlavac, M.; Kovacikova, L.; Soltesova Prnova, M.; Addova, G.; Hanquet, G.; Stefek, M.; Bohac, A.
Novel substituted N-benzyl(oxotriazinoindole) inhibitors of aldose reductase exploiting ALR2 unoccupied interactive pocket
Bioorg. Med. Chem.
29
115885
2021
Rattus norvegicus
Papastavrou, N.; Chatzopoulou, M.; Ballekova, J.; Cappiello, M.; Moschini, R.; Balestri, F.; Patsilinakos, A.; Ragno, R.; Stefek, M.; Nicolaou, I.
Enhancing activity and selectivity in a series of pyrrol-1-yl-1-hydroxypyrazole-based aldose reductase inhibitors The case of trifluoroacetylation
Eur. J. Med. Chem.
130
328-335
2017
Rattus norvegicus, Homo sapiens (P15121)
Yang, Y.; Yang, Q.; Yu, J.; Wan, W.; Wei, X.
Characterization of structural requirement for binding of gigantol and aldose reductase
Front. Biosci. (Landmark Ed.)
24
1024-1036
2019
Rattus norvegicus
Alim, Z.; Kilinc, N.; Sengul, B.; Beydemir, S.
Mechanism of capsaicin inhibition of aldose reductase activity
J. Biochem. Mol. Toxicol.
31
e21898
2017
Rattus norvegicus
Lee, H.E.; Kim, J.A.; Whang, W.K.
Chemical constituents of smilax China l. stems and their inhibitory activities against glycation, aldose reductase, alpha-glucosidase, and lipase
Molecules
22
451
2017
Rattus norvegicus
Celestina, S.K.; Sundaram, K.; Ravi, S.
Novel derivatives of rhodanine-3-hippuric acid as active inhibitors of aldose reductase synthesis, biological evaluation, and molecular docking analysis
Russ. J. Bioorg. Chem.
45
405-415
2019
Rattus norvegicus
-
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