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Literature summary for 1.1.1.2 extracted from

  • Stefek, M.; Soltesova Prnova, M.; Majekova, M.; Rechlin, C.; Heine, A.; Klebe, G.
    Identification of novel aldose reductase inhibitors based on carboxymethylated mercaptotriazinoindole scaffold (2015), J. Med. Chem., 58, 2649-2657.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(1H-indol-1-yl)acetic acid
-
Rattus norvegicus
(2,3-dihydrocyclopenta[b]indol-4(1H)-yl)acetic acid
-
Rattus norvegicus
(3-sulfanyl-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
-
Rattus norvegicus
(3-[[(2-fluorophenyl)methyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
-
Rattus norvegicus
(3-[[2-oxo-2-(2,4,6-trimethylanilino)ethyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
-
Rattus norvegicus
(4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indol-5-yl)acetic acid
-
Rattus norvegicus
(6H-indolo[2,3-b]quinoxalin-6-yl)acetic acid
-
Rattus norvegicus
(7H-indolo[2',3':5,6][1,2,4]triazino[2,3-a]benzimidazol-7-yl)acetic acid
-
Rattus norvegicus
(8-methyl-3-[[2-oxo-2-(propylamino)ethyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
-
Rattus norvegicus
2,5-dihydro-3H-[1,2,4]triazino[5,6-b]indole-3-thione
-
Rattus norvegicus
3-(1H-indol-1-yl)propanoic acid
-
Rattus norvegicus
3-[3-[(diethylamino)methyl]-1H-indol-1-yl]propanoic acid
-
Rattus norvegicus
lidorestat binding mode, overview Rattus norvegicus
additional information identification of aldose reductase inhibitors based on carboxymethylated mercaptotriazinoindole scaffold, the compouds have also lower inhibitory potency against aldehyde reductase, structure-activity relationships, overview Rattus norvegicus
[(5H-[1,2,4]triazino[5,6-b]indol-3-yl)sulfanyl]acetic acid
-
Rattus norvegicus
[3-(2,2-dimethylpropanoyl)-1H-indol-1-yl]acetic acid
-
Rattus norvegicus
[3-[(diethylamino)methyl]-1H-indol-1-yl]acetic acid
-
Rattus norvegicus
[3-[(dimethylamino)methyl]-2-methyl-1H-indol-1-yl]acetic acid
-
Rattus norvegicus
[3-[(morpholin-4-yl)methyl]-1H-indol-1-yl]acetic acid
-
Rattus norvegicus
[3-[(propan-2-yl)sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
-
Rattus norvegicus
[3-[(pyrrolidin-1-yl)methyl]-1H-indol-1-yl]acetic acid
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
D-glucuronate + NADPH + H+ Rattus norvegicus
-
? + NADP+
-
r
D-glucuronate + NADPH + H+ Rattus norvegicus Wistar
-
? + NADP+
-
r

Organism

Organism UniProt Comment Textmining
Rattus norvegicus P07943
-
-
Rattus norvegicus Wistar P07943
-
-

Purification (Commentary)

Purification (Comment) Organism
native enzyme partially from lens and kidney Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
Rattus norvegicus
-
lens
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-glucuronate + NADPH + H+
-
Rattus norvegicus ? + NADP+
-
r
D-glucuronate + NADPH + H+
-
Rattus norvegicus Wistar ? + NADP+
-
r

Synonyms

Synonyms Comment Organism
AKR1A1
-
Rattus norvegicus
aldehyde reductase
-
Rattus norvegicus
ALR1
-
Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0012
-
pH and temperature not specified in the publication Rattus norvegicus (3-[[(2-fluorophenyl)methyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
0.0048
-
pH and temperature not specified in the publication Rattus norvegicus (2,3-dihydrocyclopenta[b]indol-4(1H)-yl)acetic acid
0.0067
-
pH and temperature not specified in the publication Rattus norvegicus 3-[3-[(diethylamino)methyl]-1H-indol-1-yl]propanoic acid
0.0118
-
pH and temperature not specified in the publication Rattus norvegicus 3-(1H-indol-1-yl)propanoic acid
0.0141
-
pH and temperature not specified in the publication Rattus norvegicus [3-[(propan-2-yl)sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
0.0151
-
pH and temperature not specified in the publication Rattus norvegicus (7H-indolo[2',3':5,6][1,2,4]triazino[2,3-a]benzimidazol-7-yl)acetic acid
0.0192
-
pH and temperature not specified in the publication Rattus norvegicus [3-[(pyrrolidin-1-yl)methyl]-1H-indol-1-yl]acetic acid
0.0196
-
pH and temperature not specified in the publication Rattus norvegicus (8-methyl-3-[[2-oxo-2-(propylamino)ethyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
0.0223
-
pH and temperature not specified in the publication Rattus norvegicus [3-[(dimethylamino)methyl]-2-methyl-1H-indol-1-yl]acetic acid
0.0235
-
pH and temperature not specified in the publication Rattus norvegicus (3-[[2-oxo-2-(2,4,6-trimethylanilino)ethyl]sulfanyl]-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
0.0248
-
pH and temperature not specified in the publication Rattus norvegicus (6H-indolo[2,3-b]quinoxalin-6-yl)acetic acid
0.0325
-
pH and temperature not specified in the publication Rattus norvegicus [3-[(morpholin-4-yl)methyl]-1H-indol-1-yl]acetic acid
0.0381
-
pH and temperature not specified in the publication Rattus norvegicus [3-[(diethylamino)methyl]-1H-indol-1-yl]acetic acid
0.0406
-
pH and temperature not specified in the publication Rattus norvegicus (3-sulfanyl-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid
0.049
-
pH and temperature not specified in the publication Rattus norvegicus (4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indol-5-yl)acetic acid
0.0684
-
pH and temperature not specified in the publication Rattus norvegicus [3-(2,2-dimethylpropanoyl)-1H-indol-1-yl]acetic acid
0.0802
-
pH and temperature not specified in the publication Rattus norvegicus (1H-indol-1-yl)acetic acid