Literature summary for 1.1.1.21 extracted from

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 (2021), Bioorg. Med. Chem., 29, 115885 .

Search for more literature for 1.1.1.21

Inhibitors

Inhibitors	Comment	Organism	Structure
(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	Rattus norvegicus
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	Rattus norvegicus
additional information	synthesis of oxotriazinoindole inhibitors	Rattus norvegicus
[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	Rattus norvegicus
[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	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Rattus norvegicus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
lens	-	Rattus norvegicus	-

Synonyms

Synonyms	Comment	Organism
ALR2	-	Rattus norvegicus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000076	-	pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	[2-[(2-cyanophenyl)methyl]-3-oxo-2,3-dihydro-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
0.000139	-	pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	2-[[5-(carboxymethyl)-3-oxo-3,5-dihydro-2H-[1,2,4]triazino[5,6-b]indol-2-yl]methyl]benzoic acid
0.000234	-	pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	[2-[(2-carbamoylphenyl)methyl]-3-oxo-2,3-dihydro-5H-[1,2,4]triazino[5,6-b]indol-5-yl]acetic acid
0.000241	-	pH not specified in the publication, temperature not specified in the publication	Rattus norvegicus	(2-[[2-(hydroxymethyl)phenyl]methyl]-3-oxo-2,3-dihydro-5H-[1,2,4]triazino[5,6-b]indol-5-yl)acetic acid

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Release 2023.1 (January 2023)