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Literature summary for 1.13.11.33 extracted from

  • Tsai, W.C.; Gilbert, N.C.; Ohler, A.; Armstrong, M.; Perry, S.; Kalyanaraman, C.; Yasgar, A.; Rai, G.; Simeonov, A.; Jadhav, A.; Standley, M.; Lee, H.W.; Crews, P.; Iavarone, A.T.; Jacobson, M.P.; Neau, D.B.; Offenbacher, A.R.; Newcomer, M.; Holman, T.R.
    Kinetic and structural investigations of novel inhibitors of human epithelial 15-lipoxygenase-2 (2021), Bioorg. Med. Chem., 46, 116349 .
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-phenyl-2-([[4-(trifluoromethyl)phenyl]methyl]sulfanyl)-1H-imidazole mixed-type inhibitor, performs as potent inhibitor in a HEK-293 cell-based assay and binds in the U-shaped channel of 15-Lox-2 Homo sapiens
2-(4-chlorophenyl)-5-cyclohexyl-1,3,4-oxadiazole mixed-type inhibitor, performs as potent inhibitor in a HEK-293 cell-based assay and binds in the U-shaped channel of 15-Lox-2 Homo sapiens
2-[[(4-bromophenyl)methyl]sulfanyl]-1-phenyl-1H-imidazole mixed-type inhibitor, performs as potent inhibitor in a HEK-293 cell-based assay and binds in the U-shaped channel of 15-Lox-2 Homo sapiens
2-[[(4-ethylphenyl)methyl]sulfanyl]-1-phenyl-1H-imidazole mixed-type inhibitor, performs as potent inhibitor in a HEK-293 cell-based assay and binds in the U-shaped channel of 15-Lox-2 Homo sapiens
3-[[(4-methylphenyl)methyl]sulfanyl]-1-phenyl-1H-1,2,4-triazole mixed-type inhibitor, performs as potent inhibitor in a HEK-293 cell-based assay and binds in the U-shaped channel of 15-Lox-2 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O15296
-
-

Source Tissue

Source Tissue Comment Organism Textmining
epithelium
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
15-lipoxygenase-2
-
Homo sapiens
ALOX15B
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00034
-
pH 7.5, 23°C Homo sapiens 1-phenyl-2-([[4-(trifluoromethyl)phenyl]methyl]sulfanyl)-1H-imidazole
0.00053
-
pH 7.5, 23°C Homo sapiens 2-[[(4-bromophenyl)methyl]sulfanyl]-1-phenyl-1H-imidazole
0.00087
-
pH 7.5, 23°C Homo sapiens 2-[[(4-ethylphenyl)methyl]sulfanyl]-1-phenyl-1H-imidazole
0.0026
-
pH 7.5, 23°C Homo sapiens 2-(4-chlorophenyl)-5-cyclohexyl-1,3,4-oxadiazole
0.0031
-
pH 7.5, 23°C Homo sapiens 3-[[(4-methylphenyl)methyl]sulfanyl]-1-phenyl-1H-1,2,4-triazole