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Literature summary for 2.4.1.255 extracted from

  • Wang, Y.; Zhu, J.; Zhang, L.
    Discovery of cell-permeable O-GlcNAc transferase inhibitors via tethering in situ click chemistry (2017), J. Med. Chem., 60, 263-272 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-(4-acetamidophenyl)-4-(diphenylhydroxymethyl)-1H-1,2,3-triazole
-
Homo sapiens
1-(4-acetamidophenyl)-4-(naphthalen-2-yl)-1H-1,2,3-triazole i.e. APNT, cell-permeable inhibitor, able to inhibit OGlcNAcylation in cells without significant effects on cell viability Homo sapiens
1-(4-acetamidophenyl)-4-([1,1'-biphenyl]-4-yl)-1H-1,2,3-triazole i.e. APBT, cell-permeable inhibitor, able to inhibit OGlcNAcylation in cells without significant effects on cell viability Homo sapiens
1-(4-chloroacetamidophenyl)-4-(diphenylhydroxymethyl)-1H-1,2,3-triazole
-
Homo sapiens
1-(4-chloroacetamidophenyl)-4-(naphthalen-2-yl)-1H-1,2,3-triazole
-
Homo sapiens
1-(4-chloroacetamidophenyl)-4-([1,1'-biphenyl]-4-yl)-1H-1,2,3-triazole
-
Homo sapiens
4-azidoiodoacetanilide
-
Homo sapiens
benzoxazolinone
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O15294
-
-

Synonyms

Synonyms Comment Organism
O-GlcNAc transferase
-
Homo sapiens
OGT
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0119
-
pH 7.4, 37°C Homo sapiens benzoxazolinone
0.0667
-
pH 7.4, 37°C Homo sapiens 1-(4-acetamidophenyl)-4-(naphthalen-2-yl)-1H-1,2,3-triazole
0.0717
-
pH 7.4, 37°C Homo sapiens 1-(4-chloroacetamidophenyl)-4-(naphthalen-2-yl)-1H-1,2,3-triazole
0.0893
-
pH 7.4, 37°C Homo sapiens 1-(4-chloroacetamidophenyl)-4-(diphenylhydroxymethyl)-1H-1,2,3-triazole
0.0912
-
pH 7.4, 37°C Homo sapiens 1-(4-chloroacetamidophenyl)-4-([1,1'-biphenyl]-4-yl)-1H-1,2,3-triazole
0.139
-
pH 7.4, 37°C Homo sapiens 1-(4-acetamidophenyl)-4-([1,1'-biphenyl]-4-yl)-1H-1,2,3-triazole
0.865
-
pH 7.4, 37°C Homo sapiens 4-azidoiodoacetanilide
1.001
-
pH 7.4, 37°C Homo sapiens 1-(4-acetamidophenyl)-4-(diphenylhydroxymethyl)-1H-1,2,3-triazole

General Information

General Information Comment Organism
physiological function key enzyme involved in dynamic O-GlcNAcylation of nuclear and cytoplasmic proteins Homo sapiens