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Literature summary for 2.3.2.13 extracted from

  • Pardin, C.; Roy, I.; Lubell, W.D.; Keillor, J.W.
    Reversible and competitive cinnamoyl triazole inhibitors of tissue transglutaminase (2008), Chem. Biol. Drug Des., 72, 189-196.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli, with N-terminal His-tag Cavia cutleri

Inhibitors

Inhibitors Comment Organism Structure
(E)-1-(1-(2-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
Cavia cutleri
(E)-1-(1-(3-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
Cavia cutleri
(E)-1-(1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
Cavia cutleri
(E)-1-(1-(cyclohexylmethyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
Cavia cutleri
(E)-1-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
Cavia cutleri

Organism

Organism UniProt Comment Textmining
Cavia cutleri P08587
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Cbz-L-Glu(gamma-p-nitrophenyl ester)-Gly + ?
-
Cavia cutleri ?
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0021
-
25°C, pH 7.0 Cavia cutleri (E)-1-(1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
0.0043
-
25°C, pH 7.0 Cavia cutleri (E)-1-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
0.0094
-
25°C, pH 7.0 Cavia cutleri (E)-1-(1-(3-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
0.0107
-
25°C, pH 7.0 Cavia cutleri (E)-1-(1-(2-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
0.011
-
25°C, pH 7.0 Cavia cutleri (E)-1-(1-(cyclohexylmethyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one