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Literature summary extracted from

  • Ozaki, S.; Ebisui, E.; Hamada, K.; Goto, J.; Suzuki, A.Z.; Terauchi, A.; Mikoshiba, K.
    Potent transglutaminase inhibitors, aryl beta-aminoethyl ketones (2010), Bioorg. Med. Chem. Lett., 20, 1141-1144.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.2.13 1-(1-benzothiophen-2-yl)-3-[benzyl(tert-butyl)amino]propan-1-one
-
 Cavia porcellus
2.3.2.13 1-(furan-2-yl)-3-[(2-hydroxyethyl)(propan-2-yl)amino]propan-1-one
-
 Cavia porcellus
2.3.2.13 3-[benzyl(ethyl)amino]-1-(5-chlorothiophen-2-yl)propan-1-one
-
 Cavia porcellus
2.3.2.13 3-[benzyl(propan-2-yl)amino]-1-(5-bromothiophen-2-yl)propan-1-one
-
 Cavia porcellus
2.3.2.13 3-[benzyl(propan-2-yl)amino]-1-(5-chlorothiophen-2-yl)propan-1-one
-
 Cavia porcellus
2.3.2.13 3-[benzyl(tert-butyl)amino]-1-(4-nitrophenyl)propan-1-one
-
 Cavia porcellus
2.3.2.13 3-[benzyl(tert-butyl)amino]-1-(5-bromothiophen-2-yl)propan-1-one
-
 Cavia porcellus
2.3.2.13 3-[benzyl(tert-butyl)amino]-1-(5-chlorothiophen-2-yl)propan-1-one
-
 Cavia porcellus
2.3.2.13 3-[benzyl(tert-butyl)amino]-1-(thiophen-2-yl)propan-1-one
-
 Cavia porcellus
2.3.2.13 3-[bis(2-hydroxyethyl)amino]-1-(furan-2-yl)propan-1-one
-
 Cavia porcellus
2.3.2.13 additional information beta-aminoethyl ketones strongly inhibit TGase, alpha- and gamma-aminoalkyl ketones show very weak TGase inhibition Cavia porcellus

Organism

EC Number Organism UniProt Comment Textmining
2.3.2.13 Cavia porcellus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.2.13 liver
-
 Cavia porcellus
-

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.2.13 0.000081
-
 pH 7.5 Cavia porcellus 3-[benzyl(tert-butyl)amino]-1-(5-bromothiophen-2-yl)propan-1-one
2.3.2.13 0.0001
-
 pH 7.5 Cavia porcellus 3-[benzyl(tert-butyl)amino]-1-(5-chlorothiophen-2-yl)propan-1-one
2.3.2.13 0.00012
-
 pH 7.5 Cavia porcellus 1-(furan-2-yl)-3-[(2-hydroxyethyl)(propan-2-yl)amino]propan-1-one
2.3.2.13 0.00017
-
 pH 7.5 Cavia porcellus 3-[benzyl(tert-butyl)amino]-1-(4-nitrophenyl)propan-1-one
2.3.2.13 0.00019
-
 pH 7.5 Cavia porcellus 3-[benzyl(propan-2-yl)amino]-1-(5-bromothiophen-2-yl)propan-1-one
2.3.2.13 0.00021
-
 pH 7.5 Cavia porcellus 1-(1-benzothiophen-2-yl)-3-[benzyl(tert-butyl)amino]propan-1-one
2.3.2.13 0.00023
-
 pH 7.5 Cavia porcellus 3-[benzyl(propan-2-yl)amino]-1-(5-chlorothiophen-2-yl)propan-1-one
2.3.2.13 0.00036
-
 pH 7.5 Cavia porcellus 3-[bis(2-hydroxyethyl)amino]-1-(furan-2-yl)propan-1-one
2.3.2.13 0.00042
-
 pH 7.5 Cavia porcellus 3-[benzyl(ethyl)amino]-1-(5-chlorothiophen-2-yl)propan-1-one
2.3.2.13 0.00044
-
 pH 7.5 Cavia porcellus 3-[benzyl(tert-butyl)amino]-1-(thiophen-2-yl)propan-1-one