Literature summary for 2.3.2.13 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.

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Inhibitors

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

Organism

Organism	UniProt	Comment	Textmining
Cavia porcellus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
liver	-	Cavia porcellus	-

IC50 Value

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

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Release 2023.1 (January 2023)