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Literature summary extracted from

  • Wodtke, R.; Hauser, C.; Ruiz-Gomez, G.; Jaeckel, E.; Bauer, D.; Lohse, M.; Wong, A.; Pufe, J.; Ludwig, F.A.; Fischer, S.; Hauser, S.; Greif, D.; Pisabarro, M.T.; Pietzsch, J.; Pietsch, M.; Loeser, R.
    Nepsilon-acryloyllysine piperazides as irreversible inhibitors of transglutaminase 2 synthesis, structure-activity relationships, and pharmacokinetic profiling (2018), J. Med. Chem., 61, 4528-4560 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.2.13 1-(6-methylpyridin-2-yl)piperazine
-
 Cavia porcellus
2.3.2.13 1-(6-methylpyridin-2-yl)piperazine
-
 Homo sapiens
2.3.2.13 1-(6-nitropyridin-3-yl)piperazine
-
 Cavia porcellus
2.3.2.13 1-(6-nitropyridin-3-yl)piperazine
-
 Homo sapiens
2.3.2.13 3-iodo-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
 Cavia porcellus
2.3.2.13 3-iodo-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
 Homo sapiens
2.3.2.13 4-fluoro-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
 Cavia porcellus
2.3.2.13 4-fluoro-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
 Homo sapiens
2.3.2.13 4-fluoro-N-[(2S)-1-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
 Cavia porcellus
2.3.2.13 4-fluoro-N-[(2S)-1-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
 Homo sapiens
2.3.2.13 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxamide
-
 Cavia porcellus
2.3.2.13 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxamide
-
 Homo sapiens
2.3.2.13 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylic acid
-
 Cavia porcellus
2.3.2.13 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylic acid
-
 Homo sapiens
2.3.2.13 methyl 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylate
-
 Cavia porcellus
2.3.2.13 methyl 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylate
-
 Homo sapiens
2.3.2.13 additional information Nepsilon-acryloyllysine piperazides as irreversible inhibitors of transglutaminase 2, synthesis, structure-activity relationships, and pharmacokinetic profiling, overview. No inhibition by N-[(5R)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide Cavia porcellus
2.3.2.13 additional information Nepsilon-acryloyllysine piperazides as irreversible inhibitors of transglutaminase 2, synthesis, structure-activity relationships, and pharmacokinetic profiling, overview. No inhibition by N-[(5R)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide Homo sapiens
2.3.2.13 N,N-dimethyl-5-(piperazine-1-sulfonyl)naphthalen-1-amine
-
 Cavia porcellus
2.3.2.13 N,N-dimethyl-5-(piperazine-1-sulfonyl)naphthalen-1-amine
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-(2-cyclohexylacetamido)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-(2-cyclohexylacetamido)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[2-(4-bromophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[2-(4-bromophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[2-(4-chlorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[2-(4-chlorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[2-(4-iodophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[2-(4-iodophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[2-(4-methylphenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[2-(4-methylphenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[[(4-fluorophenyl)carbamothioyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[[(4-fluorophenyl)carbamothioyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[[(4-fluorophenyl)carbamoyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[[(4-fluorophenyl)carbamoyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[[(4-fluorophenyl)methyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[[(4-fluorophenyl)methyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-5-[[5-(dimethylamino)naphthalene-1-sulfonyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-5-[[5-(dimethylamino)naphthalene-1-sulfonyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-(4-phenylpiperazin-1-yl)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-(4-phenylpiperazin-1-yl)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-3-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-3-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-4-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-4-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-[6-(trifluoromethyl)pyridin-3-yl]piperazin-1-yl]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-[6-(trifluoromethyl)pyridin-3-yl]piperazin-1-yl]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-oxo-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]-5-(2,2,2-trifluoroacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-oxo-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]-5-(2,2,2-trifluoroacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(3-methylphenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(3-methylphenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(4-fluorobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(4-fluorobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(4-nitrobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(4-nitrobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(4-nitrophenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(4-nitrophenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-chloropyridine-2-carbonyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-chloropyridine-2-carbonyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide determination of the thermodynamic solubility of the compound Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide determination of the thermodynamic solubility of the compound Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-fluoropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-fluoropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide reversible inhibitor Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide reversible inhibitor Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamothioyl)amino]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamothioyl)amino]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylmethanesulfonyl)amino]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylmethanesulfonyl)amino]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(pyridin-2-yl)acetamido]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(pyridin-2-yl)acetamido]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-2-yl)acetamido]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-2-yl)acetamido]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-3-yl)acetamido]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-3-yl)acetamido]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide determination of the thermodynamic solubility of the compound Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide determination of the thermodynamic solubility of the compound Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Mus musculus
2.3.2.13 N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide reversible inhibitor Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide reversible inhibitor Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Mus musculus
2.3.2.13 N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-(6-tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-(6-tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 N-[(5S)-6-[4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Cavia porcellus
2.3.2.13 N-[(5S)-6-[4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(4-fluorobenzoyl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(4-fluorobenzoyl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(6-chloropyridine-2-carbonyl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(6-chloropyridine-2-carbonyl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(6-fluoropyridin-2-yl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(6-fluoropyridin-2-yl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(6-fluoropyridin-3-yl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(6-fluoropyridin-3-yl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(6-iodopyridin-2-yl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(6-iodopyridin-2-yl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(6-nitropyridin-2-yl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(6-nitropyridin-2-yl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(6-phenylpyridin-2-yl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(6-phenylpyridin-2-yl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(6-tert-butylpyridin-2-yl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(6-tert-butylpyridin-2-yl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-(pyridin-3-yl)piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-(pyridin-3-yl)piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-[(4-fluorophenyl)methyl]piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-[(4-fluorophenyl)methyl]piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-[6-(methoxycarbonyl)pyridin-3-yl]piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-[6-(methoxycarbonyl)pyridin-3-yl]piperazine-1-carboxylate
-
 Homo sapiens
2.3.2.13 tert-butyl 4-[6-(trifluoromethyl)pyridin-3-yl]piperazine-1-carboxylate
-
 Cavia porcellus
2.3.2.13 tert-butyl 4-[6-(trifluoromethyl)pyridin-3-yl]piperazine-1-carboxylate
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.3.2.13 additional information
-
 additional information kinetics of Z-Glu(HMC)-Gly-OH hydrolysis Homo sapiens
2.3.2.13 additional information
-
 additional information kinetics of Z-Glu(HMC)-Gly-OH hydrolysis Cavia porcellus
2.3.2.13 additional information
-
 additional information kinetics of Z-Glu(HMC)-Gly-OH hydrolysis Mus musculus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.3.2.13 Ca2+ required Homo sapiens
2.3.2.13 Ca2+ required Cavia porcellus
2.3.2.13 Ca2+ required Mus musculus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.2.13 protein glutamine + alkylamine Homo sapiens
-
 protein N5-alkylglutamine + NH3
-
 ?
2.3.2.13 protein glutamine + alkylamine Cavia porcellus
-
 protein N5-alkylglutamine + NH3
-
 ?
2.3.2.13 protein glutamine + alkylamine Mus musculus
-
 protein N5-alkylglutamine + NH3
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.3.2.13 Cavia porcellus H0VXN6
-
-
2.3.2.13 Homo sapiens O95932
-
-
2.3.2.13 Homo sapiens P00488
-
-
2.3.2.13 Homo sapiens P21980
-
-
2.3.2.13 Homo sapiens P22735
-
-
2.3.2.13 Homo sapiens Q08188
-
-
2.3.2.13 Mus musculus P21981
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.2.13 A-375 cell
-
 Homo sapiens
-
2.3.2.13 MeWo cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.2.13 additional information measurement of enzyme-catalyzed hydrolysis reactions of water-soluble fluorogenic acyl donor Z-Glu(HMC)-Gly-OH Homo sapiens ?
-
-
2.3.2.13 additional information measurement of enzyme-catalyzed hydrolysis reactions of water-soluble fluorogenic acyl donor Z-Glu(HMC)-Gly-OH Cavia porcellus ?
-
-
2.3.2.13 additional information measurement of enzyme-catalyzed hydrolysis reactions of water-soluble fluorogenic acyl donor Z-Glu(HMC)-Gly-OH Mus musculus ?
-
-
2.3.2.13 protein glutamine + alkylamine
-
 Homo sapiens protein N5-alkylglutamine + NH3
-
 ?
2.3.2.13 protein glutamine + alkylamine
-
 Cavia porcellus protein N5-alkylglutamine + NH3
-
 ?
2.3.2.13 protein glutamine + alkylamine
-
 Mus musculus protein N5-alkylglutamine + NH3
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.3.2.13 factor XIIIa
-
 Homo sapiens
2.3.2.13 gpTGase 2
-
 Cavia porcellus
2.3.2.13 hfXIIIa
-
 Homo sapiens
2.3.2.13 hTGase 1
-
 Homo sapiens
2.3.2.13 hTGase 2
-
 Homo sapiens
2.3.2.13 hTGase 3
-
 Homo sapiens
2.3.2.13 hTGase 6
-
 Homo sapiens
2.3.2.13 mTGase 2
-
 Mus musculus
2.3.2.13 TGase
-
 Homo sapiens
2.3.2.13 TGase 1
-
 Homo sapiens
2.3.2.13 TGase 2
-
 Homo sapiens
2.3.2.13 TGase 2
-
 Cavia porcellus
2.3.2.13 TGase 2
-
 Mus musculus
2.3.2.13 Tgase 3
-
 Homo sapiens
2.3.2.13 TGase 6
-
 Homo sapiens
2.3.2.13 transglutaminase
-
 Homo sapiens
2.3.2.13 transglutaminase 1
-
 Homo sapiens
2.3.2.13 transglutaminase 2
-
 Homo sapiens
2.3.2.13 transglutaminase 2
-
 Cavia porcellus
2.3.2.13 transglutaminase 2
-
 Mus musculus
2.3.2.13 transglutaminase 3
-
 Homo sapiens
2.3.2.13 transglutaminase 6
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.2.13 30
-
 assay at Homo sapiens
2.3.2.13 30
-
 assay at Cavia porcellus
2.3.2.13 30
-
 assay at Mus musculus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.2.13 6.5
-
 assay at Homo sapiens
2.3.2.13 6.5
-
 assay at Cavia porcellus
2.3.2.13 6.5
-
 assay at Mus musculus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.2.13 additional information
-
 additional information inhibition kinetics Homo sapiens
2.3.2.13 additional information
-
 additional information inhibition kinetics Cavia porcellus
2.3.2.13 additional information
-
 additional information inhibition kinetics Mus musculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.2.13 0.00009
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-3-yl)piperazin-1-yl]hexyl]prop-2-enamide
2.3.2.13 0.0001
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-[4-(6-nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
2.3.2.13 0.00011
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-[4-(6-fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
2.3.2.13 0.00014
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-[4-(6-iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
2.3.2.13 0.00017
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-[4-(6-tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
2.3.2.13 0.00018
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-[4-(6-chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
2.3.2.13 0.0002
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
2.3.2.13 0.00022
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-[4-(6-bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
2.3.2.13 0.00031
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
2.3.2.13 0.00034
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
2.3.2.13 0.00039
-
 pH 6.5, 30°C Homo sapiens N-[(5S)-6-[4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide

General Information

EC Number General Information Comment Organism
2.3.2.13 additional information active-site titration using N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide and Z-Glu(HMC)-Gly-OH Homo sapiens
2.3.2.13 additional information docking study and homology structure molecular modeling using the crystal structure of homologous hTGase 2 (PDB ID 2Q3Z) as template Cavia porcellus
2.3.2.13 physiological function transglutaminase 2 (TGase 2)-catalyzed transamidation represents an important post-translational mechanism for protein modification with implications in physiological and pathophysiological conditions, including fibrotic and neoplastic processes Homo sapiens
2.3.2.13 physiological function transglutaminase 2 (TGase 2)-catalyzed transamidation represents an important post-translational mechanism for protein modification with implications in physiological and pathophysiological conditions, including fibrotic and neoplastic processes Cavia porcellus