Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.3.2.13 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

Inhibitors Comment Organism Structure
1-(6-methylpyridin-2-yl)piperazine
-
Cavia porcellus
1-(6-methylpyridin-2-yl)piperazine
-
Homo sapiens
1-(6-nitropyridin-3-yl)piperazine
-
Cavia porcellus
1-(6-nitropyridin-3-yl)piperazine
-
Homo sapiens
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
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
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
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
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
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
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxamide
-
Cavia porcellus
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxamide
-
Homo sapiens
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylic acid
-
Cavia porcellus
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylic acid
-
Homo sapiens
methyl 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylate
-
Cavia porcellus
methyl 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylate
-
Homo sapiens
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
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
N,N-dimethyl-5-(piperazine-1-sulfonyl)naphthalen-1-amine
-
Cavia porcellus
N,N-dimethyl-5-(piperazine-1-sulfonyl)naphthalen-1-amine
-
Homo sapiens
N-[(5S)-5-(2-cyclohexylacetamido)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-(2-cyclohexylacetamido)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[2-(4-bromophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[2-(4-bromophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[2-(4-chlorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[2-(4-chlorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[2-(4-iodophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[2-(4-iodophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[2-(4-methylphenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[2-(4-methylphenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[[(4-fluorophenyl)carbamothioyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[[(4-fluorophenyl)carbamothioyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[[(4-fluorophenyl)carbamoyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[[(4-fluorophenyl)carbamoyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-5-[[(4-fluorophenyl)methyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-5-[[(4-fluorophenyl)methyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
Homo sapiens
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
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
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-(4-phenylpiperazin-1-yl)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-(4-phenylpiperazin-1-yl)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-3-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-3-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-4-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-4-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-[6-(trifluoromethyl)pyridin-3-yl]piperazin-1-yl]hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-[6-(trifluoromethyl)pyridin-3-yl]piperazin-1-yl]hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-oxo-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]-5-(2,2,2-trifluoroacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-oxo-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]-5-(2,2,2-trifluoroacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(3-methylphenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(3-methylphenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(4-fluorobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(4-fluorobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(4-nitrobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(4-nitrobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(4-nitrophenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(4-nitrophenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(6-bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(6-chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(6-chloropyridine-2-carbonyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-chloropyridine-2-carbonyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
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
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
N-[(5S)-6-[4-(6-fluoropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-fluoropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(6-iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide reversible inhibitor Cavia porcellus
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide reversible inhibitor Homo sapiens
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamothioyl)amino]hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamothioyl)amino]hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylmethanesulfonyl)amino]hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylmethanesulfonyl)amino]hexyl]prop-2-enamide
-
Homo sapiens
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
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
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
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
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
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
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
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
N-[(5S)-6-[4-(6-nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Mus musculus
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide reversible inhibitor Cavia porcellus
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide reversible inhibitor Homo sapiens
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Mus musculus
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-(6-tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-(6-tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
N-[(5S)-6-[4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Cavia porcellus
N-[(5S)-6-[4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
Homo sapiens
tert-butyl 4-(4-fluorobenzoyl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(4-fluorobenzoyl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(6-chloropyridine-2-carbonyl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(6-chloropyridine-2-carbonyl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(6-fluoropyridin-2-yl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(6-fluoropyridin-2-yl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(6-fluoropyridin-3-yl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(6-fluoropyridin-3-yl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(6-iodopyridin-2-yl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(6-iodopyridin-2-yl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(6-nitropyridin-2-yl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(6-nitropyridin-2-yl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(6-phenylpyridin-2-yl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(6-phenylpyridin-2-yl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(6-tert-butylpyridin-2-yl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(6-tert-butylpyridin-2-yl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-(pyridin-3-yl)piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-(pyridin-3-yl)piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-[(4-fluorophenyl)methyl]piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-[(4-fluorophenyl)methyl]piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-[6-(methoxycarbonyl)pyridin-3-yl]piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-[6-(methoxycarbonyl)pyridin-3-yl]piperazine-1-carboxylate
-
Homo sapiens
tert-butyl 4-[6-(trifluoromethyl)pyridin-3-yl]piperazine-1-carboxylate
-
Cavia porcellus
tert-butyl 4-[6-(trifluoromethyl)pyridin-3-yl]piperazine-1-carboxylate
-
Homo sapiens

KM Value [mM]

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

Metals/Ions

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

Natural Substrates/ Products (Substrates)

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

Organism

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

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

Ki Value [mM]

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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
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
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
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
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
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
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
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
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

General Information Comment Organism
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
additional information docking study and homology structure molecular modeling using the crystal structure of homologous hTGase 2 (PDB ID 2Q3Z) as template Cavia porcellus
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
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