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Literature summary extracted from

  • Marrano, C.; de Macedo, P.; Gagnon, P.; Lapierre, D.; Gravel, C.; Keillor, J.W.
    Synthesis and evaluation of novel dipeptide-bound 1,2,4-thiadiazoles as irreversible inhibitors of guinea pig liver transglutaminase (2001), Bioorg. Med. Chem., 9, 3231-3241.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.2.13 N-(3-methyl-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-glutaminylglycine irreversible, ratio kinact to Ki 0.33 micromol per min Cavia porcellus
2.3.2.13 N-[(2S)-4-[(3-methoxy-1,2,4-thiadiazol-5-yl)amino]-2-[(phenoxycarbonyl)amino]butanoyl]glycine irreversible, ratio kinact to Ki 0.71 micromol per min Cavia porcellus
2.3.2.13 N5-(3-methoxy-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-ornithylglycine irreversible, ratio kinact to Ki 0.55 micromol per min Cavia porcellus
2.3.2.13 N6-(3-methoxy-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-lysylglycine irreversible, ratio kinact to Ki 0.72 micromol per min Cavia porcellus
2.3.2.13 tert-butyl N-(3-methyl-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-glutaminylglycinate irreversible, ratio kinact to Ki 0.78 micromol per min 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
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.2.13 Cbz-L-Gln-Gly + ?
-
 Cavia porcellus ?
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.3.2.13 0.0013
-
 tert-butyl N-(3-methyl-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-glutaminylglycinate
-
 Cavia porcellus
2.3.2.13 0.0013
-
 N-[(2S)-4-[(3-methoxy-1,2,4-thiadiazol-5-yl)amino]-2-[(phenoxycarbonyl)amino]butanoyl]glycine
-
 Cavia porcellus
2.3.2.13 0.0017
-
 N6-(3-methoxy-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-lysylglycine
-
 Cavia porcellus
2.3.2.13 0.0023
-
 N5-(3-methoxy-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-ornithylglycine
-
 Cavia porcellus
2.3.2.13 0.014
-
 N-(3-methyl-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-glutaminylglycine
-
 Cavia porcellus