Literature summary for 2.3.2.13 extracted from

Duval, E.; Case, A.; Stein, R.L.; Cuny, G.D.
Structure-activity relationship study of novel tissue transglutaminase inhibitors (2005), Bioorg. Med. Chem. Lett., 15, 1885-1889.

Inhibitors

Inhibitors	Comment	Organism
2-([3-(2-chlorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.0015 mM, standard format	Homo sapiens
2-([3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.00025 mM, standard format, at 0.00018 mM, full progress curve	Homo sapiens
2-([3-(2-methoxyphenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.00082 mM, standard format, at 0.00047 mM, full progress curve	Homo sapiens
2-([3-(3-chlorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.0018 mM, standard format	Homo sapiens
2-([3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.00045 mM, full progress curve	Homo sapiens
2-([3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.00021 mM, standard format, at 0.00014 mM, full progress curve	Homo sapiens
2-([3-(3-fluorophenyl)-5-(2-hydroxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.0008 mM, standard format, at 0.00025 mM, full progress curve	Homo sapiens
2-([3-(3-fluorophenyl)-5-(3-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.0014 mM, standard format	Homo sapiens
2-([3-(3-fluorophenyl)-5-methyl-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.0002 mM, full progress curve	Homo sapiens
2-([3-(3-fluorophenyl)-5-phenyl-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.00093 mM, standard format, at 0.00071 mM, full progress curve	Homo sapiens
2-([3-(3-fluorophenyl)-7-methyl-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.00053 mM, full progress curve	Homo sapiens
2-([3-(3-methoxyphenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.0021 mM, standard format	Homo sapiens
2-([3-(4-chlorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.0005 mM, standard format, at 0.00016 mM, full progress curve	Homo sapiens
2-([3-(4-methoxyphenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.0018 mM, standard format	Homo sapiens
2-([5-(4-fluorophenyl)-4-oxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide	50% inhibition at 0.0008 mM, standard format, at 0.00029 mM, full progress curve	Homo sapiens
2-[(3-amino-2-oxopropyl)thio]-3-(3-fluorophenyl)-5-phenylthieno[2,3-d]pyrimidin-4(3H)-one	50% inhibition at 0.0053 mM, standard format	Homo sapiens
2-[(3-benzyl-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide	50% inhibition at 0.0012 mM, standard format, at 0.00048 mM, full progress curve	Homo sapiens
2-[(3-methyl-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide	50% inhibition at 0.0023 mM, standard format	Homo sapiens
2-[(4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)amino]acetohydrazide	50% inhibition at 0.0037 mM, full progress curve	Homo sapiens
2-[(4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)oxy]acetohydrazide	50% inhibition at 0.0045 mM, standard format	Homo sapiens
2-[(4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide	50% inhibition at 0.0008 mM, standard format, at 0.00025 mM, full progress curve	Homo sapiens
2-[(4-oxo-5-phenyl-3-pyridin-3-yl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide	50% inhibition at 0.002 mM, standard format	Homo sapiens
2-[(6-methyl-4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide	50% inhibition at 0.0015 mM, standard format, at 0.00016 mM, full progress curve	Homo sapiens
3-[(6-methyl-4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]propanohydrazide	50% inhibition at 0.0013 mM, standard format	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
alpha-N-t-butyloxycarbonyl-L-Lys-CH2-CH2-dansyl + N,N-dimethylcasein	-	Homo sapiens	?	-	?