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Literature summary for 2.3.2.13 extracted from

  • Case, A.; Stein, R.L.
    Kinetic analysis of the interaction of tissue transglutaminase with a nonpeptidic slow-binding inhibitor (2007), Biochemistry, 46, 1106-1115.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(1Z)-2-{[3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]sulfanyl}ethanehydrazonic acid
-
Homo sapiens
2-([3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
Homo sapiens
2-([3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
Homo sapiens
2-([3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
Homo sapiens
2-([3-(3-fluorophenyl)-4-oxo-6-phenyl-3,4-dihydroquinazolin-2-yl]thio)acetohydrazide
-
Homo sapiens
2-([3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
Homo sapiens
2-([3-(3-fluorophenyl)-5-(3-diethylaminopropoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
Homo sapiens
2-[(2-hydrazinoethyl)thio]-3,5-diphenylthieno[2,3-d]pyrimidin-4(3H)-one i.e. LDN-27219, reversible, slow-binding inhibitor that binds at the enzyme’s GTP site or a site that regulates binding of GTP Homo sapiens
2-[(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)thio]acetohydrazide
-
Homo sapiens
2-[(4-oxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide
-
Homo sapiens
2-[[3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide
-
Homo sapiens
2-[[3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide
-
Homo sapiens
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide
-
Homo sapiens
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide
-
Homo sapiens
2-[[3-(3-fluorophenyl)-4-oxo-6-phenyl-3,4-dihydroquinazolin-2-yl]thio]acetohydrazide
-
Homo sapiens
2-[[5-benzyl-3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide
-
Homo sapiens
2-[[5-[2-[3-(diethylamino)propoxy]phenyl]-3-(3-fluorophenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide
-
Homo sapiens
benzyl 3-(3-fluorophenyl)-2-[(2-hydrazino-2-oxoethyl)sulfanyl]-4-oxo-3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(4H)-carboxylate
-
Homo sapiens
LDN-27219 reversible, slow-binding inhibitor that appears not to bind at the enzyme’s active site but rather at the enzyme’s GTP site, or a site that regulates binding of GTP. The potency and kinetics of inhibition are dependent on substrate structure and suggest a novel mechanism of inhibition that involves differential binding of LDN-27219 to multiple conformational states of this enzyme Homo sapiens
tert-butyl 3-(3-fluorophenyl)-2-[(2-hydrazino-2-oxoethyl)sulfanyl]-4-oxo-3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(4H)-carboxylate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-N-benzyloxycarbonyl-L-Lys-NH-CH2-CH2-NH-dansyl + Abeta1-40 residues 1-40 of beta-amyloid protein Homo sapiens ?
-
?
2-N-benzyloxycarbonyl-L-Lys-NH-CH2-CH2-NH-dansyl + N-methyl-casein
-
Homo sapiens ?
-
?
alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl + Asp-Ala-Glu-Phe-Arg-His-Asp-Ser-Gly-Tyr-Glu-Val-His-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val i.e. beta-amyloid protein peptide comprising residues 1-40 Homo sapiens ?
-
?
alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl + N,N-dimethylated casein transpeptidation Homo sapiens ?
-
?
benzyloxycarbonyl-Pro-Gln-Nle-Phe + H2O
-
Homo sapiens ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00014
-
2-([3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate N-methylcasein Homo sapiens
0.00014
-
2-[[3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.00016
-
2-([3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate N-methylcasein Homo sapiens
0.00016
-
2-[[3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.00017
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide substrate N-methylcasein Homo sapiens
0.00017
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.00018
-
2-([3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate N-methylcasein Homo sapiens
0.00018
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.00025
-
2-[(4-oxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide substrate N-methylcasein Homo sapiens
0.00025
-
2-[(4-oxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.00061
-
2-([3-(3-fluorophenyl)-5-(3-diethylaminopropoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate N-methylcasein Homo sapiens
0.00061
-
2-[[5-[2-[3-(diethylamino)propoxy]phenyl]-3-(3-fluorophenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.0011
-
2-[[5-benzyl-3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide substrate N-methylcasein Homo sapiens
0.0011
-
benzyl 3-(3-fluorophenyl)-2-[(2-hydrazino-2-oxoethyl)sulfanyl]-4-oxo-3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(4H)-carboxylate substrate N-methylcasein Homo sapiens
0.0011
-
2-[[5-benzyl-3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.0011
-
tert-butyl 3-(3-fluorophenyl)-2-[(2-hydrazino-2-oxoethyl)sulfanyl]-4-oxo-3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(4H)-carboxylate transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.0015
-
2-([3-(3-fluorophenyl)-4-oxo-6-phenyl-3,4-dihydroquinazolin-2-yl]thio)acetohydrazide substrate N-methylcasein Homo sapiens
0.0015
-
2-[[3-(3-fluorophenyl)-4-oxo-6-phenyl-3,4-dihydroquinazolin-2-yl]thio]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.0042
-
2-[[3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.005
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide substrate Abeta1-40 Homo sapiens
0.005
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide transpeptidation of Asp-Ala-Glu-Phe-Arg-His-Asp-Ser-Gly-Tyr-Glu-Val-His-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.006
-
2-[(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)thio]acetohydrazide substrate N-methylcasein Homo sapiens
0.006
-
2-[(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)thio]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.0071
-
2-([3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate N-methylcasein Homo sapiens
0.0071
-
2-[[3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide transpeptidation of N,N-dimethylated casein by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.0073
-
2-[(4-oxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.0082
-
2-[[3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.01
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.01
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.019
-
2-([3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate Abeta1-40 Homo sapiens
0.019
-
2-[[3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide transpeptidation of Asp-Ala-Glu-Phe-Arg-His-Asp-Ser-Gly-Tyr-Glu-Val-His-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.039
-
2-[(4-oxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide substrate Abeta1-40 Homo sapiens
0.039
-
2-[(4-oxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide transpeptidation of Asp-Ala-Glu-Phe-Arg-His-Asp-Ser-Gly-Tyr-Glu-Val-His-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.041
-
2-([3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate Abeta1-40 Homo sapiens
0.041
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide transpeptidation of Asp-Ala-Glu-Phe-Arg-His-Asp-Ser-Gly-Tyr-Glu-Val-His-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.045
-
2-([3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate Abeta1-40 Homo sapiens
0.045
-
2-[[3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide transpeptidation of Asp-Ala-Glu-Phe-Arg-His-Asp-Ser-Gly-Tyr-Glu-Val-His-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.05
-
2-[[5-[2-[3-(diethylamino)propoxy]phenyl]-3-(3-fluorophenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.09
-
benzyl 3-(3-fluorophenyl)-2-[(2-hydrazino-2-oxoethyl)sulfanyl]-4-oxo-3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(4H)-carboxylate substrate Abeta1-40 Homo sapiens
0.09
-
tert-butyl 3-(3-fluorophenyl)-2-[(2-hydrazino-2-oxoethyl)sulfanyl]-4-oxo-3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(4H)-carboxylate transpeptidation of Asp-Ala-Glu-Phe-Arg-His-Asp-Ser-Gly-Tyr-Glu-Val-His-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.11
-
2-([3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate Abeta1-40 Homo sapiens
0.11
-
2-[[3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide transpeptidation of Asp-Ala-Glu-Phe-Arg-His-Asp-Ser-Gly-Tyr-Glu-Val-His-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.18
-
2-[[3-(3-fluorophenyl)-4-oxo-6-phenyl-3,4-dihydroquinazolin-2-yl]thio]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.19
-
2-[[5-benzyl-3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.2
-
tert-butyl 3-(3-fluorophenyl)-2-[(2-hydrazino-2-oxoethyl)sulfanyl]-4-oxo-3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(4H)-carboxylate hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.21
-
2-([3-(3-fluorophenyl)-5-(3-diethylaminopropoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide substrate Abeta1-40 Homo sapiens
0.21
-
2-[[5-[2-[3-(diethylamino)propoxy]phenyl]-3-(3-fluorophenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide transpeptidation of Asp-Ala-Glu-Phe-Arg-His-Asp-Ser-Gly-Tyr-Glu-Val-His-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Glu-Asp-Val-Gly-Ser-Asn-Lys-Gly-Ala-Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val by alphaN-Boc-Lys-NH-CH2-CH2-NH-dansyl Homo sapiens
0.22
-
2-[[3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens
0.5
-
2-[(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)thio]acetohydrazide hydrolysis of benzyloxycarbonyl-Pro-Gln-Nle-Phe Homo sapiens