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 enzymes 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 enzymes active site but rather at the enzymes 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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
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 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 |