Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | structure-activity relationship analysis of Phe-Arg mimetic region of human glutaminyl cyclase inhibitors. Developed of QC inhibitors that contain 3-aminoalkyloxy-4-methoxyphenyl and 4-aminoalkyloxyphenyl groups to replace the previously developed pharmacophore, overview. In vivo activity of the compounds is analyzed using HT-22 cells, an immortalized hippocampal neuronal cell line | Homo sapiens | |
N-((E)-4-(3-(4-(2-aminoethyl)piperazin-1-yl)-3-oxoprop-1-en-1-yl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-((E)-4-(3-oxo-3-(piperazin-1-yl)prop-1-en-1-yl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-((E)-4-(3-oxo-3-(piperidin-4-ylamino)prop-1-en-1-yl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(3,4-dimethoxyphenyl)-N'-[3-(5-methyl-1H-imidazol-1-yl)propyl]thiourea | - |
Homo sapiens | |
N-(3-(2-(2-aminopyridin-4-yl)ethoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(3-(2-aminoethoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(3-(3-(2-aminopyridin-4-yl)propoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(3-(3-aminopropoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(3-(4-(2-aminopyridin-4-yl)butoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(3-(4-(dimethylamino)butoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(3-(4-aminobutoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-((1-(2-aminoethyl)piperidin-4-yl)carbamoyl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-(2-(((2-aminopyridin-4-yl)methyl)amino)-2-oxoethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-(2-((1-(2-aminoethyl)piperidin-4-yl)amino)-2-oxoethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-(2-(piperazin-1-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-(2-oxo-2-(piperazin-1-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-(2-oxo-2-(piperidin-4-ylamino)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-(4-(2-aminopyridin-4-yl)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(2-(1-methylpiperidin-4-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(2-(piperazin-1-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(2-(piperidin-4-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(3-(methylamino)propoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(3-(piperazin-1-yl)propoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(3-(piperidin-4-yl)propoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(4-(methylamino)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(4-(piperazin-1-yl)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(4-(piperidin-4-yl)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(4-methoxy-3-(4-(pyrimidin-2-ylamino)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens | |
N-(E)-(4-(3-(4-(2-aminoethyl)piperazin-1-yl)-3-oxoprop-1-en-1-yl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | - |
Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Zn2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-glutaminyl-peptide | Homo sapiens | - |
5-oxoprolyl-peptide + NH3 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q16769 | isozyme sQC | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
hippocampus | - |
Homo sapiens | - |
neuron | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
L-glutaminyl-peptide | - |
Homo sapiens | 5-oxoprolyl-peptide + NH3 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
glutaminyl cyclase | - |
Homo sapiens |
hQC | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000064 | - |
pH and temperature not specified in the publication | Homo sapiens | N-((E)-4-(3-(4-(2-aminoethyl)piperazin-1-yl)-3-oxoprop-1-en-1-yl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000073 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(2-(piperidin-4-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000079 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-(2-aminoethoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000079 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-(2-((1-(2-aminoethyl)piperidin-4-yl)amino)-2-oxoethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000079 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(4-(piperidin-4-yl)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000088 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-(4-aminobutoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000088 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(3-(piperidin-4-yl)propoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.000009 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-(3-aminopropoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000112 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(E)-(4-(3-(4-(2-aminoethyl)piperazin-1-yl)-3-oxoprop-1-en-1-yl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000114 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-(2-oxo-2-(piperazin-1-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000129 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-(2-oxo-2-(piperidin-4-ylamino)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.000015 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-(3-(2-aminopyridin-4-yl)propoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.000015 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(4-(piperazin-1-yl)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000152 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(4-(pyrimidin-2-ylamino)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000158 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(3-(piperazin-1-yl)propoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000159 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-(4-(2-aminopyridin-4-yl)butoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000162 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-((1-(2-aminoethyl)piperidin-4-yl)carbamoyl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000184 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(2-(piperazin-1-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000187 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-(2-(piperazin-1-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000194 | - |
pH and temperature not specified in the publication | Homo sapiens | N-((E)-4-(3-oxo-3-(piperazin-1-yl)prop-1-en-1-yl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000206 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(2-(1-methylpiperidin-4-yl)ethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.000022 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(4-(methylamino)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000247 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-(4-(2-aminopyridin-4-yl)butoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.000026 | - |
pH and temperature not specified in the publication | Homo sapiens | N-((E)-4-(3-oxo-3-(piperidin-4-ylamino)prop-1-en-1-yl)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000264 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-(2-(2-aminopyridin-4-yl)ethoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000268 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-methoxy-3-(3-(methylamino)propoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000292 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3,4-dimethoxyphenyl)-N'-[3-(5-methyl-1H-imidazol-1-yl)propyl]thiourea | |
0.0000468 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-(4-(dimethylamino)butoxy)-4-methoxyphenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea | |
0.0000565 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-(2-(((2-aminopyridin-4-yl)methyl)amino)-2-oxoethoxy)phenyl)-N'-(3-(5-methyl-1H-imidazol-1-yl)propyl)thiourea |