Application | Comment | Organism |
---|---|---|
drug development | acetylcholinesterase, butyrylcholinesterase and beta-amyloid are the predominant biological targets in the search for anti-Alzheimer's agents | Equus caballus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(2-fluorobenzyl)-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine | - |
Equus caballus | |
1-(2-fluorobenzyl)-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine | - |
Equus caballus | |
1-(3-chlorobenzyl)-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine | - |
Equus caballus | |
1-(3-chlorobenzyl)-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine | - |
Equus caballus | |
1-benzyl-N-[3-(2,3-dihydro-1H-indol-1-yl)propyl]piperidin-4-amine | - |
Equus caballus | |
1-benzyl-N-[5-(2,3-dihydro-1H-indol-1-yl)pentyl]piperidin-4-amine | - |
Equus caballus | |
1-benzyl-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine | - |
Equus caballus | |
1-benzyl-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine | - |
Equus caballus | |
2-(3-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(3-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(3-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(3-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(6-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(6-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(6-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(6-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(8-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(8-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione | a selective BChE inhibitor | Equus caballus | |
2-(8-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-(8-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-[3-[(1-benzylpiperidin-4-yl)amino]propyl]-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-[5-[(1-benzylpiperidin-4-yl)amino]pentyl]-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-[6-[(1-benzylpiperidin-4-yl)amino]hexyl]-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
2-[8-[(1-benzylpiperidin-4-yl)amino]octyl]-1H-isoindole-1,3(2H)-dione | - |
Equus caballus | |
4-[(4-[[6-(1H-indol-1-yl)hexyl]amino]piperidin-1-yl)methyl]phenol | - |
Equus caballus | |
4-[(4-[[8-(1H-indol-1-yl)octyl]amino]piperidin-1-yl)methyl]phenol | - |
Equus caballus | |
donepezil | - |
Equus caballus | |
additional information | evaluation of a combination of both anticholinesterase and beta-amyloid anti-aggregation activities in one molecule, and therapeutic potential in vivo. Design and synthesis of 28 compounds as derivatives of donepezil that contain the N-benzylpiperidine moiety combined with the phthalimide or indole moieties. No or poor inhibition by 2-[5-[(1-benzylpiperidin-4-yl)amino]pentyl]-1H-isoindole-1,3(2H)-dione | Equus caballus | |
N-[6-(1H-indol-1-yl)hexyl]-1-(4-methoxybenzyl)piperidin-4-amine | - |
Equus caballus | |
N-[8-(1H-indol-1-yl)octyl]-1-(4-methoxybenzyl)piperidin-4-amine | - |
Equus caballus | |
tacrine | - |
Equus caballus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Equus caballus | P81908 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
commercial preparation | - |
Equus caballus | - |
serum | - |
Equus caballus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
butyrylthiocholine + H2O | - |
Equus caballus | thiocholine + butyrate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
butyrylcholinesterase | - |
Equus caballus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Equus caballus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8 | - |
assay at | Equus caballus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00034 | - |
pH 8.0, 25°C | Equus caballus | 4-[(4-[[8-(1H-indol-1-yl)octyl]amino]piperidin-1-yl)methyl]phenol | |
0.00052 | - |
pH 8.0, 25°C | Equus caballus | 4-[(4-[[6-(1H-indol-1-yl)hexyl]amino]piperidin-1-yl)methyl]phenol | |
0.00072 | - |
pH 8.0, 25°C | Equus caballus | 2-(8-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione | |
0.00075 | - |
pH 8.0, 25°C | Equus caballus | 1-(2-fluorobenzyl)-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine | |
0.00081 | - |
pH 8.0, 25°C | Equus caballus | 2-(8-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione | |
0.00083 | - |
pH 8.0, 25°C | Equus caballus | 1-(2-fluorobenzyl)-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine | |
0.00093 | - |
pH 8.0, 25°C | Equus caballus | 1-benzyl-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine | |
0.00108 | - |
pH 8.0, 25°C | Equus caballus | 1-benzyl-N-[5-(2,3-dihydro-1H-indol-1-yl)pentyl]piperidin-4-amine | |
0.00133 | - |
pH 8.0, 25°C | Equus caballus | 1-(3-chlorobenzyl)-N-[8-(1H-indol-1-yl)octyl]piperidin-4-amine | |
0.00178 | - |
pH 8.0, 25°C | Equus caballus | 1-(3-chlorobenzyl)-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine | |
0.00187 | - |
pH 8.0, 25°C | Equus caballus | 2-(8-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione | |
0.00198 | - |
pH 8.0, 25°C | Equus caballus | 2-[8-[(1-benzylpiperidin-4-yl)amino]octyl]-1H-isoindole-1,3(2H)-dione | |
0.00232 | - |
pH 8.0, 25°C | Equus caballus | 2-(6-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione | |
0.00273 | - |
pH 8.0, 25°C | Equus caballus | 2-(6-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione | |
0.00341 | - |
pH 8.0, 25°C | Equus caballus | 1-benzyl-N-[6-(1H-indol-1-yl)hexyl]piperidin-4-amine | |
0.004 | - |
pH 8.0, 25°C | Equus caballus | 2-(6-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione | |
0.00446 | - |
pH 8.0, 25°C | Equus caballus | N-[8-(1H-indol-1-yl)octyl]-1-(4-methoxybenzyl)piperidin-4-amine | |
0.00453 | - |
pH 8.0, 25°C | Equus caballus | 2-(3-[[1-(3-chlorobenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione | |
0.00565 | - |
pH 8.0, 25°C | Equus caballus | 2-(8-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]octyl)-1H-isoindole-1,3(2H)-dione | |
0.00739 | - |
pH 8.0, 25°C | Equus caballus | 2-(6-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]hexyl)-1H-isoindole-1,3(2H)-dione | |
0.00813 | - |
pH 8.0, 25°C | Equus caballus | N-[6-(1H-indol-1-yl)hexyl]-1-(4-methoxybenzyl)piperidin-4-amine | |
0.00937 | - |
pH 8.0, 25°C | Equus caballus | 2-(3-[[1-(4-hydroxybenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione | |
0.01052 | - |
pH 8.0, 25°C | Equus caballus | 2-(3-[[1-(2-fluorobenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione | |
0.01285 | - |
pH 8.0, 25°C | Equus caballus | 2-[6-[(1-benzylpiperidin-4-yl)amino]hexyl]-1H-isoindole-1,3(2H)-dione | |
0.0153 | - |
pH 8.0, 25°C | Equus caballus | 1-benzyl-N-[3-(2,3-dihydro-1H-indol-1-yl)propyl]piperidin-4-amine | |
0.0268 | - |
pH 8.0, 25°C | Equus caballus | 2-(3-[[1-(4-methoxybenzyl)piperidin-4-yl]amino]propyl)-1H-isoindole-1,3(2H)-dione | |
0.0518 | - |
pH 8.0, 25°C | Equus caballus | 2-[3-[(1-benzylpiperidin-4-yl)amino]propyl]-1H-isoindole-1,3(2H)-dione |