Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-nitro-N'-[(R)-1-phenylethyl]isophthalamide | - |
Homo sapiens | |
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)-amino]-N'-[(R)-1-(4-fluorophenyl)ethyl]isophthalamide | - |
Homo sapiens | |
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)amino]-N-[(R)-1-phenylethyl]isophthalamide | shows inhibitory effects on beta amyloid production of amyloid precursor protein-transfected HEK293 cells and mild protective effect against hydrogen peroxide-induced cell injury | Homo sapiens | |
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropyl-5-nitroisophthalamide | - |
Homo sapiens | |
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropyl-5-[methyl(methylsulfonyl)amino]isophthalamide | - |
Homo sapiens | |
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropylisophthalamide | - |
Homo sapiens | |
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-nitroisophthalamide | - |
Homo sapiens | |
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-isophthalamide | - |
Homo sapiens | |
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-phenylethyl]isophthalamide | - |
Homo sapiens | |
donepezil | 7.9% inhibition at 0.025 mM | Homo sapiens | |
N-((4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]carbamoyl-5-hydroxy-2-methyloct-4-yl)-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenyl ethyl]isophthalamide | 48.7% inhibition at 0.025 mM | Homo sapiens | |
N-((4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]carbamoyl-5-hydroxy-2-methyloct-4-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]isophthalamide | 47.5% inhibition at 0.025 mM | Homo sapiens | |
N-((4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-5-hydroxy-2-methyloctan-4-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]isophthalamide | 23.8% inhibition at 0.025 mM | Homo sapiens | |
N-((4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]methylcarbamoyl-5-hydroxy-2-methyloct-4-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]isophthalamide | 45.9% inhibition at 0.025 mM | Homo sapiens | |
N-((4S,5S,7R)-2-[7-(4-benzylpiperazin-1-yl)]carbamoyl-5-hydroxy-2-methyloct-4-yl)-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide | 5.2% inhibition at 0.025 mM | Homo sapiens | |
N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethyl-carbamoyl-3-hydroxy-1-phenylbut-2-yl)-5-[methyl-(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide | - |
Homo sapiens | |
N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-3-hydroxy-1-phenylbut-2-yl)-N',N'-dipropyl-5-nitroisophthalamide | - |
Homo sapiens | |
N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-3-hydroxy-1-phenylbut-2-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]iso phthalamide | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
HEK-293 cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
S-acetylthiocholine + H2O | detection with 5,5'-dithio-bis-2-nitrobenzoic acid, i.e. DTNB | Homo sapiens | acetate + thiocholine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
AChE | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00105 | - |
pH 8.0, 37°C | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropyl-5-[methyl(methylsulfonyl)amino]isophthalamide | |
0.00111 | - |
pH 8.0, 37°C | Homo sapiens | N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethyl-carbamoyl-3-hydroxy-1-phenylbut-2-yl)-5-[methyl-(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide | |
0.00127 | - |
pH 8.0, 37°C | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropyl-5-nitroisophthalamide | |
0.00135 | - |
pH 8.0, 37°C | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)-amino]-N'-[(R)-1-(4-fluorophenyl)ethyl]isophthalamide | |
0.00139 | - |
pH 8.0, 37°C | Homo sapiens | N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-3-hydroxy-1-phenylbut-2-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]iso phthalamide | |
0.00168 | - |
pH 8.0, 37°C | Homo sapiens | N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-3-hydroxy-1-phenylbut-2-yl)-N',N'-dipropyl-5-nitroisophthalamide | |
0.00183 | - |
pH 8.0, 37°C, in vitro AChE inhibition | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)amino]-N-[(R)-1-phenylethyl]isophthalamide | |
0.00209 | - |
pH 8.0, 37°C | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-nitroisophthalamide | |
0.00228 | - |
pH 8.0, 37°C | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropylisophthalamide | |
0.00253 | - |
pH 8.0, 37°C | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-nitro-N'-[(R)-1-phenylethyl]isophthalamide | |
0.00306 | - |
pH 8.0, 37°C | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-phenylethyl]isophthalamide | |
0.0117 | - |
pH 8.0, 37°C | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-isophthalamide | |
0.0987 | - |
in vivo in amyloid precursor protein-transfected HEK293 cells | Homo sapiens | (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)amino]-N-[(R)-1-phenylethyl]isophthalamide |