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Literature summary for 3.1.1.7 extracted from

  • Shen, Y.; Sheng, R.; Zhang, J.; He, Q.; Yang, B.; Hu, Y.
    2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity (2008), Bioorg. Med. Chem., 16, 7646-7653.
    View publication on PubMed
Search for more literature for 3.1.1.7

Inhibitors

Inhibitors Comment Organism Structure
2-(3-(2-(diethylamino)ethyl)phenoxy)-5,6-dimethoxyindan-1-one
-
 Rattus norvegicus
2-(3-(2-(ethyl(methyl)amino)ethyl)phenoxy)-5,6-dimethoxy-indan-1-one
-
 Rattus norvegicus
2-(3-(3-(diethylamino)propanoyl)phenoxy)-5,6-dimethoxy-indan-1-one
-
 Rattus norvegicus
2-(4-(2-(diethylamino)acetyl)phenoxy)-5,6-dimethoxyindan-1-one
-
 Rattus norvegicus
2-(4-(2-(diethylamino)ethyl)phenoxy)-5,6-dimethoxyindan-1-one
-
 Rattus norvegicus
2-(4-(2-(ethyl(methyl)amino)acetyl)phenoxy)-5,6-dimethoxy-indan-1-one
-
 Rattus norvegicus
2-(4-(2-(ethyl(methyl)amino)ethyl)phenoxy)-5,6-dimethoxy-indan-1-one
-
 Rattus norvegicus
2-(4-(3-(diethylamino)propanoyl)phenoxy)-5,6-dimethoxy-indan-1-one displays neuroprotective effect against H2O2-induced cell death Rattus norvegicus
2-(4-(3-(diethylamino)propyl)phenoxy)-5,6-dimethoxyindan-1-one
-
 Rattus norvegicus
2-(4-(3-(ethyl(methyl)amino)propanoyl)phenoxy)-5,6-dimethoxy-indan-1-one
-
 Rattus norvegicus
2-(4-(4-(diethylamino)butanoyl)phenoxy)-5,6-dimethoxy-indan-1-one
-
 Rattus norvegicus
2-(4-(4-(diethylamino)butyl)phenoxy)-5,6-dimethoxyindan-1-one
-
 Rattus norvegicus
2-(4-(4-(ethyl(methyl)amino)butanoyl)phenoxy)-5,6-dimethoxy-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(3-(2-(piperidin-1-yl)ethyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(3-(2-(pyrrolidin-1-yl)ethyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(3-(3-(pyrrolidin-1-yl)propanoyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(2-(piperidin-1-yl)acetyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(2-(piperidin-1-yl)ethyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(2-(pyrrolidin-1-yl)acetyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(2-(pyrrolidin-1-yl)ethyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(3-(piperidin-1-yl)propanoyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(3-(piperidin-1-yl)propyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(3-(pyrrolidin-1-yl)propanoyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(3-(pyrrolidin-1-yl)propyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(4-(piperidin-1-yl)butanoyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(4-(pyrrolidin-1-yl)butanoyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
5,6-dimethoxy-2-(4-(4-(pyrrolidin-1-yl)butyl)phenoxy)-indan-1-one
-
 Rattus norvegicus
donepezil
-
 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain cortex
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-acetylthiocholine iodide + H2O detection with 5,5'-dithio-bis-2-nitrobenzoic acid, i.e. DTNB Rattus norvegicus acetate + thiocholine iodide
-
 ?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000078
-
 pH 7.4, 37°C Rattus norvegicus 2-(4-(3-(diethylamino)propanoyl)phenoxy)-5,6-dimethoxy-indan-1-one
0.00000185
-
 pH 7.4, 37°C Rattus norvegicus 2-(4-(3-(ethyl(methyl)amino)propanoyl)phenoxy)-5,6-dimethoxy-indan-1-one
0.00000373
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(2-(pyrrolidin-1-yl)ethyl)phenoxy)-indan-1-one
0.00000416
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(3-(pyrrolidin-1-yl)propanoyl)phenoxy)-indan-1-one
0.00000502
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(2-(piperidin-1-yl)ethyl)phenoxy)-indan-1-one
0.00000516
-
 pH 7.4, 37°C Rattus norvegicus 2-(4-(2-(ethyl(methyl)amino)ethyl)phenoxy)-5,6-dimethoxy-indan-1-one
0.0000173
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(3-(piperidin-1-yl)propanoyl)phenoxy)-indan-1-one
0.0000268
-
 pH 7.4, 37°C Rattus norvegicus donepezil
0.0000316
-
 pH 7.4, 37°C Rattus norvegicus 2-(4-(2-(ethyl(methyl)amino)acetyl)phenoxy)-5,6-dimethoxy-indan-1-one
0.0000376
-
 pH 7.4, 37°C Rattus norvegicus 2-(4-(4-(ethyl(methyl)amino)butanoyl)phenoxy)-5,6-dimethoxy-indan-1-one
0.0000406
-
 pH 7.4, 37°C Rattus norvegicus 2-(4-(4-(diethylamino)butanoyl)phenoxy)-5,6-dimethoxy-indan-1-one
0.0000421
-
 pH 7.4, 37°C Rattus norvegicus 2-(4-(2-(diethylamino)ethyl)phenoxy)-5,6-dimethoxyindan-1-one
0.000062
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(4-(pyrrolidin-1-yl)butanoyl)phenoxy)-indan-1-one
0.000209
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(3-(pyrrolidin-1-yl)propyl)phenoxy)-indan-1-one
0.00024
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(2-(pyrrolidin-1-yl)acetyl)phenoxy)-indan-1-one
0.000277
-
 pH 7.4, 37°C Rattus norvegicus 2-(4-(3-(diethylamino)propyl)phenoxy)-5,6-dimethoxyindan-1-one
0.00028
-
 pH 7.4, 37°C Rattus norvegicus 2-(4(2-(diethylamino)acetyl)phenoxy)-5,6-dimethoxyindan-1-one
0.000364
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(2-(piperidin-1-yl)acetyl)phenoxy)-indan-1-one
0.000415
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(4-(pyrrolidin-1-yl)butyl)phenoxy)-indan-1-one
0.000481
-
 pH 7.4, 37°C Rattus norvegicus 2-(4-(4-(diethylamino)butyl)phenoxy)-5,6-dimethoxyindan-1-one
0.000529
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(4-(piperidin-1-yl)butanoyl)phenoxy)-indan-1-one
0.00064
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(4-(3-(piperidin-1-yl)propyl)phenoxy)-indan-1-one
0.00071
-
 pH 7.4, 37°C Rattus norvegicus 2-(3-(2-(ethyl(methyl)amino)ethyl)phenoxy)-5,6-dimethoxy-indan-1-one
0.000832
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(3-(3-(pyrrolidin-1-yl)propanoyl)phenoxy)-indan-1-one
0.00155
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(3-(2-(piperidin-1-yl)ethyl)phenoxy)-indan-1-one
0.00177
-
 pH 7.4, 37°C Rattus norvegicus 5,6-dimethoxy-2-(3-(2-(pyrrolidin-1-yl)ethyl)phenoxy)-indan-1-one
0.00209
-
 pH 7.4, 37°C Rattus norvegicus 2-(3-(2-(diethylamino)ethyl)phenoxy)-5,6-dimethoxyindan-1-one
0.00237
-
 pH 7.4, 37°C Rattus norvegicus 2-(3-(3-(diethylamino)propanoyl)phenoxy)-5,6-dimethoxy-indan-1-one