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Literature summary for 3.1.1.8 extracted from

  • Darvesh, S.; McDonald, R.S.; Penwell, A.; Conrad, S.; Darvesh, K.V.; Mataija, D.; Gomez, G.; Caines, A.; Walsh, R.; Martin, E.
    Structure-activity relationships for inhibition of human cholinesterases by alkyl amide phenothiazine derivatives (2004), Bioorg. Med. Chem., 13, 211-222.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
10-(2,2-dimethylpropanoyl)-10H-phenothiazine relative potency EC 3.1.1.8 to EC 3.1.1.7 is 4.7 Homo sapiens
10-(2-ethylbutanoyl)-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-(3,3-dimethylbutanoyl)-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-(3-methylbutanoyl)-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-(chloroacetyl)-10H-phenothiazine relative potency EC 3.1.1.8 to EC 3.1.1.7 is 7.3 Homo sapiens
10-(cyclobutylcarbonyl)-10H-phenothiazine relative potency EC 3.1.1.8 to EC 3.1.1.7 is 11.6 Homo sapiens
10-(cycloheptylcarbonyl)-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-(cyclohexylacetyl)-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-(cyclohexylcarbonyl)-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-(cyclopentylacetyl)-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-(cyclopentylcarbonyl)-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-(cyclopropylcarbonyl)-10H-phenothiazine relative potency EC 3.1.1.8 to EC 3.1.1.7 is 1.9 Homo sapiens
10-(methoxyacetyl)-10H-phenothiazine relative potency EC 3.1.1.8 to EC 3.1.1.7 is 0.8 Homo sapiens
10-acetyl-10H-phenothiazine relative potency EC 3.1.1.8 to EC 3.1.1.7 is 1.1 Homo sapiens
10-butyryl-10H-phenothiazine relative potency EC 3.1.1.8 to EC 3.1.1.7 is 1.9 Homo sapiens
10-heptanoyl-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-hexanoyl-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-isobutyryl-10H-phenothiazine relative potency EC 3.1.1.8 to EC 3.1.1.7 is 2.7 Homo sapiens
10-pentanoyl-10H-phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
10-propionyl-10H-phenothiazine relative potency EC 3.1.1.8 to EC 3.1.1.7 is 1.8 Homo sapiens
chlorpromazine not inhibitory to EC 3.1.1.7 Homo sapiens
ethopropazine not inhibitory to EC 3.1.1.7 Homo sapiens
N-methylphenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens
phenothiazine not inhibitory to EC 3.1.1.7 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000166
-
ethopropazine pH 8.0, 23°C Homo sapiens
0.00086
-
10-(cycloheptylcarbonyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00126
-
10-(cyclohexylcarbonyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00168
-
10-(cyclohexylacetyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00222
-
10-(cyclopentylacetyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00359
-
10-(3,3-dimethylbutanoyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00421
-
10-(cyclopentylcarbonyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0048
-
10-(cyclobutylcarbonyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00633
-
10-(2,2-dimethylpropanoyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00637
-
10-hexanoyl-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00643
-
10-(2-ethylbutanoyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00646
-
10-(3-methylbutanoyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.00831
-
10-heptanoyl-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0102
-
10-pentanoyl-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0109
-
10-(chloroacetyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0132
-
10-isobutyryl-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0162
-
10-butyryl-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0231
-
10-(cyclopropylcarbonyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0256
-
10-propionyl-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0296
-
10-(methoxyacetyl)-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0318
-
phenothiazine pH 8.0, 23°C Homo sapiens
0.0322
-
chlorpromazine pH 8.0, 23°C Homo sapiens
0.0358
-
10-acetyl-10H-phenothiazine pH 8.0, 23°C Homo sapiens
0.0369
-
N-methylphenothiazine pH 8.0, 23°C Homo sapiens