Protein Variants | Comment | Organism |
---|---|---|
A328F | the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme | Homo sapiens |
A328W | the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme | Homo sapiens |
A328Y | the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme | Homo sapiens |
A539T | the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme | Homo sapiens |
D70G | the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme | Homo sapiens |
F329A | the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme | Homo sapiens |
Y332A | the mutant is more sensitive to aryl phenothiazine carbamate inhibitors and deactivation, i.e. 4-biphenyl phenothiazine carbamate, compared to the wild-type enzyme | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-naphthyl phenothiazine carbamate | - |
Homo sapiens | |
2-(1-piperidinyl)ethyl phenothiazine carbamate | - |
Homo sapiens | |
2-(1-pyrrolidinyl)ethyl phenothiazine carbamate | - |
Homo sapiens | |
2-(4-morpholino)ethyl phenothiazine carbamate | - |
Homo sapiens | |
2-(diethylamino)ethyl 10H-phenothiazine-10-carboxylate | - |
Homo sapiens | |
2-(dimethylamino)ethyl 10H-phenothiazine-10-carboxylate | - |
Homo sapiens | |
2-chlorophenyl phenothiazine carbamate | - |
Homo sapiens | |
2-methoxyphenyl phenothiazine carbamate | - |
Homo sapiens | |
2-methylphenyl phenothiazine carbamate | - |
Homo sapiens | |
2-naphthyl phenothiazine carbamate | - |
Homo sapiens | |
2-t-butylphenyl phenothiazine carbamate | - |
Homo sapiens | |
3-(diethylamino)propyl 10H-phenothiazine-10-carboxylate | - |
Homo sapiens | |
3-(N,N-dimethylamino) phenyl phenothiazine carbamate | binding by residues F329 and Y332, structure, overview | Homo sapiens | |
3-chlorophenyl phenothiazine carbamate | - |
Homo sapiens | |
3-methoxyphenyl phenothiazine carbamate | - |
Homo sapiens | |
3-methylphenyl phenothiazine carbamate | - |
Homo sapiens | |
4-biphenyl phenothiazine carbamate | - |
Homo sapiens | |
4-chlorophenyl phenothiazine carbamate | - |
Homo sapiens | |
4-methoxyphenyl phenothiazine carbamate | - |
Homo sapiens | |
4-methylphenyl phenothiazine carbamate | - |
Homo sapiens | |
4-t-butylphenyl phenothiazine carbamate | - |
Homo sapiens | |
butyl carbamate | - |
Homo sapiens | |
cyclopentyl phenothiazine carbamate | - |
Homo sapiens | |
donepezil | - |
Homo sapiens | |
ethyl carbamate | - |
Homo sapiens | |
galanthamine | - |
Homo sapiens | |
iso-propyl carbamate | - |
Homo sapiens | |
methyl carbamate | - |
Homo sapiens | |
additional information | inhibitor molecular mechanics calculations, general mechanism of pseudoirreversible cholinesterase inhibition by carbamates. Enzyme deactivation is initiated by nucleophilic attack of the catalytic triad serine oxygen on the carbonyl group of the carbamate, structure-activity relationships of wild-type and mutant enzymes, overview | Homo sapiens | |
phenyl phenothiazine carbamate | - |
Homo sapiens | |
propyl phenothiazine carbamate | - |
Homo sapiens | |
rivastigmine | - |
Homo sapiens | |
tert-butyl 10H-phenothiazine-10-carboxylate | - |
Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
extracellular | - |
Homo sapiens | - |
- |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
plasma | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
butyrylthiocholine + H2O | detection using 5,5'-dithiobis(2-nitrobenzoic acid) | Homo sapiens | butyrate + thiocholine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
BuChE | - |
Homo sapiens |
butyrylcholinesterase | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
23 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | molecular mechanics calculations and inhibition kinetics, overview | Homo sapiens | |
0.0006 | - |
2-(diethylamino)ethyl 10H-phenothiazine-10-carboxylate | 23°C | Homo sapiens | |
0.00065 | - |
2-(1-pyrrolidinyl)ethyl phenothiazine carbamate | 23°C | Homo sapiens | |
0.00074 | - |
3-(diethylamino)propyl 10H-phenothiazine-10-carboxylate | 23°C | Homo sapiens | |
0.0024 | - |
2-(4-morpholino)ethyl phenothiazine carbamate | 23°C | Homo sapiens | |
0.0025 | - |
2-(dimethylamino)ethyl 10H-phenothiazine-10-carboxylate | 23°C | Homo sapiens | |
0.0032 | - |
2-(1-piperidinyl)ethyl phenothiazine carbamate | 23°C | Homo sapiens | |
0.0032 | - |
cyclopentyl phenothiazine carbamate | 23°C | Homo sapiens | |
0.0043 | - |
tert-butyl 10H-phenothiazine-10-carboxylate | 23°C | Homo sapiens | |
0.0102 | - |
methyl carbamate | 23°C | Homo sapiens | |
0.0134 | - |
n-butyl carbamate | 23°C | Homo sapiens | |
0.0181 | - |
iso-propyl carbamate | 23°C | Homo sapiens | |
0.0234 | - |
ethyl carbamate | 23°C | Homo sapiens | |
0.26 | - |
propyl phenothiazine carbamate | 23°C | Homo sapiens |