| + |
ACHE | down-regulates quantity 
chemical modification
|
acetylcholine |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-253983 |
|
|
|
|
| pmid |
sentence |
| 15841900 |
Acetylcholinesterase (AChE) is one of the most crucial enzymes for nerve response and function. AChE catalyzes the hydrolysis of acylcholine esters with a relative specificity for acetylcholine.|The intracellular effects of acetylcholine are mediated by the activation of nicotinic and muscarinic acetylcholine receptors (AChRs). AChE terminates transmission of neuronal impulses by rapid hydrolysis of acetylcholine. |
|
| Publications: |
1 |
| + |
edrophonium | down-regulates activity
chemical inhibition
|
ACHE |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258667 |
|
|
in vitro |
|
| pmid |
sentence |
| 9301662 |
With the aim of performing a rigorous test of the anti-AChE properties of our compounds, the kinetics of enzyme inhibition were studied in purified enzyme preparations. The inhibition data are shown in Table 1. Additionally, known competitive inhibitors of AChE (procainamide and edrophonium) were included in the study for comparative purposes. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
3-[(2-Bromo-4,5-dimethoxyphenyl)methyl]-2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one | down-regulates activity
chemical inhibition
|
ACHE |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257760 |
|
|
Homo sapiens |
Serum |
| pmid |
sentence |
| 17888667 |
AChE inhibitory activity study was carried out by using Ellman colorimetric assay with neostigmine as a reference standard against targets from different species, such as pure electric eel AChE, human serum AChE, and rat brain AChE. Among the compounds synthesized, compounds 5a, 5b, 5j showed good inhibition against AChE. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
neostigmine | down-regulates activity
chemical inhibition
|
ACHE |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257758 |
|
|
Homo sapiens |
Serum |
| pmid |
sentence |
| 17888667 |
AChE inhibitory activity study was carried out by using Ellman colorimetric assay with neostigmine as a reference standard against targets from different species, such as pure electric eel AChE, human serum AChE, and rat brain AChE. Among the compounds synthesized, compounds 5a, 5b, 5j showed good inhibition against AChE. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
pralidoxime | up-regulates activity 
chemical activation
|
ACHE |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257889 |
|
|
in vitro |
|
| pmid |
sentence |
| 21215642 |
These compounds were synthesized, evaluated in vitro on human AChE (hAChE) inhibited by tabun, paraoxon, methylparaoxon and DFP and then compared to commercial hAChE reactivators (pralidoxime, HI-6, trimedoxime, obidoxime, methoxime) or previously prepared compounds (K027, K203). Three of these novel compounds showed a promising ability to reactivate hAChE comparable or better than the used standards. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
Pyridostigmine | down-regulates activity
chemical inhibition
|
ACHE |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257879 |
|
|
in vitro |
|
| pmid |
sentence |
| 20627738 |
The compounds 3-[(dimethylamino)carboxyl]oxy]-N,N,N-trimethylammonium methyl sulfate, better known as neostigmine methyl sulfate (3),1 and 3-[(dimethylcarbamoyl)oxy]-1-methylpyridinium bromide, pyridostigmine bromide (4)2 (Figure 1) are well known peripheral cholinesterase inhibitors |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
Galanthamine hydrobromide | down-regulates
chemical inhibition
|
ACHE |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-192583 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
3-[(4-Bromophenyl)methyl]-2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one | down-regulates activity
chemical inhibition
|
ACHE |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257761 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 17888667 |
AChE inhibitory activity study was carried out by using Ellman colorimetric assay with neostigmine as a reference standard against targets from different species, such as pure electric eel AChE, human serum AChE, and rat brain AChE. Among the compounds synthesized, compounds 5a, 5b, 5j showed good inhibition against AChE. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
procainamide | down-regulates activity
chemical inhibition
|
ACHE |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258668 |
|
|
in vitro |
|
| pmid |
sentence |
| 9301662 |
With the aim of performing a rigorous test of the anti-AChE properties of our compounds, the kinetics of enzyme inhibition were studied in purified enzyme preparations. The inhibition data are shown in Table 1. Additionally, known competitive inhibitors of AChE (procainamide and edrophonium) were included in the study for comparative purposes. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
4'-((2-Butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile | down-regulates activity
chemical inhibition
|
ACHE |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257759 |
|
|
Homo sapiens |
Serum |
| pmid |
sentence |
| 17888667 |
AChE inhibitory activity study was carried out by using Ellman colorimetric assay with neostigmine as a reference standard against targets from different species, such as pure electric eel AChE, human serum AChE, and rat brain AChE. Among the compounds synthesized, compounds 5a, 5b, 5j showed good inhibition against AChE. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
ACHE
- 
- 