Page last updated: 2024-08-07 16:11:06
Acetylcholinesterase
An acetylcholinesterase that is encoded in the genome of mouse. [OMA:P21836, PRO:DNx]
Synonyms
AChE;
EC 3.1.1.7
Research
Bioassay Publications (31)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 3 (9.68) | 18.2507 |
| 2000's | 6 (19.35) | 29.6817 |
| 2010's | 18 (58.06) | 24.3611 |
| 2020's | 4 (12.90) | 2.80 |
Compounds (40)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tacrine | Mus musculus (house mouse) | Kd | 0.0180 | 1 | 1 |
| ambenonium | Mus musculus (house mouse) | Kd | 50.0000 | 2 | 2 |
| propidium iodide | Mus musculus (house mouse) | Kd | 1.1000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| orotidylic acid | Mus musculus (house mouse) | Km | 13.0000 | 1 | 2 |
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Design, synthesis, cholinesterase inhibition and molecular modelling study of novel tacrine hybrids with carbohydrate derivatives.Bioorganic & medicinal chemistry, , 11-01, Volume: 26, Issue:20, 2018
N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer's agents.Bioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor.Journal of medicinal chemistry, , Oct-09, Volume: 57, Issue:19, 2014
The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.Biochemistry, , Oct-22, Volume: 52, Issue:42, 2013
Lead optimization studies towards the discovery of novel carbamates as potent AChE inhibitors for the potential treatment of Alzheimer's disease.Bioorganic & medicinal chemistry, , Nov-01, Volume: 20, Issue:21, 2012
Fragment-based drug discovery.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology.Journal of medicinal chemistry, , Jul-19, Volume: 39, Issue:15, 1996
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.Biochemistry, , Oct-22, Volume: 52, Issue:42, 2013
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.Biochemistry, , Oct-22, Volume: 52, Issue:42, 2013
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , May-05, Volume: 235, 2022
[no title available]Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
Design, synthesis and pharmacological evaluation of some novel indanone derivatives as acetylcholinesterase inhibitors for the management of cognitive dysfunction.Bioorganic & medicinal chemistry, , 01-01, Volume: 26, Issue:1, 2018
Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
Synthesis of aminoalkyl-substituted aurone derivatives as acetylcholinesterase inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 23, Issue:1, 2015
Synthesis of aminoalkyl-substituted coumarin derivatives as acetylcholinesterase inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 22, Issue:4, 2014
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.Journal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Design and synthesis of newer potential 4-(N-acetylamino)phenol derived piperazine derivatives as potential cognition enhancers.Bioorganic chemistry, , Volume: 60, 2015
Lead optimization studies towards the discovery of novel carbamates as potent AChE inhibitors for the potential treatment of Alzheimer's disease.Bioorganic & medicinal chemistry, , Nov-01, Volume: 20, Issue:21, 2012
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.Journal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
Divergent structure-activity relationships of structurally similar acetylcholinesterase inhibitors.Journal of medicinal chemistry, , Oct-10, Volume: 56, Issue:19, 2013
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.Journal of medicinal chemistry, , Jun-12, Volume: 51, Issue:11, 2008
Fragment-based drug discovery.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010