**2-(3-methylphenoxy)-N-[4-(4-methylsulfonyl-1-piperazinyl)phenyl]acetamide** is a chemical compound, often referred to by its shorthand name **MK-0457**, that has shown potential as a **selective serotonin reuptake inhibitor (SSRI)**.
**Importance for Research:**
* **Potential Antidepressant Activity:** SSRIs are a class of drugs commonly used to treat depression. MK-0457's ability to inhibit serotonin reuptake suggests it could potentially be an effective antidepressant.
* **Selectivity:** MK-0457 exhibits selectivity for serotonin reuptake over other neurotransmitter transporters, which might translate into fewer side effects compared to non-selective SSRIs.
* **Novel Structure:** The unique chemical structure of MK-0457 distinguishes it from existing SSRIs, making it a promising candidate for further research and potential development as a new antidepressant drug.
* **Mechanism of Action:** Understanding how MK-0457 interacts with serotonin transporters could provide insights into the underlying mechanisms of depression and the development of new therapeutic strategies.
* **Preclinical Studies:** Research on MK-0457 has involved preclinical studies in animal models, which have shown encouraging results regarding its antidepressant effects and safety profile.
**Current Status:**
While MK-0457 has demonstrated potential as an SSRI in preclinical research, it has not progressed to clinical trials for human use. Further research is needed to fully evaluate its safety and efficacy in humans.
**Note:** It is crucial to remember that preclinical studies are not always predictive of human outcomes. While MK-0457 appears promising, further research is essential before any potential clinical applications can be considered.
ID Source | ID |
---|---|
PubMed CID | 652920 |
CHEMBL ID | 1562453 |
CHEBI ID | 106003 |
Synonym |
---|
smr000014653 |
n-[4-(4-methanesulfonyl-piperazin-1-yl)-phenyl]-2-m-tolyloxy-acetamide |
2-(3-methylphenoxy)-n-{4-[4-(methylsulfonyl)piperazin-1-yl]phenyl}acetamide |
STK174320 |
MLS000030235 |
CHEBI:106003 |
AKOS000462589 |
2-(3-methylphenoxy)-n-[4-(4-methylsulfonylpiperazin-1-yl)phenyl]acetamide |
HMS2371H14 |
AB00403448-08 |
CHEMBL1562453 |
2-(3-methylphenoxy)-n-[4-(4-methylsulfonyl-1-piperazinyl)phenyl]acetamide |
Q27183799 |
Class | Description |
---|---|
piperazines | |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Cruzipain | Trypanosoma cruzi | Potency | 39.8107 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 2.8184 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 31.6228 | 0.0013 | 18.0743 | 39.8107 | AID926 |
DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 3.9811 | 0.1000 | 28.9256 | 213.3130 | AID588591 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 112.2020 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
lethal(3)malignant brain tumor-like protein 1 isoform I | Homo sapiens (human) | Potency | 6.3096 | 0.0752 | 15.2253 | 39.8107 | AID485360 |
lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 3.1623 | 0.0200 | 10.7869 | 31.6228 | AID912 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (20.00) | 29.6817 |
2010's | 3 (60.00) | 24.3611 |
2020's | 1 (20.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.56) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |