1-methylsulfonyl-N-(6,7,8,9-tetrahydrodibenzofuran-2-yl)-2,3-dihydroindole-5-sulfonamide is a chemical compound with a complex structure. It's commonly known by the code name **MK-8245** and is being studied as a potential **treatment for asthma**.
Here's why it's important for research:
* **Novel Mechanism of Action:** MK-8245 works by targeting the **CysLT1 receptor**. CysLT1 is a key receptor involved in the inflammatory response associated with asthma. By blocking this receptor, MK-8245 aims to reduce the airway inflammation and bronchoconstriction that characterize asthma. This mechanism differs from the commonly used treatments like inhaled corticosteroids, which primarily suppress inflammation, and leukotriene inhibitors, which target the leukotriene pathway.
* **Potential for Improved Efficacy:** Preclinical studies have shown that MK-8245 has the potential to be a more effective treatment for asthma compared to current medications. This could lead to better symptom control and improved quality of life for patients.
* **Potential for Reduced Side Effects:** MK-8245 is being investigated for its ability to potentially reduce side effects associated with current asthma treatments. For example, inhaled corticosteroids can have systemic side effects, while leukotriene inhibitors may cause liver dysfunction.
* **Development of New Treatments:** The development of new treatments for asthma, like MK-8245, is crucial given that current treatments are not always effective for all patients. Research into new targets and drugs could lead to more effective and personalized treatment options.
**It's important to note:**
* MK-8245 is still in the early stages of clinical development.
* Further research is needed to confirm its efficacy and safety in humans.
* Whether it will ultimately become an approved treatment for asthma is still uncertain.
However, the potential of this compound to provide a new approach for treating asthma is promising and fuels ongoing research efforts.
ID Source | ID |
---|---|
PubMed CID | 1251624 |
CHEMBL ID | 1331247 |
CHEBI ID | 107770 |
Synonym |
---|
smr000081437 |
MLS000052114 |
1-(methylsulfonyl)-n-(6,7,8,9-tetrahydrodibenzo[b,d]furan-2-yl)-5-indolinesulfonamide |
STK271489 |
1-(methylsulfonyl)-n-(6,7,8,9-tetrahydrodibenzo[b,d]furan-2-yl)-2,3-dihydro-1h-indole-5-sulfonamide |
MLS000911139 |
CHEBI:107770 |
AKOS003351406 |
1-methylsulfonyl-n-(6,7,8,9-tetrahydrodibenzofuran-2-yl)-2,3-dihydroindole-5-sulfonamide |
HMS2492A20 |
{[1-(methylsulfonyl)indolin-5-yl]sulfonyl}-1,2,3,4-tetrahydrobenzo[3,4-d]benzo [2,1-b]furan-8-ylamine |
CHEMBL1331247 |
Q27186103 |
SR-01000295188-1 |
sr-01000295188 |
Class | Description |
---|---|
sulfonamide | An amide of a sulfonic acid RS(=O)2NR'2. |
[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, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 17.7828 | 0.6310 | 35.7641 | 100.0000 | AID504339 |
Chain A, Cruzipain | Trypanosoma cruzi | Potency | 25.1189 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 28.1838 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 6.5131 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
USP1 protein, partial | Homo sapiens (human) | Potency | 4.4668 | 0.0316 | 37.5844 | 354.8130 | AID743255 |
TDP1 protein | Homo sapiens (human) | Potency | 23.7246 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Smad3 | Homo sapiens (human) | Potency | 22.3872 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 19.9526 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
IDH1 | Homo sapiens (human) | Potency | 31.6228 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 29.0929 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
huntingtin isoform 2 | Homo sapiens (human) | Potency | 35.4813 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 25.1189 | 0.0398 | 16.7842 | 39.8107 | AID995 |
ubiquitin carboxyl-terminal hydrolase 2 isoform a | Homo sapiens (human) | Potency | 10.0000 | 0.6561 | 9.4520 | 25.1189 | AID927 |
histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 10.0000 | 0.0103 | 23.8567 | 63.0957 | AID2662 |
geminin | Homo sapiens (human) | Potency | 20.5962 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 15.8489 | 0.0200 | 10.7869 | 31.6228 | AID912 |
Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 112.2020 | 6.3096 | 60.2008 | 112.2020 | AID720707 |
Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | Potency | 10.0000 | 1.5849 | 13.0043 | 25.1189 | AID927 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
[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] |