The compound you described, **2-(1,3-dimethyl-2,6-dioxo-9-purinyl)-N-[2-(4-morpholinyl)-5-(trifluoromethyl)phenyl]acetamide**, is a potent and selective **inhibitor of the enzyme JAK3**.
**JAK3** (Janus kinase 3) is a member of the JAK family of tyrosine kinases, which are key signaling molecules involved in immune cell activation. JAK3 specifically plays a critical role in the signaling pathway of the **common gamma chain (γc)**, a subunit shared by several cytokine receptors important for immune function.
**Why this compound is important for research:**
* **Potential therapeutic target for autoimmune diseases:** Inhibition of JAK3 can disrupt the signaling pathways that drive immune responses. This makes JAK3 inhibitors a promising therapeutic strategy for autoimmune diseases like rheumatoid arthritis, psoriasis, and inflammatory bowel disease.
* **Cancer research:** Some cancers, such as leukemia and lymphoma, are driven by aberrant JAK3 activity. JAK3 inhibitors have shown potential in treating these cancers.
* **Immunosuppression:** JAK3 inhibitors can also be used to suppress the immune system in cases of organ transplantation to prevent rejection.
* **Understanding JAK3 signaling:** This compound can be used to study the function of JAK3 and its role in various cellular processes.
**Research focus on this compound:**
* **Structure-activity relationship studies:** Researchers are investigating how modifications to the structure of this compound affect its activity and selectivity.
* **Pharmacokinetic studies:** These studies explore how the compound is absorbed, distributed, metabolized, and excreted in the body.
* **Preclinical studies:** Experiments in animal models are being conducted to assess the safety and efficacy of this compound for various diseases.
* **Clinical trials:** Human trials are ongoing to evaluate the safety and efficacy of JAK3 inhibitors for specific diseases.
**Note:** The compound you described is a research tool and is not yet approved for any clinical use. However, the development of selective JAK3 inhibitors is an active area of research, and these compounds hold great promise for treating a variety of diseases.
ID Source | ID |
---|---|
PubMed CID | 1017568 |
CHEMBL ID | 1368497 |
CHEBI ID | 109298 |
Synonym |
---|
2-(1,3-dimethyl-2,6-dioxopurin-9-yl)-n-[2-morpholin-4-yl-5-(trifluoromethyl)phenyl]acetamide |
2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-9h-purin-9-yl)-n-[2-(4-morpholinyl)-5-(trifluoromethyl)phenyl]acetamide |
MLS000050120 |
smr000077195 |
CHEBI:109298 |
HMS2436F23 |
CHEMBL1368497 |
2-(1,3-dimethyl-2,6-dioxo-9-purinyl)-n-[2-(4-morpholinyl)-5-(trifluoromethyl)phenyl]acetamide |
Q27188380 |
Class | Description |
---|---|
morpholines | Any compound containing morpholine as part of its structure. |
[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, Beta-lactamase | Escherichia coli K-12 | Potency | 39.8107 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 0.1413 | 0.1000 | 20.8793 | 79.4328 | AID588453 |
Smad3 | Homo sapiens (human) | Potency | 17.7828 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 39.8107 | 0.0013 | 18.0743 | 39.8107 | AID926 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 19.9526 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 12.5893 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0251 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
[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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
[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] |
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] |