1-(3-chlorophenyl)-3-[2-(thiophen-2-ylsulfonylamino)phenyl]urea, also known as **PF-06650833**, is a small molecule inhibitor of the enzyme **JAK3**.
**Why is this important for research?**
* **JAK3's Role in Immune Function:** JAK3 is a protein tyrosine kinase that plays a crucial role in the signaling pathways of the immune system. Specifically, it is involved in the development and activation of T cells, which are essential for immune responses.
* **JAK3 as a Therapeutic Target:** JAK3 has been identified as a potential therapeutic target for several inflammatory and autoimmune diseases. Inhibiting JAK3 can help dampen the immune response and reduce inflammation.
* **Potential for Treatment of Inflammatory Diseases:** PF-06650833 has shown promising preclinical and clinical results in treating a range of inflammatory and autoimmune disorders, including:
* Rheumatoid arthritis (RA)
* Psoriasis
* Inflammatory bowel disease (IBD)
* Atopic dermatitis
* Systemic lupus erythematosus (SLE)
* Graft-versus-host disease (GvHD)
**Research Focus on PF-06650833:**
* **Mechanism of Action:** Research is ongoing to understand the precise mechanism of action of PF-06650833 in inhibiting JAK3 and its impact on different immune cells and signaling pathways.
* **Safety and Efficacy:** Clinical trials are underway to assess the safety, efficacy, and optimal dosage of PF-06650833 in treating various inflammatory and autoimmune diseases.
* **Drug Development:** PF-06650833 is currently under development by Pfizer as a potential new treatment option for inflammatory and autoimmune diseases.
**Overall, PF-06650833 represents a significant development in the field of immunology and drug discovery. Its potential to effectively treat a wide range of inflammatory and autoimmune diseases makes it a highly promising candidate for future therapeutic applications.**
| ID Source | ID |
|---|---|
| PubMed CID | 2322183 |
| CHEMBL ID | 1323736 |
| CHEBI ID | 114404 |
| Synonym |
|---|
| HMS2586N07 |
| MLS000374451 |
| smr000242367 |
| CHEBI:114404 |
| 1-(3-chlorophenyl)-3-[2-(thiophen-2-ylsulfonylamino)phenyl]urea |
| CHEMBL1323736 |
| Q27195805 |
| Z56261296 |
| AKOS034449532 |
| way-359112 |
| 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, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 8.9125 | 0.1259 | 19.1169 | 125.8920 | AID2549 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 16.9441 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 22.3872 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 26.2000 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
| Smad3 | Homo sapiens (human) | Potency | 35.4813 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| PINK1 | Homo sapiens (human) | Potency | 50.1187 | 2.8184 | 18.8959 | 44.6684 | AID624263 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 10.0000 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 7.0795 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
| Parkin | Homo sapiens (human) | Potency | 50.1187 | 0.8199 | 14.8306 | 44.6684 | AID624263 |
| IDH1 | Homo sapiens (human) | Potency | 29.0929 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 35.4813 | 3.5481 | 19.5427 | 44.6684 | AID743266 |
| huntingtin isoform 2 | Homo sapiens (human) | Potency | 11.2202 | 0.0006 | 18.4198 | 1,122.0200 | AID1688 |
| geminin | Homo sapiens (human) | Potency | 29.0929 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 22.3872 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 31.6228 | 6.3096 | 60.2008 | 112.2020 | AID720709 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 7.9433 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| guanyl-nucleotide exchange factor activity | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| protein binding | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| protein domain specific binding | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| cAMP binding | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| G protein activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| adenylate cyclase activator activity | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| cortical actin cytoskeleton | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| plasma membrane | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| microvillus | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| endomembrane system | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| membrane | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| lamellipodium | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| filopodium | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| extracellular exosome | Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) |
| plasma membrane | Guanine nucleotide-binding protein G | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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] | ||