**[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl]-[(3R)-2,3-dihydro-1,4-benzodioxin-3-yl]methanone** is a complex organic molecule with a long and descriptive chemical name. It's more commonly referred to by its simpler name, **SB-203580**, and it's a research tool with significant importance in the field of **biology and drug discovery**.
**Here's why it's important:**
* **p38 MAP Kinase Inhibitor:** SB-203580 is a potent and selective inhibitor of the **p38 mitogen-activated protein kinase (MAPK)**. p38 MAPK is a key enzyme involved in inflammatory responses, cell growth, and apoptosis (programmed cell death).
* **Research Tool for Inflammation and Disease:** By inhibiting p38 MAPK, SB-203580 helps researchers understand the role of this enzyme in various diseases, including:
* **Inflammatory diseases:** Conditions like rheumatoid arthritis, inflammatory bowel disease, and asthma are linked to p38 MAPK activation.
* **Neurodegenerative disorders:** p38 MAPK is implicated in Alzheimer's disease and Parkinson's disease.
* **Cancer:** p38 MAPK can contribute to tumor growth and metastasis.
* **Drug Discovery:** SB-203580 serves as a starting point for developing new drugs that target p38 MAPK. By understanding its interactions with the enzyme, researchers can design more effective and specific inhibitors for treating inflammatory diseases and other conditions.
**Key Points to Remember:**
* **SB-203580 is a research tool, not a medicine.** It's not approved for use in treating patients.
* **The structure of the molecule is complex.** It's important to note that the chemical name is a precise description of the molecule's composition and arrangement of atoms.
* **p38 MAPK is a vital target for drug discovery.** By inhibiting this enzyme, researchers hope to develop novel treatments for a wide range of diseases.
If you're interested in learning more about SB-203580 and p38 MAPK, I recommend searching for scientific articles and publications on these topics.
| ID Source | ID |
|---|---|
| PubMed CID | 6604102 |
| CHEMBL ID | 1363589 |
| CHEBI ID | 95247 |
| SCHEMBL ID | 97513 |
| Synonym |
|---|
| NCGC00018158-01 |
| MLS001165720 |
| smr000550476 |
| [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-[(3r)-2,3-dihydro-1,4-benzodioxin-3-yl]methanone |
| NCGC00018158-04 |
| HMS2233L12 |
| SCHEMBL97513 |
| CHEMBL1363589 |
| r-doxazosin |
| 70918-17-1 |
| doxazosin, (r)- |
| F6HQ441M9W , |
| piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(((2r)-2,3-dihydro-1,4-benzodioxin-2-yl)carbonyl)- |
| piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((2,3-dihydro-1,4-benzodioxin-2-yl)carbonyl)-, (r)- |
| (4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl)((2r)-2,3-dihydro-1,4-benzodioxin-2-yl)methanone |
| methanone, (4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl)((2r)-2,3-dihydro-1,4-benzodioxin-2-yl)- |
| unii-f6hq441m9w |
| CHEBI:95247 |
| Q27167084 |
| [4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl]-[(3r)-2,3-dihydro-1,4-benzodioxin-3-yl]methanone |
| (r)-(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl)(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanone |
| EN300-19631171 |
| 2-{4-[(2r)-2,3-dihydro-1,4-benzodioxine-2-carbonyl]piperazin-1-yl}-6,7-dimethoxyquinazolin-4-amine |
| PD132712 |
| Class | Description |
|---|---|
| N-arylpiperazine | |
| [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, Ferritin light chain | Equus caballus (horse) | Potency | 22.3872 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
| acid sphingomyelinase | Homo sapiens (human) | Potency | 25.1189 | 14.1254 | 24.0613 | 39.8107 | AID504937 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 89.1251 | 0.1000 | 20.8793 | 79.4328 | AID588456 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 0.2908 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
| glucocerebrosidase | Homo sapiens (human) | Potency | 22.3872 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 56.2341 | 0.7079 | 36.9043 | 89.1251 | AID504333 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 70.7946 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 31.6228 | 0.0103 | 23.8567 | 63.0957 | AID2662 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 6.3096 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
| [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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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] | ||