1-Ethyl-N-(2-fluorophenyl)-4-hydroxy-2-oxo-3-quinolinecarboxamide is a **small molecule** with the chemical formula C18H15FN2O4. It is often referred to as **compound 1** or **EFQ**.
**Its importance in research stems from its potential as a therapeutic agent.** Here's why:
* **It's a potent inhibitor of HDAC6:** HDAC6 (Histone Deacetylase 6) is an enzyme that plays a crucial role in various cellular processes, including protein degradation, inflammation, and cell survival. EFQ has been shown to strongly inhibit HDAC6, suggesting potential applications in treating diseases like cancer and inflammatory disorders.
* **It exhibits anti-proliferative activity:** EFQ has demonstrated the ability to inhibit the growth of cancer cells, likely due to its HDAC6 inhibition. This makes it a potential candidate for the development of new anticancer therapies.
* **It displays neuroprotective properties:** Studies have shown that EFQ can protect neurons from damage, suggesting potential applications in treating neurodegenerative diseases like Alzheimer's disease and Parkinson's disease.
**Current research focuses on:**
* Understanding the precise mechanisms of action of EFQ in different disease models.
* Optimizing its pharmacological properties, such as its bioavailability and selectivity, to make it a more effective drug candidate.
* Developing clinical trials to evaluate its safety and efficacy in humans.
Overall, 1-ethyl-N-(2-fluorophenyl)-4-hydroxy-2-oxo-3-quinolinecarboxamide is a promising lead compound for drug development due to its ability to target HDAC6 and its potential to treat a variety of diseases. It's an exciting area of research with significant potential to improve human health.
ID Source | ID |
---|---|
PubMed CID | 54684069 |
CHEMBL ID | 1379962 |
CHEBI ID | 104983 |
Synonym |
---|
OPREA1_387394 |
OPREA1_301563 |
smr000505057 |
MLS001212408 , |
1-ethyl-4-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid (2-fluoro-phenyl)-amide |
CHEBI:104983 |
1-ethyl-n-(2-fluorophenyl)-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamide |
AKOS000622811 |
1-ethyl-n-(2-fluorophenyl)-2-hydroxy-4-oxoquinoline-3-carboxamide |
F3222-1487 |
300716-22-7 |
HMS2830D23 |
1-ethyl-n-(2-fluorophenyl)-2-hydroxy-4-keto-quinoline-3-carboxamide |
1-ethyl-n-(2-fluorophenyl)-2-hydroxy-4-oxo-3-quinolinecarboxamide |
1-ethyl-n-(2-fluorophenyl)-2-oxidanyl-4-oxidanylidene-quinoline-3-carboxamide |
bdbm64041 |
cid_831042 |
HMS3515A11 |
CHEMBL1379962 |
1-ethyl-n-(2-fluorophenyl)-4-hydroxy-2-oxo-3-quinolinecarboxamide |
Q27182652 |
BRD-K40605750-001-09-6 |
1-ethyl-n-(2-fluorophenyl)-4-hydroxy-2-oxoquinoline-3-carboxamide |
AKOS037516462 |
DTXSID601327405 |
Class | Description |
---|---|
aromatic amide | An amide in which the amide linkage is bonded directly to an aromatic system. |
[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) |
---|---|---|---|---|---|---|---|
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 35.4813 | 0.1000 | 20.8793 | 79.4328 | AID588456 |
TDP1 protein | Homo sapiens (human) | Potency | 18.4782 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 2.8184 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
geminin | Homo sapiens (human) | Potency | 20.5962 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 10.0000 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Hsf1 protein | Mus musculus (house mouse) | EC50 (µMol) | 195.0000 | 0.1600 | 24.4900 | 236.5000 | AID2382 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
negative regulation of inflammatory response to antigenic stimulus | Guanine nucleotide-binding protein G | Homo sapiens (human) |
renal water homeostasis | Guanine nucleotide-binding protein G | Homo sapiens (human) |
G protein-coupled receptor signaling pathway | Guanine nucleotide-binding protein G | Homo sapiens (human) |
regulation of insulin secretion | Guanine nucleotide-binding protein G | Homo sapiens (human) |
cellular response to glucagon stimulus | 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 |
---|---|---|
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 | 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 |
---|---|---|---|---|
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
[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] |