2-(4-fluorophenyl)-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine is a chemical compound with the molecular formula C₁₅H₁₃FN₄. It's a heterocyclic compound containing a triazolopyrimidine core structure, and is often referred to by its shorter name, **FPT**.
**Importance in Research:**
FPT has gained significant interest in research due to its potential **pharmacological activities**, primarily as a **kinase inhibitor**. Kinases are enzymes that play critical roles in cell signaling pathways, and their dysregulation is implicated in various diseases, including cancer, inflammatory disorders, and neurological disorders.
**Specific Research Areas:**
* **Cancer Research:** FPT has demonstrated inhibitory activity against several kinases involved in cancer cell growth and proliferation, such as **Aurora kinases** and **CDK2**. This makes it a potential candidate for cancer treatment, either alone or in combination with other therapies.
* **Inflammation Research:** FPT has shown promise as an inhibitor of **MAPK kinases**, which are key regulators of inflammatory responses. This could potentially lead to new treatments for inflammatory diseases like rheumatoid arthritis and inflammatory bowel disease.
* **Neurological Disorders:** FPT's ability to modulate kinase activity in the brain has led to its investigation as a potential treatment for neurodegenerative disorders like Alzheimer's disease and Parkinson's disease.
**Current Status:**
FPT is currently in the **early stages of preclinical development**. More research is needed to fully understand its pharmacological properties, efficacy, and safety before it can be considered for clinical trials in humans.
**Key Points:**
* FPT is a heterocyclic compound with potential kinase inhibitory activity.
* It is being investigated for its therapeutic potential in cancer, inflammatory diseases, and neurological disorders.
* FPT is currently in preclinical development, and more research is required before it can be tested in humans.
It's crucial to note that the information provided is based on available research data and may not represent the complete understanding of FPT's properties and potential applications. Ongoing research will further clarify its therapeutic potential and potential limitations.
ID Source | ID |
---|---|
PubMed CID | 753357 |
CHEMBL ID | 1334701 |
CHEBI ID | 114929 |
Synonym |
---|
smr000120478 |
MLS000527904 , |
2-(4-fluoro-phenyl)-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine |
EU-0048027 |
STK015954 |
2-(4-fluorophenyl)-5,7-dimethyl[1,2,4]triazolo[1,5-a]pyrimidine |
CHEBI:114929 |
2-(4-fluorophenyl)-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine |
HMS2162B11 |
CCG-114415 |
AKOS005377698 |
HMS3308E11 |
CHEMBL1334701 |
Q27196773 |
Class | Description |
---|---|
triazoles | An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms. |
[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 | 50.1187 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 16.9441 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
Nrf2 | Homo sapiens (human) | Potency | 2.5119 | 0.0920 | 8.2222 | 23.1093 | AID624171 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 8.9125 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
ClpP | Bacillus subtilis | Potency | 28.1838 | 1.9953 | 22.6730 | 39.8107 | AID651965 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 16.0892 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
P53 | Homo sapiens (human) | Potency | 44.6684 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
pyruvate kinase | Leishmania mexicana mexicana | Potency | 25.1189 | 0.3981 | 13.7447 | 31.6228 | AID1721; AID1722 |
NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 3.9811 | 0.0126 | 2.4518 | 25.0177 | AID485313 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 5.1735 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 1.1220 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 35.4813 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
Endothelin receptor type B | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 0.5623 | 15.1609 | 31.6228 | AID1721 |
Endothelin-1 receptor | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 0.5623 | 15.1609 | 31.6228 | AID1721 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 0.8913 | 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 |
---|---|---|
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 |
---|---|---|---|---|
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. |
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. |
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 | |||
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 | |||
[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] |