Page last updated: 2024-12-09

2-(4-fluorophenyl)-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

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.

Cross-References

ID SourceID
PubMed CID753357
CHEMBL ID1334701
CHEBI ID114929

Synonyms (14)

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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
triazolesAn 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 Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency50.11870.044717.8581100.0000AID485294
LuciferasePhotinus pyralis (common eastern firefly)Potency16.94410.007215.758889.3584AID588342
Nrf2Homo sapiens (human)Potency2.51190.09208.222223.1093AID624171
glp-1 receptor, partialHomo sapiens (human)Potency8.91250.01846.806014.1254AID624417
ClpPBacillus subtilisPotency28.18381.995322.673039.8107AID651965
ATAD5 protein, partialHomo sapiens (human)Potency16.08920.004110.890331.5287AID504466; AID504467
P53Homo sapiens (human)Potency44.66840.07319.685831.6228AID504706
pyruvate kinaseLeishmania mexicana mexicanaPotency25.11890.398113.744731.6228AID1721; AID1722
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency3.98110.01262.451825.0177AID485313
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency5.17350.00419.984825.9290AID504444
ras-related protein Rab-9AHomo sapiens (human)Potency1.12200.00022.621531.4954AID485297
survival motor neuron protein isoform dHomo sapiens (human)Potency35.48130.125912.234435.4813AID1458
Endothelin receptor type BRattus norvegicus (Norway rat)Potency25.11890.562315.160931.6228AID1721
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency25.11890.562315.160931.6228AID1721
Guanine nucleotide-binding protein GHomo sapiens (human)Potency0.89131.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. 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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. 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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. 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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability 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]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's3 (60.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.56

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.

MetricThis Compound (vs All)
Research Demand Index12.56 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.56)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]