Page last updated: 2024-12-09

2-(3-chlorophenyl)-5-(prop-2-enylamino)-4-oxazolecarbonitrile

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

2-(3-chlorophenyl)-5-(prop-2-enylamino)-4-oxazolecarbonitrile, also known as **GW842507X**, is a **potent and selective inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4)**.

Here's why it's important for research:

* **Diabetes Treatment:** DPP-4 is a key enzyme involved in the degradation of incretin hormones, like GLP-1 and GIP, which play a crucial role in regulating blood glucose levels. Inhibiting DPP-4 allows these incretins to persist in the bloodstream for longer, leading to increased insulin secretion and improved glucose control. This makes GW842507X a promising candidate for the treatment of type 2 diabetes.
* **Metabolic Disorders:** DPP-4 inhibition has also been linked to benefits in other metabolic disorders, such as obesity and cardiovascular disease.
* **Drug Development:** GW842507X has served as a valuable tool in understanding the role of DPP-4 in various physiological processes. Its high selectivity and potency have made it a useful model compound for the development of novel DPP-4 inhibitors with improved therapeutic properties.
* **Research into DPP-4:** GW842507X's ability to inhibit DPP-4 has allowed researchers to study the enzyme's function in more detail and explore its potential involvement in other biological processes.

**It's important to note that:**

* While GW842507X holds promise as a potential drug, it is not currently commercially available.
* Further research is ongoing to evaluate its safety and efficacy in humans.

Overall, 2-(3-chlorophenyl)-5-(prop-2-enylamino)-4-oxazolecarbonitrile (GW842507X) is a significant research tool that has contributed to our understanding of DPP-4 and its potential as a target for drug development. It is a potent and selective inhibitor of DPP-4, which makes it valuable for studying the role of this enzyme in various metabolic disorders and for developing new treatments for diabetes and other related conditions.

Cross-References

ID SourceID
PubMed CID2218783
CHEMBL ID1551144
CHEBI ID92521

Synonyms (15)

Synonym
NCGC00183415-01
MLS002276476
smr001318014
STK896026
2-(3-chlorophenyl)-5-(prop-2-en-1-ylamino)-1,3-oxazole-4-carbonitrile
2-(3-chlorophenyl)-5-(prop-2-enylamino)-1,3-oxazole-4-carbonitrile
HMS2215E04
AKOS005636253
HMS3329D13
CHEMBL1551144
CHEBI:92521
SR-01000284442-1
sr-01000284442
Q27164251
2-(3-chlorophenyl)-5-(prop-2-enylamino)-4-oxazolecarbonitrile
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
1,3-oxazoles
[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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATAD5 protein, partialHomo sapiens (human)Potency23.09990.004110.890331.5287AID504467
Smad3Homo sapiens (human)Potency35.48130.00527.809829.0929AID588855
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.12510.354828.065989.1251AID504847
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency50.11873.548119.542744.6684AID743266
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency70.79460.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency29.09290.004611.374133.4983AID624296; AID624297
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency24.64330.060110.745337.9330AID485367; AID504636; AID504637
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
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.
AID651635Viability Counterscreen for Primary 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.
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.
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
[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]