2-(4-chlorophenyl)-5-(methylamino)-4-oxazolecarbonitrile is a **chemical compound** with the molecular formula C11H8ClN3O. It is also known by its common name, **SAR1386**.
**Importance in Research:**
SAR1386 is a research chemical with potential **pharmacological activity**. Specifically, it has been studied for its role as a **potent and selective inhibitor of the enzyme glycogen synthase kinase 3 (GSK-3)**.
**GSK-3** is a serine/threonine protein kinase involved in various cellular processes, including:
* **Regulation of glycogen synthesis:** GSK-3 inhibits glycogen synthase, the enzyme responsible for glycogen synthesis.
* **Cell growth and differentiation:** GSK-3 plays a role in cell cycle regulation and apoptosis.
* **Neurotransmission:** GSK-3 is implicated in neurodegenerative diseases such as Alzheimer's disease.
**Research on SAR1386:**
Research on SAR1386 has focused on its potential therapeutic applications in the following areas:
* **Diabetes:** As an inhibitor of GSK-3, SAR1386 may help regulate blood sugar levels and improve insulin sensitivity.
* **Neurodegenerative diseases:** By inhibiting GSK-3, SAR1386 may protect against neuronal damage and potentially slow the progression of neurodegenerative diseases like Alzheimer's disease.
* **Cancer:** Some studies suggest that GSK-3 inhibitors may have anti-cancer properties by affecting cell growth and survival.
**Note:**
It's crucial to understand that SAR1386 is still in the **research phase** and is not currently approved for any medical use. Its safety and efficacy in humans have not been fully established.
Further research is needed to investigate its potential therapeutic applications and determine its safety profile before it can be considered for clinical use.
ID Source | ID |
---|---|
PubMed CID | 661037 |
CHEMBL ID | 1547372 |
CHEBI ID | 121992 |
Synonym |
---|
AKOS002347960 |
NCGC00019649-02 |
smr000036828 |
MLS000036624 |
NCGC00019649-01 |
CHEBI:121992 |
STK896228 |
2-(4-chlorophenyl)-5-(methylamino)-1,3-oxazole-4-carbonitrile |
NCGC00019649-03 |
HMS2466N22 |
bdbm50011743 |
CHEMBL1547372 , |
2-(4-chlorophenyl)-5-(methylamino)-4-oxazolecarbonitrile |
Q27210617 |
Class | Description |
---|---|
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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 25.1189 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 28.1838 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 10.6910 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 39.8107 | 0.1000 | 20.8793 | 79.4328 | AID588453; AID588456 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 13.0816 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 7.9433 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
lysosomal alpha-glucosidase preproprotein | Homo sapiens (human) | Potency | 24.9271 | 0.0366 | 19.6376 | 50.1187 | AID2100 |
NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 2.5119 | 0.0126 | 2.4518 | 25.0177 | AID485313 |
polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 19.9526 | 1.0000 | 12.2326 | 31.6228 | AID2162 |
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 3.5481 | 0.0018 | 15.6638 | 39.8107 | AID894 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 14.5810 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 3.5481 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 0.3548 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 5.6234 | 1.0000 | 10.4756 | 28.1838 | AID1457 |
[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) |
---|---|---|---|---|---|---|---|
Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) | IC50 (µMol) | 25.0000 | 0.0400 | 2.0998 | 10.0000 | AID1138905 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
arachidonate 12(S)-lipoxygenase activity | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
iron ion binding | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
protein binding | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
phosphatidylinositol-4,5-bisphosphate binding | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
linoleate 13S-lipoxygenase activity | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
arachidonate 15-lipoxygenase activity | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Process | via Protein(s) | Taxonomy |
---|---|---|
lipid droplet | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
cytosol | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
plasma membrane | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
cytoplasmic side of plasma membrane | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
membrane | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
plasma membrane | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
cytosol | Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
AID1138905 | Inhibition of recombinant N-terminal His6-tagged human reticulocyte 12/15-lipoxygenase using arachidonic acid as substrate by UV-vis spectrometric analysis | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10 | Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies. |
[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 (16.67) | 29.6817 |
2010's | 4 (66.67) | 24.3611 |
2020's | 1 (16.67) | 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 (12.35) 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 | 6 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |