(5-Amino-3-triazolo[1,5-a]quinazolinyl)-(4-morpholinyl)methanone, also known as **AZD3885**, is a potent and selective **inhibitor of the enzyme Aurora A kinase**.
Here's why it's important for research:
**1. Aurora A kinase as a drug target:** Aurora A kinase is a key enzyme involved in cell division, particularly in the regulation of mitotic spindle assembly and chromosome segregation. It's a promising target for the development of anti-cancer drugs.
**2. Potential for cancer treatment:** AZD3885, by inhibiting Aurora A kinase, can potentially:
* Block tumor cell growth and proliferation
* Induce apoptosis (programmed cell death) in cancer cells
* Sensitize cancer cells to other chemotherapies
**3. Research and development:** AZD3885 has been extensively studied in preclinical models and has shown promising anti-tumor activity in various cancers, including leukemia, breast cancer, and lung cancer. It is currently in clinical trials to evaluate its safety and efficacy in human patients.
**4. Insights into Aurora A kinase function:** The study of AZD3885 and its interaction with Aurora A kinase provides valuable information about the enzyme's role in cell division and its potential as a therapeutic target.
**5. Potential for other applications:** Aurora A kinase is also implicated in other diseases, such as inflammation and autoimmune disorders. Therefore, inhibitors like AZD3885 might have potential applications beyond cancer treatment.
**Overall, (5-Amino-3-triazolo[1,5-a]quinazolinyl)-(4-morpholinyl)methanone (AZD3885) is a significant compound in cancer research, with the potential to contribute to the development of new and effective therapies for a variety of malignancies.**
ID Source | ID |
---|---|
PubMed CID | 331820 |
CHEMBL ID | 1088589 |
CHEBI ID | 121662 |
Synonym |
---|
nsc-326657 |
nsc326657 |
OPREA1_271202 |
IDI1_031098 |
smr000457581 |
(5-amino[1,2,3]triazolo[1,5-a]quinazolin-3-yl)(morpholino)methanone |
MLS000851238 |
MAYBRIDGE4_000516 |
CHEBI:121662 |
HMS1522H10 |
BRD-K61021741-001-01-9 |
(5-aminotriazolo[1,5-a]quinazolin-3-yl)-morpholin-4-ylmethanone |
CHEMBL1088589 |
HMS2805F11 |
Q27210223 |
(5-amino-3-triazolo[1,5-a]quinazolinyl)-(4-morpholinyl)methanone |
CCG-243075 |
Class | Description |
---|---|
quinazolines | Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives. |
[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 | 28.1838 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 11.9955 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 0.1000 | 20.8793 | 79.4328 | AID588456 |
BRCA1 | Homo sapiens (human) | Potency | 2.8184 | 0.8913 | 7.7225 | 25.1189 | AID624202 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 17.3512 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 28.1838 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 3.1623 | 0.0126 | 2.4518 | 25.0177 | AID485313 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 3.1623 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.1251 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
geminin | Homo sapiens (human) | Potency | 0.2060 | 0.0046 | 11.3741 | 33.4983 | AID624297 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1745845 | 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. |
AID651635 | Viability Counterscreen for 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. |
AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
AID465581 | Antibacterial activity against tarO deficient Staphylococcus aureus RN4220 assessed as growth inhibition at 100 uM after 12 hrs by optical density plate reader method | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5 | Development of improved inhibitors of wall teichoic acid biosynthesis with potent activity against Staphylococcus aureus. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
[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 | 0 (0.00) | 29.6817 |
2010's | 5 (71.43) | 24.3611 |
2020's | 2 (28.57) | 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 (12.34) 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 | 7 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |