2-(4-chlorophenyl)-N-[2-(4-morpholinyl)ethyl]-4-quinazolinamine, also known as **CI-994**, is a compound that has shown promising activity as a **selective inhibitor of the enzyme Aurora kinase A**.
**Aurora kinase A** is a protein kinase that plays a crucial role in cell division, particularly in the process of mitosis. It is involved in regulating microtubule formation and chromosome segregation.
**Why CI-994 is important for research:**
* **Potential anti-cancer agent:** Aurora kinase A is often overexpressed in various cancer types, leading to uncontrolled cell growth and proliferation. CI-994's selective inhibition of this kinase has made it a promising candidate for the development of new cancer therapies.
* **Investigating Aurora kinase A's role in cell division:** CI-994 can be used as a tool to study the function of Aurora kinase A in normal and cancerous cells. By inhibiting its activity, researchers can investigate its role in various cellular processes and identify potential therapeutic targets.
* **Understanding the mechanism of action:** Studying CI-994's interactions with Aurora kinase A can provide valuable insights into the enzyme's structure and function, which can be used to design more effective and specific inhibitors.
**Current research on CI-994:**
* **Preclinical studies:** CI-994 has demonstrated anti-tumor activity in various preclinical models of cancer.
* **Clinical trials:** While CI-994 has not yet been approved for clinical use, there are ongoing clinical trials evaluating its safety and efficacy in patients with different cancer types.
**In summary,** CI-994 is a significant compound in cancer research due to its selective inhibition of Aurora kinase A and its potential as a novel anti-cancer therapeutic. Further research and clinical trials are ongoing to explore its full potential and its role in understanding the intricate mechanisms of cell division.
ID Source | ID |
---|---|
PubMed CID | 1181447 |
CHEMBL ID | 1484660 |
CHEBI ID | 123312 |
Synonym |
---|
CBMICRO_031912 |
BIM-0031984.P001 |
OPREA1_000153 |
NEURO1_000676 |
CHEMDIV1_010473 |
smr000107606 |
MLS000111684 , |
CHEBI:123312 |
HMS616M01 |
2-(4-chlorophenyl)-n-(2-morpholin-4-ylethyl)quinazolin-4-amine |
AKOS001673401 |
HMS2391E10 |
CHEMBL1484660 |
[2-(4-chlorophenyl)quinazolin-4-yl]-(2-morpholinoethyl)amine |
cid_1181447 |
bdbm30980 |
2-(4-chlorophenyl)-n-[2-(4-morpholinyl)ethyl]-4-quinazolinamine |
SR-01000495435-1 |
sr-01000495435 |
Q27213021 |
mfcd02079956 |
2-(4-chlorophenyl)-n-[2-(morpholin-4-yl)ethyl]quinazolin-4-amine |
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, Beta-lactamase | Escherichia coli K-12 | Potency | 28.1838 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 22.3872 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
TDP1 protein | Homo sapiens (human) | Potency | 29.0929 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 21.4509 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 1.0000 | 0.0013 | 18.0743 | 39.8107 | AID926 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 10.0000 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
IDH1 | Homo sapiens (human) | Potency | 19.9526 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 70.7946 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 19.9526 | 0.0398 | 16.7842 | 39.8107 | AID995 |
flap endonuclease 1 | Homo sapiens (human) | Potency | 79.4328 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
geminin | Homo sapiens (human) | Potency | 24.8446 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 12.5893 | 0.0200 | 10.7869 | 31.6228 | AID912 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
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. |
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. |
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. |
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 | |||
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. |
[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] |