(4-Chlorophenyl)-[4-(7-chloro-4-quinolinyl)-1-piperazinyl]methanone, also known as **Chloroquine**, is a well-known antimalarial drug. It is a synthetic compound that works by inhibiting the growth of the parasite that causes malaria, Plasmodium falciparum.
**Here's why it's important for research:**
* **Malaria Treatment:** Chloroquine is a mainstay in the treatment of malaria, particularly for uncomplicated P. falciparum malaria. Its effectiveness and affordability make it a crucial tool in malaria control efforts.
* **Mechanism of Action:** Understanding the mechanism of action of chloroquine is vital for developing new antimalarials. Researchers are constantly studying how chloroquine inhibits the parasite's growth, which can lead to the discovery of novel targets and drug candidates.
* **Drug Resistance:** Unfortunately, drug resistance is a significant threat to chloroquine's effectiveness. Research into chloroquine resistance is critical to understanding how the parasite develops resistance and to finding new treatments.
* **Other Potential Uses:** Chloroquine has also shown potential in treating other conditions, such as autoimmune diseases like rheumatoid arthritis and lupus. Research is ongoing to explore these possibilities.
**Additionally:**
* Chloroquine has been investigated as a potential antiviral agent, particularly against COVID-19. However, research in this area is still evolving, and its efficacy against the virus remains uncertain.
**Important Note:**
While Chloroquine is a valuable research tool and can be an effective treatment for malaria, it should only be used under the guidance of a healthcare professional. Self-medication can be dangerous.
ID Source | ID |
---|---|
PubMed CID | 1251584 |
CHEMBL ID | 1360505 |
CHEBI ID | 92634 |
SCHEMBL ID | 9978124 |
Synonym |
---|
AKOS000424799 |
MLS000676065 , |
7-chloro-4-[4-(4-chlorobenzoyl)-1-piperazinyl]quinoline |
smr000296226 |
(4-chlorophenyl)-[4-(7-chloroquinolin-4-yl)piperazin-1-yl]methanone |
(4-chlorophenyl)[4-(7-chloroquinolin-4-yl)piperazin-1-yl]methanone |
STK205927 |
BRD-K36111767-001-07-6 |
BRD-K36111767-001-05-0 |
ml #: ml189 |
HMS2706G19 |
CHEMBL1360505 |
MLS003179195 |
cid_1251584 |
(4-chlorophenyl)-[4-(7-chloro-4-quinolinyl)-1-piperazinyl]methanone |
[4-(7-chloranylquinolin-4-yl)piperazin-1-yl]-(4-chlorophenyl)methanone |
bdbm43528 |
(4-chlorophenyl)-[4-(7-chloro-4-quinolyl)piperazino]methanone |
SCHEMBL9978124 |
(4-chlorophenyl)-[4-(7-chloro-4-quinolyl)piperazin-1-yl]methanone |
CHEBI:92634 |
NCGC00386822-01 |
Q27164346 |
Z57723686 |
nsc-805858 |
nsc805858 |
337328-21-9 |
ml189 |
EN300-18305179 |
7-chloro-4-[4-(4-chlorobenzoyl)piperazin-1-yl]quinoline |
Excerpt | Reference | Relevance |
---|---|---|
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Class | Description |
---|---|
pyridines | Any organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives. |
piperazines | |
[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 | 25.1189 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 11.2202 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 29.0810 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 21.0441 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 15.8489 | 0.1800 | 13.5574 | 39.8107 | AID1460 |
Smad3 | Homo sapiens (human) | Potency | 7.0795 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.6008 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 10.0000 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
G | Vesicular stomatitis virus | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 8.4866 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
67.9K protein | Vaccinia virus | Potency | 12.5893 | 0.0001 | 8.4406 | 100.0000 | AID720579 |
IDH1 | Homo sapiens (human) | Potency | 29.0929 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 20.5962 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 39.8107 | 0.0398 | 16.7842 | 39.8107 | AID1454 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 100.0000 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 14.1406 | 0.0079 | 8.2332 | 1,122.0200 | AID2546; AID2551 |
survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 14.1254 | 0.1259 | 12.2344 | 35.4813 | AID1458 |
Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 100.0000 | 6.3096 | 60.2008 | 112.2020 | AID720709 |
Interferon beta | Homo sapiens (human) | Potency | 8.4866 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 39.8107 | 1.9953 | 25.5327 | 50.1187 | AID624288 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[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) |
---|---|---|---|---|---|---|---|
STAT3, partial | Homo sapiens (human) | IC50 (µMol) | 22.0200 | 0.0760 | 4.0758 | 8.6430 | AID1409 |
Gli1 | Mus musculus (house mouse) | IC50 (µMol) | 3.0100 | 0.0270 | 4.2939 | 11.4000 | AID602464 |
signal transducer and activator of transcription 1-alpha/beta isoform alpha | Homo sapiens (human) | IC50 (µMol) | 55.7000 | 9.2540 | 9.2540 | 9.2540 | AID1396 |
protein Wnt-3a precursor | Mus musculus (house mouse) | IC50 (µMol) | 8.3000 | 0.4410 | 4.9952 | 14.8000 | AID651570 |
[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) |
---|---|---|---|---|---|---|---|
heat shock protein 90 | Candida albicans | EC50 (µMol) | 100.2877 | 0.1200 | 6.4855 | 33.8530 | AID2387; AID2400; AID2423 |
calcineurin A1, putative | Candida dubliniensis CD36 | EC50 (µMol) | 180.0000 | 4.6630 | 6.3810 | 8.0990 | AID2388 |
[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) |
---|---|---|---|---|---|---|---|
LMP1 [Human herpesvirus 4] | human gammaherpesvirus 4 (Epstein-Barr virus) | AC50 | 52.8250 | 0.0680 | 39.9389 | 277.4300 | AID504861; AID504882 |
calcineurin A1, putative | Candida dubliniensis CD36 | AC50 | 0.6513 | 0.6513 | 1.9383 | 3.5430 | AID488836 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID616564 | Growth inhibition of Candida albicans isolate CaCi-2 at 1 uM after 48 hrs by Almar blue fluorimetry in presence of fluconazole | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. |
AID616560 | Antifungal activity against Candida albicans isolate CaCi-2 after 48 hrs by Almar blue fluorimetry | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. |
AID616557 | Growth inhibition of Candida albicans isolate CaCi-2 assessed as relative fungal growth in presence of Fluconazole after 48 hrs by Almar blue fluorometry | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. |
AID616559 | Aqueous solubility of the compound in phosphate buffered saline | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. |
AID616558 | Growth inhibition of Candida albicans isolate CaCi-8 assessed as relative fungal growth in presence of Fluconazole after 48 hrs by Almar blue fluorometry | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. |
AID616563 | Inhibition of calcineurin signaling pathway in Candida albicans | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. |
AID616565 | Growth inhibition of Candida albicans isolate CaCi-8 at 1 uM after 48 hrs by Almar blue fluorometry in presence of Fluconazole | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. |
AID616561 | Cytotoxicity in mouse NIH/3T3 cells after 48 hrs by Almar blue fluorimetry | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. |
AID616562 | Inhibition of HSP90 signaling pathway in Candida albicans | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates. |
[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 (11.11) | 29.6817 |
2010's | 5 (55.56) | 24.3611 |
2020's | 3 (33.33) | 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 (12.21) 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 | 9 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |