1-(4-chlorophenyl)sulfonyl-N-[3-methoxy-4-(1-tetrazolyl)phenyl]-4-piperidinecarboxamide, also known as **AZD6765**, is a small molecule that acts as a **potent and selective inhibitor of the enzyme Bruton's tyrosine kinase (BTK)**.
**BTK** is a crucial enzyme in the B-cell receptor (BCR) signaling pathway, which plays a vital role in the development and activation of B lymphocytes. Inhibition of BTK disrupts this pathway, leading to the suppression of B-cell function and the inhibition of antibody production.
**AZD6765** is important for research due to its potential therapeutic applications in several diseases, including:
* **Chronic Lymphocytic Leukemia (CLL):** CLL is a type of blood cancer characterized by the overproduction of abnormal B-cells. AZD6765 has shown promising results in clinical trials for CLL, demonstrating significant efficacy in reducing tumor burden and improving overall survival.
* **Waldenström Macroglobulinemia (WM):** WM is another B-cell malignancy characterized by the production of monoclonal IgM antibodies. AZD6765 has also demonstrated clinical activity in WM, leading to reductions in IgM levels and improvements in symptoms.
* **Immune Thrombocytopenia (ITP):** ITP is an autoimmune disorder characterized by a low platelet count. AZD6765 is being investigated as a potential treatment for ITP due to its ability to modulate the immune system.
* **Other B-cell-mediated disorders:** AZD6765 is being explored for its potential to treat various other B-cell-mediated disorders, such as rheumatoid arthritis, lupus, and inflammatory bowel disease.
**Research on AZD6765** focuses on understanding its mechanism of action, its efficacy in different disease settings, its safety profile, and its potential to be developed into a safe and effective treatment for various B-cell-mediated disorders.
**In addition to its therapeutic potential, AZD6765 is also a valuable research tool for studying the role of BTK in various biological processes and for identifying novel targets for drug development.**
| ID Source | ID |
|---|---|
| PubMed CID | 646200 |
| CHEMBL ID | 1446015 |
| CHEBI ID | 109240 |
| Synonym |
|---|
| MLS000027869 , |
| MLS000889559 |
| smr000003878 |
| 1-(4-chloro-benzenesulfonyl)-piperidine-4-carboxylic acid (3-methoxy-4-tetrazol-1-yl-phenyl)-amide |
| CHEBI:109240 |
| 1-(4-chlorophenyl)sulfonyl-n-[3-methoxy-4-(tetrazol-1-yl)phenyl]piperidine-4-carboxamide |
| AKOS000703794 |
| HMS2489H10 |
| AB00398018-09 |
| CHEMBL1446015 |
| Q27188318 |
| 1-(4-chlorophenyl)sulfonyl-n-[3-methoxy-4-(1-tetrazolyl)phenyl]-4-piperidinecarboxamide |
| Class | Description |
|---|---|
| tetrazoles | An azole in which the five-membered heterocyclic aromatic skeleton contains four N atoms and one C atom. |
| [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 | 4.7718 | 0.0447 | 17.8581 | 100.0000 | AID485294; AID485341 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 22.3872 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
| 67.9K protein | Vaccinia virus | Potency | 17.7828 | 0.0001 | 8.4406 | 100.0000 | AID720580 |
| IDH1 | Homo sapiens (human) | Potency | 2.5119 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 39.8107 | 3.5481 | 19.5427 | 44.6684 | AID743266 |
| pyruvate kinase PKM isoform a | Homo sapiens (human) | Potency | 0.0100 | 0.0401 | 7.4590 | 31.6228 | AID1631; AID1634 |
| ubiquitin carboxyl-terminal hydrolase 2 isoform a | Homo sapiens (human) | Potency | 12.5893 | 0.6561 | 9.4520 | 25.1189 | AID927 |
| geminin | Homo sapiens (human) | Potency | 18.3564 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 0.5012 | 0.0158 | 12.3113 | 615.5000 | AID1461 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 25.1189 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | Potency | 12.5893 | 1.5849 | 13.0043 | 25.1189 | AID927 |
| [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) |
|---|---|---|---|---|---|---|---|
| Potassium inwardly-rectifying channel, subfamily J, member 1 | Homo sapiens (human) | EC50 (µMol) | 2.1783 | 0.6473 | 4.9711 | 9.3289 | AID2753 |
| [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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| 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. |
| 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. |
| [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] | ||