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Molecular properties generated using the CDK
|Compound class||Synthetic organic|
|example 90 [US20160264548]|
|This compound is reported as an irreversible, covalent inhibitor of Bruton's tyrosine kinase (BTK) . It is compound 23 (example 90) as claimed in Merck's patent US20160264548A1 .
Because of its expression pattern on B cells, macrophages, neutrophils, and monocytes (NOT T cells) and its essential role in B lymphocyte development and function, BTK continues to be investigated as a valid therapeutic target for the treatment of diseases that involve B-cell and/or macrophage activation (e.g. B-cell malignancies, asthma and rheumatoid arthritis). Ibrutinib was the first-in-class small molecule BTK inhibitor to reach the clinic. Unfortunately, ibrutinib causes severe adverse effects that are in the main, attributed to its off-target profile. As a result, second-generation BTK inhibitors with optimised structures and improved selectivity are being developed. Inhibitor 16 described here, exhibits comparable cellular potency to ibrutinib but has a higher kinome selectivity against undesirable off-targets.
|GtoPdb PubChem SID||375973263|
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