Qiu, Hui published the artcileDiscovery of potent and selective reversible Bruton’s tyrosine kinase inhibitors, Quality Control of 76283-09-5, the publication is Bioorganic & Medicinal Chemistry (2021), 116163, database is CAplus and MEDLINE.
Bruton’s tyrosine kinase (BTK) is a cytoplasmic, non-receptor tyrosine kinase member of the TEC family of tyrosine kinases. Pre-clin. and clin. data have shown that targeting BTK can be used for the treatment for B-cell disorders. Here we disclose the discovery of a novel imidazo[4,5-b]pyridine series of potent, selective reversible BTK inhibitors through a rational design approach. From a starting hit mol. I, medicinal chem. optimization led to the development of a lead compound II, which exhibited 58 nM BTK inhibitory potency in human whole blood and high kinome selectivity. Addnl., the compound demonstrated favorable pharmacokinetics (PK), and showed potent dose-dependent efficacy in a rat CIA model.
Bioorganic & Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, Quality Control of 76283-09-5.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary