In 2014,Sharp, Phillip P.; Garnier, Jean-Marc; Huang, David C. S.; Burns, Christopher J. published 《Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition》.MedChemComm published the findings.Related Products of 847818-74-0 The information in the text is summarized as follows:
The ability of various functional groups to engage the acetyl-lysine (KAc) binding site within bromo- and extra-terminal domain (BET) protein family members BRD2, BRD3 and BRD4 was evaluated by screening small mol. fragments – coupled to a known arylsulfonamide scaffold – in biochem. inhibition assays. Useful structure activity relationships have been established and novel functional groups that bind to the KAc binding pocket identified. Addnl. microsomal degradation studies were also undertaken revealing significant differences in metabolic stability between two commonly employed BET inhibitor fragments. In addition to this study using 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole, there are many other studies that have used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Related Products of 847818-74-0) was used in this study.
1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Related Products of 847818-74-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics