In 2018,Vasta, James D.; Corona, Cesear R.; Wilkinson, Jennifer; Zimprich, Chad A.; Hartnett, James R.; Ingold, Morgan R.; Zimmerman, Kristopher; Machleidt, Thomas; Kirkland, Thomas A.; Huwiler, Kristin G.; Ohana, Rachel Friedman; Slater, Michael; Otto, Paul; Cong, Mei; Wells, Carrow I.; Berger, Benedict-Tilman; Hanke, Thomas; Glas, Carina; Ding, Ke; Drewry, David H.; Huber, Kilian V. M.; Willson, Timothy M.; Knapp, Stefan; Muller, Susanne; Meisenheimer, Poncho L.; Fan, Frank; Wood, Keith V.; Robers, Matthew B. published 《Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement》.Cell Chemical Biology published the findings.Name: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate The information in the text is summarized as follows:
For kinase inhibitors, intracellular target selectivity is fundamental to pharmacol. mechanism. Although a number of acellular techniques have been developed to measure kinase binding or enzymic inhibition, such approaches can fail to accurately predict engagement in cells. Here we report the application of an energy transfer technique that enabled the first broad-spectrum, equilibrium-based approach to quant. profile target occupancy and compound affinity in live cells. Using this method, we performed a selectivity profiling for clin. relevant kinase inhibitors against 178 full-length kinases, and a mechanistic interrogation of the potency offsets observed between cellular and biochem. anal. For the multikinase inhibitor crizotinib, our approach accurately predicted cellular potency and revealed improved target selectivity compared with biochem. measurements. Due to cellular ATP, a number of putative crizotinib targets are unexpectedly disengaged in live cells at a clin. relevant drug dose. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Name: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate)
tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers. Ethers lack the hydroxyl groups of alcohols. Name: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate Without the strongly polarized O―H bond, ether molecules cannot engage in hydrogen bonding with each other.
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem