Gesmundo, Nathan J. published the artcileNanoscale synthesis and affinity ranking, Product Details of C8H8N2O, the main research area is structure drug discovery.
Most drugs are developed through iterative rounds of chem. synthesis and biochem. testing to optimize the affinity of a particular compound for a protein target of therapeutic interest. This process is challenging because candidate mols. must be selected from a chem. space of more than 1060 drug-like possibilities1, and a single reaction used to synthesize each mol. has more than 107 plausible permutations of catalysts, ligands, additives and other parameters2. The merger of a method for high-throughput chem. synthesis with a biochem. assay would facilitate the exploration of this enormous search space and streamline the hunt for new drugs and chem. probes. Miniaturized high-throughput chem. synthesis3-7 has enabled rapid evaluation of reaction space, but so far the merger of such syntheses with bioassays has been achieved with only low-d. reaction arrays, which analyze only a handful of analogs prepared under a single reaction condition8-13. High-d. chem. synthesis approaches that have been coupled to bioassays, including on-bead14, on-surface15, on-DNA16 and mass-encoding technologies17, greatly reduce material requirements, but they require the covalent linkage of substrates to a potentially reactive support, must be performed under high dilution and must operate in a mixture format. These reaction attributes limit the application of transition-metal catalysts, which are easily poisoned by the many functional groups present in a complex mixture, and of transformations for which the kinetics require a high concentration of reactant. Here the authors couple high-throughput nanomole-scale synthesis with a label-free affinity-selection mass spectrometry bioassay. Each reaction is performed at a 0.1-M concentration in a discrete well to enable transition-metal catalysis while consuming less than 0.05 mg of substrate per reaction. The affinity-selection mass spectrometry bioassay is then used to rank the affinity of the reaction products to target proteins, removing the need for time-intensive reaction purification This method enables the primary synthesis and testing steps that are critical to the invention of protein inhibitors to be performed rapidly and with minimal consumption of starting materials.
Nature (London, United Kingdom) published new progress about Chemical library. 82090-52-6 belongs to class imidazoles-derivatives, name is Imidazo[1,2-a]pyridin-2-ylmethanol, and the molecular formula is C8H8N2O, Product Details of C8H8N2O.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem