Enamine, a premier supplier of Building Blocks, Fragments and Screening Compounds, and Astex Pharmaceuticals (UK), a prominent biotech company focused on discovery and development of innovative medicines targeting cancer and CNS disorders, have cooperated to provide wide access to Astex’ MiniFrag library, an efficient Fragment-based Drug Discovery tool for identification of hot and warm spots of protein targets.
The concept recently proposed by Astex (O’Reilly, Drug Discovery Today, 2019), implies high concentration crystallographic screening of a balanced set comprising 80 chemically diverse, highly soluble, ultra-low- molecular-weight fragments, that provides comprehensive insight into the nature of protein binding sites and mode of determinative ligand-target interactions, allowing to guide fragment evolution strategy and significantly facilitating structure optimization of fragment-derived lead candidates.
Enamine, which has the most extensive fragment stock database, was approved by Astex to be the exclusive supplier offering the MiniFrag Library on a commercial basis. The Library is readily available from Enamine in any suitable format, including dry samples or assay-ready high concentration (1M, 100mM) aqueous soaks in containers of preferred type. The detected MiniFrag hits can be followed-up with a wide range of stock available and synthetically feasible derivatives as well as with building blocks for introduction of the relevant structural features for lead optimization.
Enamine Europe Sales Director Andrey Tarnovskiy commented: “Astex has pioneered Fragment-based Drug Discovery and continues to excel in the development of new techniques accelerating research work in the field. We at Enamine are proud to have been given approval by Astex to leverage this advance in Fragment screening and to make the advantages and usability of the MiniFrag library easily accessible by the medchem community across the globe in a time- and cost-efficient manner.”
Enamine Head Strategic Alliances Michael Bossert added: “We have a long-lasting relationship with Astex and we are excited to render this highly sophisticated discovery tool available, not only to contribute to the growth of our products pipeline but to provide it to our clients who otherwise might never have gotten a chance to access it.”