Thermo Fisher Scientific has introduced a tool to accelerate hit-to-lead programmes in the drug discovery process.
Maybridge Quick2Lead compound kits are designed to save time and money by allowing rapid compound library synthesis around bioactive 'hits' emerging from screening assays.
The kits are made up of pre-weighed, diverse building block selections, easing rapid capture of structure-activity (SAR) data from the closely related structural analogues within the library.
Quick2Lead compound kits are available as five functionality-based kits, each one containing 48 selected compounds.
This allows the exploration of a wide area of chemical space, to maximise credible SAR data acquisition for the conversion of an initial hit into an optimisable lead.
Since these compounds are all pre-weighed, the kits are ready to use by simply adding solvent and transferring straight to a synthesiser.
The five functional groups available include carboxylic acids, sulphonyl chlorides, amines, anilines and boronic acids.
Each of these functional groups is applicable to a wide range of parallel synthesis methodologies.
Although each kit taps into the diverse Maybridge collection, they all include compounds from the top levels of the relevant Topliss tree, ensuring quality and rigour in interaction testing.
Each preselected compound is supplied as 0.1mMol in a 5ml vial.
This saves time and money at several levels - minimising stock, avoiding disposal and reducing storage footprint.
The preselection process also avoids the 'dead time' that can be experienced while waiting for multiple building blocks from internal and external sources.
Maybridge Quick2Lead kits arrive as a complete library, delivered rapidly ex-stock.