Practical Approaches to Efficient Screening: Information-Rich Screening Protocol

The past approach of high-throughput screening of everything in the corporate collection has been shown to be very expensive in terms of reagents cost, disposal cost, and compound collection depletion. It is well known that screening campaigns produce several hits, ofwhich only 50% confirmon average. More efficientways of screening can provide an informative structure-activity relationship (SAR), which in turn can be used to buildmathematical models for further probing the activity space and directing chemical synthesis. The authors report new methods and insights to extract themaximum possible information from a screening experiment and findmost of the possible hits in the corporate collection while screening as few compounds as possible.