Secondary Recovery Significantly Improves Screening Quality of Fragment Libraries

At the opening bell of the Society for Biomecular Sciences (SBS) 16th Annual Conference & Exhibition in Phoenix, Microsonic Systems Inc. (“Microsonics”) announced that its HENDRIX SM100 Ultrasonic Fluid Processor (“HENDRIX SM100”) significantly improves fragment-based drug screening quality by re-solubilizing precipitated samples back into solution.

Recent data shows that by adding the HENDRIX SM100 to the fragment-based drug discovery process, researchers are able to re-solubilize precipitated fragment libraries and consequently “recover” the originally “lost” samples. This process both increases the sample concentrations and improves the accuracy of screening results.

“Using Lateral Ultrasonic Thrust™ technology to solubilize, thaw, mix and suspend is proving to be a highly effective tool to increase screening yields,” stated Bruce Jamieson, Senior Vice President of Sales & Marketing. “In fact, our customers have told us that by virtually eliminating precipitates from their compound libraries, the HENDRIX SM100 is allowing them to screen a significantly higher proportion of their compounds than they would have been able to otherwise, a process we are calling ‘secondary recovery.’”

Microsonics will be presenting a poster at the SBS conference titled “Improve the Integrity of Your Fragment Library for Fragment-Based Drug Discovery”. The poster reports experimental data that shows that, compared to the control group, the secondary recovery process increases primary screening activity by up to 384%, and by as much as two logs of concentration reduction in fragment IC50 values.

Fragment-based drug discovery (FBDD) is gaining recognition for its many advantages over high-throughput screening, including better hit-to-lead rates and broad chemical space for possible compound scaffolds. Due to the low affinity of fragments for biological targets, fragment libraries may contain weak hits, requiring screening concentrations as high as 200mM. Although many fragments are soluble in DMSO, environmental shocks introduced by DMSO hydration or repeat freeze/thaw cycles can cause precipitation, and consequently affect the accuracy of FBDD screening results. Using the HENDRIX SM100, precipitates can now be recovered across an entire microplate or tube rack simultaneously in just a few minutes.