Call for Papers  

Article Details

Review Article

Development and Application of Activity-based Fluorescent Probes for High-Throughput Screening

[ Vol. 29 , Issue. 10 ]


Juan Cheng and Xin Li*   Pages 1739 - 1756 ( 18 )


High-throughput screening facilitates the rapid identification of novel hit compounds; however, it remains challenging to design effective high-throughput assays, partially due to the difficulty of achieving sensitivity in the assay techniques. Among the various analytical methods that are used, fluorescence-based assays dominate due to their high sensitivity and ease of operation. Recent advances in activity-based sensing/imaging have further expanded the availability of fluorescent probes as monitors for high-throughput screening of result outputs. In this study, we have reviewed various activity-based fluorescent probes used in high-throughput screening assays, with an emphasis on their structure-related working mechanisms. Moreover, we have explored the possibility of developing additional and better probes to boost hit identification and drug development against various targets.


High-throughput screening, fluorescent probe, drug target, hit identification, enzyme, receptor, metabolite.


College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, Zhejiang, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, Zhejiang

Read Full-Text article