Action plan for hit identification (APHID): KAT6A as a case study
Xiangyan Yi, Lian Xue, Tim Thomas, Jonathan B Baell
Future Medicinal Chemistry | FUTURE SCI LTD | Published : 2020
Here, we describe our action plan for hit identification (APHID) that guides the process of hit triage, with elimination of less tractable hits and retention of more tractable hits. We exemplify the process with reference to our high-throughput screening (HTS) campaign against the enzyme, KAT6A, that resulted in successful identification of a tractable hit. We hope that APHID could serve as a useful, concise and digestible guide for those involved in HTS and hit triage, especially those that are relatively new to this exciting and continually evolving technology.
Awarded by National Health and Medical Research Council of Australia (NHMRC)
The National Health and Medical Research Council of Australia (NHMRC) is thanked for the research support (grant numbers 1030704 and 1080146) and fellowship support for JB Baell (2012-2016 senior research fellowship number 1020411, 2017 principal research fellowship number 1117602). Acknowledged is the Australian Federal Government Education Investment Fund Super Science Initiative and the Victorian State Government, Victoria Science Agenda Investment Fund for infrastructure support and the facilities and the scientific and technical assistance of the Australian Translational Medicinal Chemistry Facility (ATMCF), Monash Institute of Pharmaceutical Sciences (MIPS). ATMCF is supported by Therapeutic Innovation Australia (TIA). TIA is supported by the Australian Government through the National Collaborative Research Infrastructure Strategy (NCRIS) program. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.