Abstract
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.
Original language | English |
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Pages (from-to) | 423-437 |
Number of pages | 15 |
Journal | Future Medicinal Chemistry |
Volume | 12 |
Issue number | 5 |
DOIs | |
Publication status | Published - 1 Mar 2020 |
Keywords
- APHID
- counter screen
- histone acetyltransferase inhibitor
- hit triage
- HTS
- KAT
- KAT6A
- lysine acetyltransferase inhibitor
- PAINS
Equipment
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Australian Translational Medicinal Chemistry Facility (ATMCF)
Paul Stupple (Manager)
Faculty of Pharmacy and Pharmaceutical SciencesFacility/equipment: Facility