Action plan for hit identification (APHID): KAT6A as a case study

Xiangyan Yi, Lian Xue, Tim Thomas, Jonathan B. Baell

Research output: Contribution to journalArticleResearchpeer-review

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 languageEnglish
Pages (from-to)423-437
Number of pages15
JournalFuture Medicinal Chemistry
Volume12
Issue number5
DOIs
Publication statusPublished - 1 Mar 2020

Keywords

  • APHID
  • counter screen
  • histone acetyltransferase inhibitor
  • hit triage
  • HTS
  • KAT
  • KAT6A
  • lysine acetyltransferase inhibitor
  • PAINS

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