关键词: APHID HTS KAT KAT6A PAINS counter screen histone acetyltransferase inhibitor hit triage lysine acetyltransferase inhibitor

Mesh : Enzyme Inhibitors / chemistry pharmacology High-Throughput Screening Assays Histone Acetyltransferases / antagonists & inhibitors metabolism Humans Molecular Structure

来  源:   DOI:10.4155/fmc-2019-0212   PDF(Sci-hub)

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.
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