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Updated: Dec 28, 2025

Assays for Validating Histone Acetyltransferase Inhibitors

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

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

Xiangyan Yi¹, Lian Xue^1,2, Tim Thomas³

¹School of Pharmaceutical Sciences, Nanjing Tech University, Number 30 South Puzhu Road, Nanjing, 211816, PR China.

Future Medicinal Chemistry

|February 18, 2020

Summary

This summary is machine-generated.

We introduce an Action Plan for Hit Identification (APHID) to streamline hit triage in drug discovery. This method prioritizes tractable hits from high-throughput screening (HTS) campaigns, exemplified by targeting the KAT6A enzyme.

Keywords:

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

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Last Updated: Dec 28, 2025

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Area of Science:

Drug Discovery and Development
Biochemistry and Enzymology
Chemical Biology

Background:

High-throughput screening (HTS) generates numerous hits, necessitating efficient methods for prioritizing promising compounds.
Hit triage is a critical step in HTS, determining which hits warrant further investigation.
The enzyme KAT6A is a potential therapeutic target, requiring effective hit identification strategies.

Purpose of the Study:

To present a structured Action Plan for Hit Identification (APHID) to guide hit triage.
To demonstrate the utility of APHID using a real-world HTS campaign.
To provide a digestible resource for researchers new to HTS and hit triage.

Main Methods:

Development of the APHID framework for hit triage.
Application of APHID to an HTS campaign targeting the KAT6A enzyme.
Evaluation of hit tractability for elimination or retention.

Main Results:

Successful identification of a tractable hit against KAT6A using the APHID process.
Demonstration of APHID's effectiveness in eliminating less tractable hits.
Validation of APHID as a practical guide for hit triage.

Conclusions:

APHID provides a robust and efficient strategy for hit triage in HTS.
The APHID framework facilitates the selection of promising drug candidates.
This approach is particularly valuable for researchers entering the field of HTS.