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Updated: Jul 15, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
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Discrete On-DNA Screening: A Frontier for Rapid Hit-to-Lead Optimization Applied to p38α.

Hangke Ma1, Peng Chen2, Siyue Chen1

  • 1Pharmaron (Ningbo) Technology Development Co., Ltd., No. 800 Bin-Hai Fourth Road, Qianwan New Area, Ningbo 315336, China.

ACS Medicinal Chemistry Letters
|July 14, 2026
PubMed
Summary

A new on-DNA screening method allows functional evaluation of DNA-linked molecules, overcoming limitations of traditional high-throughput screening (HTS) and DNA-encoded library (DEL) selection for drug discovery.

Keywords:
Hit-to-leadKinase inhibitorOn-DNA screeningStructure−activity relationship (SAR)p38α MAP kinase

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Area of Science:

  • Medicinal Chemistry
  • Drug Discovery Technologies
  • Biotechnology

Background:

  • High-throughput screening (HTS) and DNA-encoded library (DEL) selection are vital in drug discovery.
  • These methods have limitations, including high infrastructure needs and affinity-only selection constraints.

Purpose of the Study:

  • To develop a robust on-DNA compound screening method.
  • To enable direct functional evaluation of DNA-linked small molecules, bypassing traditional limitations.

Main Methods:

  • A novel on-DNA screening platform was developed.
  • A focused library of trisubstituted benzamides was synthesized and screened on-DNA against p38α MAPK.

Main Results:

  • The platform successfully prioritized advanced structures.
  • Compound I-13 was identified as a potent p38α inhibitor (IC50 = 65 nM) with significant isoform selectivity.
  • I-13 demonstrated 4-fold selectivity over p38β and >461 fold over p38γ and p38δ.

Conclusions:

  • The developed on-DNA screening platform offers a powerful, low-barrier alternative to HTS and DEL.
  • This method facilitates rapid, functional hit-to-lead discovery.
  • Further optimization for p38α/β isoform selectivity is a future direction.