ArticleSLAS discovery : advancing life sciences R & D2019
Development of a Selection Method for Discovering Irreversible (Covalent) Binders from a DNA-Encoded Library.
Article in SLAS discovery : advancing life sciences R & D, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 35 citations in OpenAlex.
- Discovery of Small-Molecule Ligands for the E3 Ligase STUB1/CHIP from a DNA-Encoded Library Screen.ACS medicinal chemistry letters · 2025Article
- Identification of Structurally Novel KRASJournal of medicinal chemistry · 2025Article
- Development of small molecule non-covalent coronavirus 3CL protease inhibitors from DNA-encoded chemical library screening.Nature communications · 2025Article
- DNA encoded peptide library for SARS-CoV-2 3CL protease covalent inhibitor discovery and profiling.RSC chemical biology · 2024Article
- Identification and Evaluation of Reversible Covalent Binders to Cys55 of Bfl-1 from a DNA-Encoded Chemical Library Screen.ACS medicinal chemistry letters · 2024Article
- Advances in covalent drug discovery.Nature reviews. Drug discovery · 2022Review
- Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins.ACS medicinal chemistry letters · 2022Article
- Strategies for developing DNA-encoded libraries beyond binding assays.Nature chemistry · 2022Review
- Structural characterization of a peptoid-inspired conformationally constrained oligomer (PICCO) bound to streptavidin.Chemical communications (Cambridge, England) · 2020Article
- Encoded Library Technologies as Integrated Lead Finding Platforms for Drug Discovery.Molecules (Basel, Switzerland) · 2019Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
DNA-encoded libraries (DELs) have been broadly applied to identify chemical probes for target validation and lead discovery. To date, the main application of the DEL platform has been the identification of reversible ligands using multiple rounds of affinity selection. Irreversible (covalent) inhibition offers a unique mechanism of action for drug discovery research. In this study, we report a developing method of identifying irreversible (covalent) ligands from DELs. The new method was validated by using 3C protease (3CP) and on-DNA irreversible tool compounds (rupintrivir derivatives) spiked into a library at the same concentration as individual members of that library. After affinity selections against 3CP, the irreversible tool compounds were specifically enriched compared with the library members. In addition, we compared two immobilization methods and concluded that microscale columns packed with the appropriate affinity resin gave higher tool compound recovery than magnetic beads.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.