ArticleACS medicinal chemistry letters2021
Trends in Hit-to-Lead Optimization Following DNA-Encoded Library Screens.
Article in ACS medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 46 citations in OpenAlex.
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- Toward target 2035: EUbOPEN - a public-private partnership to enable & unlock biology in the open.RSC medicinal chemistry · 2025Article
- The long road of drug development for endometriosis - Pains, gains, and hopes.Journal of controlled release : official journal of the Controlled Release Society · 2024Review
- Unnatural Amino Acids: Strategies, Designs, and Applications in Medicinal Chemistry and Drug Discovery.Journal of medicinal chemistry · 2024Review
- Building Block-Centric Approach to DNA-Encoded Library Design.Journal of chemical information and modeling · 2024Article
- Chemical Space Profiling of SARS-CoV-2 PLACS medicinal chemistry letters · 2024Article
- Article
- Development of the Inverse Sonogashira Reaction for DEL Synthesis.ACS medicinal chemistry letters · 2023Article
- Combining pharmacophore models derived from DNA-encoded chemical libraries with structure-based exploration to predict Tankyrase 1 inhibitors.European journal of medicinal chemistry · 2023Article
- Navigating chemical reaction space - application to DNA-encoded chemistry.Chemical science · 2022Article
- Chemical Evolution of Natural Product Structure.Journal of the American Chemical Society · 2022Article
- Strategies for developing DNA-encoded libraries beyond binding assays.Nature chemistry · 2022Review
- Power in Numbers: Harnessing Combinatorial and Integrated Screens to Advance Nanomedicine.JACS Au · 2022Review
- DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry.ACS medicinal chemistry letters · 2021Article
- Target-Based Evaluation of "Drug-Like" Properties and Ligand Efficiencies.Journal of medicinal chemistry · 2021Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
DNA-encoded library (DEL) screens have emerged as a powerful hit-finding tool for a number of biological targets. In this Innovations article, we review published hit-to-lead optimization studies following DEL screens. Trends in molecular property changes from hit to lead are identified, and specific optimization tactics are exemplified in case studies. Across the studies, physicochemical property and structural changes post-DEL screening are similar to those which occur during hit-to-lead optimization following high throughputscreens (HTS). However, unique aspects of DEL-the combinatorial synthetic methods which enable DEL synthesis and the linker effects at the DNA attachment point-impact the strategies and outcomes of hit-to-lead optimizations.
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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.