DNA-encoded chemistry: enabling the deeper sampling of chemical space

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ChEMBL: a large-scale bioactivity database for drug discovery

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Accurate whole human genome sequencing using reversible terminator chemistry

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How to improve R&D productivity: the pharmaceutical industry's grand challenge

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Rapid generation of functional human IgG antibodies derived from Fab-on-phage display libraries

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Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?

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Recent advances in field effect transistor biosensors for drug screening applications

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On-DNA Binder Confirmation: Increasing Confidence in DEL Hits

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Discovery of a novel small molecule degrader of wild type and mutant estrogen receptors using DNA encoded libraries

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Discovery of a CHI3L1-targeted small molecule modulating neuroinflammation in Alzheimer's disease via DNA-encoded library (DEL) screening

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Enhanced screening via a pure DNA-encoded peptide library enabled by an Fmoc modification

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Unlocking chemical diversity in aptamers with DNA orthogonal barcodes

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Discrete On-DNA Screening: A Frontier for Rapid Hit-to-Lead Optimization Applied to p38α

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From DNA-encoded library (DEL) screening to in vivo validation: LILRB4 (ILT3)-targeted small molecules reprograms myeloid immune suppression

Abdel‐Rahman, S. A., & Gabr, M. T. (2026) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2026.119740 · Cited by 2

Encoding Thiol Metabolite Information into a DNA Sequence by Disulfide Exchange Reaction on Oligodeoxynucleotides for Parallel Analysis of the Metabolite and mRNA

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DNA Encoding Strategy for the Identification and Quantification of Poorly Reactive Target Metabolite Using Phenylboronic Acid-tethered Oligodeoxynucleotides

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A detection system using sensing motif-tethered oligodeoxynucleotides for multiplex biomolecular analysis

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Rational Design Strategies in DNA‐Encoded Libraries for Drug Discovery

Wang, X., Li, L., Shen, X., & Lu, X. (2025) · Angewandte Chemie · doi:10.1002/ange.202511839 · Cited by 2

Surf–DNA-Enabled DNA-Encoded Library-Compatible Amino Radical Transfer C(sp2)–C(sp3) Coupling

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RNA Acylation Method via a DNA-Templated Acyl Transfer Reaction

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Barcoding mit Nukleinsäuren: Anwendung der DNA‐Sequenzierung als molekulares Zählwerk

Liszczak, G., & Muir, T. W. (2018) · Angewandte Chemie · doi:10.1002/ange.201808956 · Cited by 2

Integrated Bacterial Production and Functional Screening of Expanded Cyclic Peptide Libraries for Identifying Chemical Rescuers of Pathogenic Protein Misfolding and Aggregation

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mRNA Display and Its Growing Potential in the Discovery ofDe NovoTherapeutic Peptide Candidates

Helmling, C., & Cunningham, C. N. (2022) · ACS symposium series · doi:10.1021/bk-2022-1417.ch002 · Cited by 2

Initiating DNA-Encoded Library Synthesis with a Hexathymidine DNA Oligonucleotide

Škopić, M. K., Smith, D. D. S., Gohla, A., Kunig, V. B. K., & Brunschweiger, A. (2022) · Methods in molecular biology · doi:10.1007/978-1-0716-2545-3_14 · Cited by 2

Cheminformatics Approaches Aiding the Design and Selection of DNA-Encoded Libraries

Zhu, H., Montgomery, J. I., & Stanton, R. V. (2022) · Topics in medicinal chemistry · doi:10.1007/7355_2022_148 · Cited by 2

Drug Discovery with DNA‐Encoded Library Technology

Ding, Y., & Scott, S. (2022) · doi:10.1002/9781119627784.ch8 · Cited by 2

Discovering Cell-targeting Ligands and the Cell Surface Receptors via Selection of DNA-encoded Chemical Libraries (DELs) against Cancer Cells without Predefined TargetsPreprint

Gui, Y., Hou, R., Huang, Y., Zhou, Y., Liu, S., Meng, L., Li, Y., Lam, F. S., Wong, C. S., Yin, C. T., et al. (2024) · ChemRxiv · doi:10.26434/chemrxiv-2024-3mrz3 · Cited by 1

High-Throughput Synthesis and Screening of a Cyanimide Library Identifies Selective Inhibitors of ISG15-specific Protease USP18Preprint

Kooij, R., Pol, V., Gan, J., van Doodewaerd, B. R., Sapmaz, A., Fritz, G., Knobeloch, K., & Geurink, P. P. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.04.18.649523 · Cited by 2

Permutational Encoding Strategy Accelerates HIT Validation from Single-Stranded DNA-Encoded Libraries

Puglioli, S., Fabbri, M., Comacchio, C., Alvigini, L., Luca, R. D., Oehler, S., Gilardoni, E., Bassi, G., Cazzamalli, S., Neri, D., et al. (2024) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.4c00233 · Cited by 1

DNA-Encoded Peptide Library Synthesis and Applications, a Mini-Review

Matysiak, S., & Hellmuth, K. (2025) · Methods in molecular biology · doi:10.1007/978-1-0716-4578-9_2 · Cited by 1

Solid‐Phase Synthesis of 1,3,5,6‐Tetra‐Substituted 3,5‐Dihydroimidazo[4,5‐c][1,2]Thiazin‐4( 1 H)‐One 2,2‐Dioxide Derivatives

Moon, J., Lee, H., Kim, S., & Lee, T. (2025) · Journal of Heterocyclic Chemistry · doi:10.1002/jhet.70045 · Cited by 1

A comprehensive review on the role of acetamido as a linker for the design and discovery of anticancer agents

Shimpi, A. A., & Juvale, K. (2025) · Medical Oncology · doi:10.1007/s12032-025-03043-2 · Cited by 1

Synthesis of DNA-Encoded Bicyclic Peptides via Cysteine-Promoted Cyclization and Amide Condensation Reaction

Gan, Y., Zeng, Y., Guan, H., Li, W., Shaginian, A., Li, J., Gao, S., & Liu, G. (2025) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.5c00455 · Cited by 1

A pre-synthetic conjugation methodology of DNA and RNA: combining on-column conjugation and tandem oligonucleotide synthesis

Saraya, J. S., & O’Flaherty, D. K. (2026) · Organic & Biomolecular Chemistry · doi:10.1039/d5ob01870f · Cited by 4

Discovery and optimization of small molecule inhibitors of the SLIT2/ROBO1 protein-protein interaction using DNA-encoded libraries

García-Vázquez, N., Yuan, S., & Gabr, M. T. (2026) · European Journal of Medicinal Chemistry Reports · doi:10.1016/j.ejmcr.2026.100346 · Cited by 1

Developments in the design and therapeutic applications of GSK3β inhibitors

Daoud, S., & Taha, M. O. (2026) · Future Medicinal Chemistry · doi:10.1080/17568919.2026.2675873 · Cited by 1

Advances in respiratory syncytial virus therapeutics: A comprehensive review of small-molecule inhibitors, monoclonal antibodies, and vaccines

Bai, G., Huang, X., & He, Y. (2026) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2026.119092 · Cited by 1

A tailored CoA ligase–N-acyltransferase cascade for on-DNA amide bond formation gives access to broad substrate scope

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From nature to synthetic analogues: recent advances in the design and synthesis of natural product-based libraries

Cheng‐Sánchez, I., Fuentes-Pino, I., Hllafi, M. E., Moya‐Utrera, F., López‐Romero, J. M., Díaz, A., Sánchez‐Ruiz, A., Kurosu, M., & Sarabia, F. (2026) · Organic Chemistry Frontiers · doi:10.1039/d6qo00727a · Cited by 1

DNA-Compatible α-Aminoamide Synthesis for a DNA-Encoded Library

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DNA-Templated Synthesis Optimization

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Step IIIb: The Drug-Like Chemical Diversity Pool: Diverse and Targeted Compound Collections

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Screening of Big Pharma’s Library against Various in-house Biological Targets

Knez, D., Gobec, S., & Hrast, M. (2022) · Molecules · doi:10.3390/molecules27144484 · Cited by 1

Selection Strategies in DNA-Encoded Libraries

Gui, Y., & Li, X. (2022) · Topics in medicinal chemistry · doi:10.1007/7355_2022_149 · Cited by 1

Design, synthesis and validation of a new Crimped Head-Piece for DNA-Encoded libraries generation

Rama-Garda, R., Martín-Ortega, M. D., Sánchez, A. D. J., Priego, J., de Blas, J., Torrado, A., Domínguez, E., Haro, R., Rivera‐Sagredo, A., Román, J. P., et al. (2024) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2024.117596 · Cited by 1

Lead Generation

Narjes, F., Pairaudeau, G., & Petrović, D. (2023) · Royal Society of Chemistry eBooks · doi:10.1039/9781788018982-00682 · Cited by 1

Translation of Deoxyribonucleic Acid into Synthetic Alpha Helical Peptides for Darwinian Evolution

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Synthesis of thiazolo[4,5- d ]pyrimidine derivatives based on purine via solid-phase synthesis

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Chemical Approaches for Beta-cell Biology

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PhotoAffinity Bits: A Photoaffinity-Based Fragment Screening Platform for Efficient Identification of Protein LigandsPreprint

Grant, E. K., Fallon, D. J., Hann, M. M., Fantom, K. G. M., Quinn, C. J., Zappacosta, F., Annan, R. S., Chung, C., Bamborough, P., Dixon, D. P., et al. (2020) · ChemRxiv · doi:10.26434/chemrxiv.12053445.v1 · Cited by 1

Covalent DNA-Encoded Library Workflow Drives Discovery of SARS-CoV-2 Non-structural Proteins InhibitorsPreprint

Lu, X., Hu, H., Mei, L., Wang, X., Xiong, L., Zhu, Y., Liu, S., Zhao, W., Seydimemet, M., Li, L., et al. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.05.08.593105 · Cited by 1

Leitmolekülsuche mit DNA-codierten Bibliotheken

Rudolph, M. G. (2017) · BIOspektrum · doi:10.1007/s12268-017-0778-4

A carbohydrate-derived trifunctional scaffold for medicinal chemistry library synthesis

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Molecular Approaches to Explore Drug-Target Interactions

Al-Amin, R. A. (2019)

Navigating the Biological‐Material Interface with the Guide of Chemical Biology

Shieh, P. (2020) · ChemBioChem · doi:10.1002/cbic.202000529

DNA-encoded Chemistry and Its Use in Discovering Chemical Probes

Keefe, A. D. (2020) · Royal Society of Chemistry eBooks · doi:10.1039/9781839160745-00014

Induced pluripotent stem cells as tools to investigate the neurobiology of bipolar disorder and advance novel therapeutic discovery

Zhao, W., Garza, J. C., Perlis, R. H., & Haggarty, S. J. (2020) · Elsevier eBooks · doi:10.1016/b978-0-12-819182-8.00014-4 · Cited by 1

Assay Development and High‐Throughput Screening

Carettoni, D., & Bader, B. (2021) · Wiley eBooks · doi:10.1002/0471266949.bmc165.pub2

Virtual Screening for Chemists

Saha, I., & Harran, P. G. (2021) · ACS in focus · doi:10.1021/acsinfocus.7e5001

Compound Screening

Numao, S., Etienne, G., Malojcic, G., Schmidt, E. K., & Dumelin, C. E. (2021) · Elsevier eBooks · doi:10.1016/b978-0-12-820472-6.00078-5

Faculty Opinions recommendation of Ultra-large library docking for discovering new chemotypes.

Meiler, J. (2019) · Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature · doi:10.3410/f.735010483.793558380

Faculty Opinions recommendation of Ultra-large library docking for discovering new chemotypes.

Che, Y. (2019) · Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature · doi:10.3410/f.735010483.793556602

Faculty Opinions recommendation of Ultra-large library docking for discovering new chemotypes.

Lowe, J. A., III (2019) · Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature · doi:10.3410/f.735010483.793556210

Trendbericht Biochemie 2022: Bioaktive Substanzen entdecken: von Display‐Methoden zu selbstkodierten Substanzbibliotheken

Pomplun, S. J. (2022) · Nachrichten aus der Chemie · doi:10.1002/nadc.20224126035

On-DNA Pd and Cu-Promoted C-N Cross-Coupling Reactions

Lu, X., & Wang, X. (2022) · Methods in molecular biology · doi:10.1007/978-1-0716-2545-3_8

Screening and Characterizing of GPCR –Ligand Interactions with Mass Spectrometry‐Based Technologies

Qin, S., Lu, Y., & Shui, W. (2022) · Wiley eBooks · doi:10.1002/9781119564782.ch22

Beyond Inhibition

Kostić, M., & Jones, L. H. (2022) · Wiley eBooks · doi:10.1002/9781119774198.ch15

DNA‐ENCODED CHEMICAL LIBRARIES USED FOR DRUG DISCOVERY

Zhao, G., Yang, S., Li, X., & Li, Y. (2022) · Wiley eBooks · doi:10.1002/9781119692799.ch8

Barcoding Strategies for the Synthesis of Genetically Encoded Chemical Libraries

Lessing, A., Detta, E., Scheuermann, J., & Brunschweiger, A. (2022) · Topics in medicinal chemistry · doi:10.1007/7355_2022_146

Interactions Between Systems, Their Differences and Environments

Jost, J., & Restrepo, G. (2022) · Wissenschaft und Philosophie · doi:10.1007/978-3-031-10094-9_4

Targeted Small Molecule Drug Discovery

DiMartino, J. F. (2022) · Pediatric oncology · doi:10.1007/978-3-031-06357-2_2

2.2 Metal-Promoted DEL-Compatible C—C Bond Forming Reactions

Migliorini, F., Puglioli, S., Neri, D., Cazzamalli, S., & Favalli, N. (2024) · Haug Verlag in Georg Thieme Verlag KG eBooks · doi:10.1055/sos-sd-241-00025

Assay Development and Screening Strategies for Epigenetic Targets

Brown, P. J. (2024) · Royal Society of Chemistry eBooks · doi:10.1039/9781837674916-00017

Emerging Technologies for Epigenetic Drug Discovery

(2024) · Royal Society of Chemistry eBooks · doi:10.1039/9781837674916-part2

Hit discovery from DNA-encoded chemical library

Li, Y., Zhao, G., Huang, J., & Li, Y. (2024) · Elsevier eBooks · doi:10.1016/b978-0-443-23932-8.00003-0

A Systematic Blueprint to Ligand the Proteome

Calabrese, M. F. (2025) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c03091

Discovering Cell‐Targeting Ligands and Cell‐Surface Receptors by Selection of DNA‐Encoded Chemical Libraries against Cancer Cells without Predefined Targets

Gui, Y., Hou, R., Huang, Y., Zhou, Y., Liu, S., Meng, L., Li, Y., Lam, F. S., Ding, R., Cao, Y. W., et al. (2025) · Angewandte Chemie · doi:10.1002/ange.202421172

Application of DELs for E3 Ligase Ligand Discovery and Targeted Protein Degradation

Malone, M. L., Sanchez, N. A., Hu, S. L., & Phelps, C. B. (2025) · Royal Society of Chemistry eBooks · doi:10.1039/9781788016032-00134

Solid-phase DNA-encoded Library Technology

Hu, J., Burdick, J. P., & Paegel, B. M. (2025) · Royal Society of Chemistry eBooks · doi:10.1039/9781788016032-00041

DNA framework array enables ultra-high throughput DNA synthesisPreprint

Li, C., Saimaiti, Y., Li, M., Wang, S., Yin, F., Fang, Z., Jia, S., Wang, F., Ye, D., Wang, L., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.05.30.657018 · Cited by 1

Native Massenspektrometrie erleichtert die Hit‐Validierung in der DNA‐Encoded Library Technologie

Bittner, P., Gloger, A., Keller, M., Oehler, S., Lessing, A., Zhang, Q., Ma, Z., Su, W., Satz, A. L., Kuai, L., et al. (2025) · Angewandte Chemie · doi:10.1002/ange.202504470

In Situ Click Chemistry Screen Facilitated by an On‐Nanoparticle DNA‐Encoded Library Identifies Highly Selective and Potent Peptoid Ligands for a Phosphatase

Kim, M., Kim, J., Wang, H. M., Kim, H., Ahn, D., Lee, J.-S., Son, C. Y., Chung, S. J., Shin, M. H., & Lim, H. (2025) · Angewandte Chemie · doi:10.1002/ange.202511606

The parallel and combinatorial synthesis and screening in drug discovery

Furka, Á. (2025) · Structural Chemistry · doi:10.1007/s11224-025-02595-3

DNA self-assembly encoding in spatial multi-omics imaging

Tang, X., Diao, Q., Zhu, X., & Pan, Q. (2025) · Cell Reports Physical Science · doi:10.1016/j.xcrp.2025.102811

Expansion of DNA-Encoded Library Hits Using Generative Chemistry and Ultra-Large Compound CatalogsPreprint

Novy, B., Lin, S.-H., Shell, D. J., Maxfield, T., Merten, E. M., Zhilinskaya, I., Wellnitz, J., Guduru, S. K. R., Hardy, P. B., Pearce, K. H., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.09.30.679600

High‐Throughput Synthesis and Screening of a Cyanimide Library Identifies Selective Inhibitors of ISG15‐Specific Protease mUSP18

Kooij, R., Pol, V., Gan, J., van Doodewaerd, B. R., Sapmaz, A., Alonso, M. C., Fritz, G., Knobeloch, K., & Geurink, P. P. (2025) · Angewandte Chemie · doi:10.1002/ange.202510941

Targeting the Ubiquitin-Proteasome System in cancer

Spallek, R., McLaughlin, C., & Sapkota, G. P. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-29808-0.00078-9

Unlocking drug discovery potential: Harnessing BELKA for predictive modeling of small molecule binding affinities

Singhal, U., Daga, N., & Srishti (2025) · AIP conference proceedings · doi:10.1063/5.0296331

DNA-Encoded Chemical Library Screening with Target Titration Analysis: DELTA

Faver, J. C., Sundersingh, F. S., Viarengo‐Baker, L. A., Chen, Y.-C., Billings, K., Riley, P., Tsai, C.-H., & Kollmann, C. S. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c02259

Multiplexed Detection of Reactive Biomolecules via Chemoresponsive DNA Accumulation on Fluorescence-Encoded Beads

Nishihara, T., Sugawara, M., Mio, R., Motohashi, Y., & Tanabe, K. (2026) · Chemical & Biomedical Imaging · doi:10.1021/cbmi.5c00226

A Novel Method for Normalizing Data from DNA-Encoded Library SelectionsPreprint

Lengyel‐Zhand, Z., Jiang, Z., Montgomery, J. I., Zhu, H., Riccardi, K. A., Corpina, R. A., Burchett, W., Abdelmessih, M., Stanton, R. V., Craig, T. K., et al. (2026) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.64898/2026.01.20.700605

Integrating Functional Response and Target Binding for Mechanism-Centered Drug Screening by High-Mass MALDI-MS

Tan, C., Gao, Y., Buggert, M., Zhou, Y., & Zenobi, R. (2026) · ACS Central Science · doi:10.1021/acscentsci.5c01944

Microfluidic Agarose µ -Droplets for DNA-Encoded Chemical Library ScreeningPreprint

Kim, Y., Kim, H., Hong, J., Kang, M., 배재영, Ko, S., Kim, M., Koh, B., Kim, H., Shim, S., et al. (2026) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.64898/2026.02.15.706034

Toward the chemoenzymatic synthesis of DNA-encoded libraries

Schaub, D., Lessing, A., von Haugwitz, G., Meyer, F., Scheuermann, J., & Buller, R. (2026) · Zürcher Hochschule für Angewandte Wissenschaften digital collection (Zurich University of Applied Sciences) · doi:10.21256/zhaw-35744

DNA-Encoded Libraries (DELs) for Discovering New Molecular Probes: Application to Live-Cell Bioimaging and Personalized Theranostics

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Targeting kinases with DNA-encoded libraries: current landscape and future directions

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