{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["16(3)"],"submitter":["Stevens R"],"funding":["Royal Commission for the Exhibition of 1851","GlaxoSmithKline","Society of Chemical Industry","University of Strathclyde"],"pubmed_abstract":["High-throughput chemistry (HTC) and direct-to-biology (D2B) platforms allow for plate-based compound synthesis and biological evaluation of crude mixtures in cellular assays. The rise of these workflows has rapidly accelerated drug-discovery programs in the field of targeted protein degradation (TPD) in recent years by removing a key bottleneck of compound purification. However, the number of chemical transformations amenable to this methodology remain minimal, leading to limitations in the exploration of chemical space using existing library-based approaches. In this work, we expanded the toolbox by synthesising a library of degraders in D2B format. First, reaction conditions are established for performing key medicinal chemistry transformations, including reductive amination, S<sub>N</su"],"journal":["RSC medicinal chemistry"],"pagination":["1141-1150"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11664481"],"repository":["biostudies-literature"],"pubmed_title":["Expanding the reaction toolbox for nanoscale direct-to-biology PROTAC synthesis and biological evaluation."],"pmcid":["PMC11664481"],"pubmed_authors":["Cryan J","Klimaszewska D","Stevens R","Miah AH","Shrives HJ","Stacey P","Harling JD","Battersby DJ","Burley GA"],"additional_accession":[]},"is_claimable":false,"name":"Expanding the reaction toolbox for nanoscale direct-to-biology PROTAC synthesis and biological evaluation.","description":"High-throughput chemistry (HTC) and direct-to-biology (D2B) platforms allow for plate-based compound synthesis and biological evaluation of crude mixtures in cellular assays. The rise of these workflows has rapidly accelerated drug-discovery programs in the field of targeted protein degradation (TPD) in recent years by removing a key bottleneck of compound purification. However, the number of chemical transformations amenable to this methodology remain minimal, leading to limitations in the exploration of chemical space using existing library-based approaches. In this work, we expanded the toolbox by synthesising a library of degraders in D2B format. First, reaction conditions are established for performing key medicinal chemistry transformations, including reductive amination, S<sub>N</su","dates":{"release":"2025-01-01T00:00:00Z","publication":"2025 Mar","modification":"2026-06-08T05:13:18.712Z","creation":"2025-04-04T02:54:31.362Z"},"accession":"S-EPMC11664481","cross_references":{"pubmed":["39720740"],"doi":["10.1039/d4md00760c"]}}