ArticleACS combinatorial science2015
Rapid lead discovery through iterative screening of one bead one compound libraries.
Article in ACS combinatorial science, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed.
- Navigating the Expansive Landscapes of Soft Materials: A User Guide for High-Throughput Workflows.ACS polymers Au · 2023Review
- Mega-High-Throughput Screening Platform for the Discovery of Biologically Relevant Sequence-Defined Non-Natural Polymers.ACS central science · 2022Article
- Massively Parallel Optimization of the Linker Domain in Small Molecule Dimers Targeting a Toxic r(CUG) Repeat Expansion.ACS medicinal chemistry letters · 2021Article
- Identification of a covalent binder to the oncoprotein gankyrin using a NIR-Based OBOC screening method.RSC advances · 2021Article
- Beyond protein binding: recent advances in screening DNA-encoded libraries.Chemical communications (Cambridge, England) · 2019Review
- Developments with bead-based screening for novel drug discovery.Expert opinion on drug discovery · 2019Article
- Review
- Facile Synthesis of a Next Generation Safety-Catch Acid-Labile Linker, SCAL-2, Suitable for Solid-Phase Synthesis, On-Support Display and for Post-Synthesis Tagging.ChemistrySelect · 2017Article
- Discovery of Peptidomimetic Ligands of EED as Allosteric Inhibitors of PRC2.ACS combinatorial science · 2017Article
- Chromodomain Ligand Optimization via Target-Class Directed Combinatorial Repurposing.ACS chemical biology · 2016Article
- Development of a large peptoid-DOTA combinatorial library.Biopolymers · 2016Article
- Identification of selective covalent inhibitors of platelet activating factor acetylhydrolase 1B2 from the screening of an oxadiazolone-capped peptoid-azapeptoid hybrid library.Bioorganic & medicinal chemistry · 2016Article
- Design of a Microfluidic Chip for Magnetic-Activated Sorting of One-Bead-One-Compound Libraries.ACS combinatorial science · 2016Article
- Rapid Discovery of Functional Small Molecule Ligands against Proteomic Targets through Library-Against-Library Screening.ACS combinatorial science · 2016Article
- Discovery of Phosphorylated Peripherin as a Major Humoral Autoantigen in Type 1 Diabetes Mellitus.Cell chemical biology · 2016Article
- Towards vast libraries of scaffold-diverse, conformationally constrained oligomers.Chemical communications (Cambridge, England) · 2016Article
- Targeting Stereotyped B Cell Receptors from Chronic Lymphocytic Leukemia Patients with Synthetic Antigen Surrogates.The Journal of biological chemistry · 2016Article
- Conformational Restriction of Peptides Using Dithiol Bis-Alkylation.Methods in enzymology · 2016Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
Primary hits that arise from screening one bead one compound (OBOC) libraries against a target of interest rarely have high potency. However, there has been little work focused on the development of an efficient workflow for primary hit improvement. In this study, we show that by characterizing the binding constants for all of the hits that arise from a screen, structure-activity relationship (SAR) data can be obtained to inform the design of "derivative libraries" of a primary hit that can then be screened under more demanding conditions to obtain improved compounds. Here, we demonstrate the rapid improvement of a primary hit against matrix metalloproteinase-14 using this approach.
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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.