ChemInform · 2000 · 34 citations · 16 references
PharmacyMedicinal ChemistryPharmacologyCombinatorial ChemistryDrug DiscoveryLead OptimizationChemical Library DesignHit-to-lead OptimizationLead Compound DesignLead DiscoveryLigand BindingPotency OptimizationCell-based AssaysCell-based Pharmacological AssaysCell-based Screening AssaysIntracellular Signaling PathwaysLead Compound DiscoveryLead Compound OptimizationLead Compound ScreeningSubcellular Protein Localization
Both solid- and liquid-phase combinatorial chemistry have emerged as powerful tools for identifying pharmacologically active compounds and optimizing the biological activity of a lead compound. Complementary high-throughput in vitro assays are essential for compound evaluation. Cell-based assays that use optical endpoints permit investigation of a wide variety of functional properties of these compounds including specific intracellular biochemical pathways, protein-protein interactions, and the subcellular localization of targets. Integration of combinatorial chemistry with contemporary pharmacology now represents an important factor in drug discovery and development.
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Genomic sciences and the medicine of tomorrow
Jürgen Drews · Nature Biotechnology · 1996 · 245 citations