MedChemComm · 2011 · 354 citations · 15 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryLead OptimizationHit-to-lead OptimizationHit-to-lead ProgressionLead Compound DesignLead DiscoveryPotency OptimizationSelectivity OptimizationLead Compound DiscoveryLead Compound OptimizationLead Compound PrioritizationLead Compound ScreeningMechanism-based Lead OptimizationMolecular Property OptimizationPhenotypic Hit-to-lead OptimizationStructure-guided Lead Discovery
Molecular Obesity is the tendency for lead optimisation to yield candidate molecules that are unfit for their continued survival towards becoming a drug. Reasons for this and other issues are discussed.
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