Is There a Difference between Leads and Drugs? A Historical Perspective

By Tudor I. Oprea, A. Davis, S. Teague, Paul D. Leeson. Journal of chemical information and computer sciences, 2001

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How researchers see this paper

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Impact of high-throughput screening in biomedical research (2011, background): “A strong emphasis on the physicochemical properties of compounds — using concepts such as drug-like properties and lead-like properties”
Molecular docking and ligand specificity in fragment-based inhibitor discovery (2009, background): “It is also an enzyme for which efforts to develop noncovalent inhibitors have been unsuccessful, including our own with compounds in the 'lead-like' or 'drug-like' size range”
The influence of drug-like concepts on decision-making in medicinal chemistry (2007, background): “This allows the processes of chemical optimization, which frequently increase physical propertie”
A decade of fragment-based drug design: strategic advances and lessons learned (2007, background): “The process of lead optimization typically results in an increase in both the size and lipophilicity of the original hi”
Fragment-based lead discovery (2004, background): “And last, starting the chemical optimization stage with a low-molecular-mass fragment is likely to produce leads whose M r is still within the range desired for lead-likenes”