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Updated: May 20, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
Published on: May 16, 2021
Drug efficiency: a new concept to guide lead optimization programs towards the selection of better clinical
Simone Braggio1, Dino Montanari, Tino Rossi
1Discovery DMPK, Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline R&D, Via A. Fleming 4, Verona 37135, Italy +39 045 821 8663; +39 340 3731587 ; +39 045 921 8153 ; simone.m.braggio@gsk.com.
Abstract:
As a result of their wide acceptance and conceptual simplicity, drug-like concepts are having a major influence on the drug discovery process, particularly in the selection of the 'optimal' absorption, distribution, metabolism, excretion and toxicity and physicochemical parameters space. While they have an undisputable value when assessing the potential of lead series or in evaluating inherent risk of a portfolio of drug candidates, they result much less useful in weighing up compounds for the selection of the best potential clinical candidate. We introduce the concept of drug efficiency as a new tool both to guide the drug discovery program teams during the lead optimization phase and to better assess the developability potential of a drug candidate.
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