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Updated: Apr 15, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
Published on: May 16, 2021
Lead optimization attrition analysis (LOAA): a novel and general methodology for medicinal chemistry
Mark Munson1, Harvey Lieberman1, Elina Tserlin2
1Lead Generation Candidate Realization, Sanofi, 153 Second Avenue, Waltham, MA 02451, USA.
Abstract:
Herein, we report a novel and general method, lead optimization attrition analysis (LOAA), to benchmark two distinct small-molecule lead series using a relatively unbiased, simple technique and commercially available software. We illustrate this approach with data collected during lead optimization of two independent oncology programs as a case study. Easily generated graphics and attrition curves enabled us to calibrate progress and support go/no go decisions on each program. We believe that this data-driven technique could be used broadly by medicinal chemists and management to guide strategic decisions during drug discovery.
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