Three Pillars of Early Drug Discovery Success Part 2: Assayability – The Hidden Determinant of Drug Discovery Success

Drug discovery is an exercise in measurement. Every decision made during target validation, hit identification, and lead optimization depends on data generated by assays. Yet assay quality (beyond Z-factors and assay windows) remains one of the most underappreciated determinants of discovery success. Conversely, assay failure is one of the most underappreciated sources of program attrition.This white paper, the second in a three-part series, examines assayability in depth. What it means, why it matters, what it costs when it fails, and how the field is evolving to treat measurement (assayability) as a strategic asset rather than merely having a supporting role.

Three Pillars of Early Drug Discovery Success: Part 1: Introduction to druggability, ligandability, and assayability

This white paper introduces a framework for evaluating early drug discovery programs through three interconnected pillars: druggability, ligandability, and assayability. It defines druggability as the likelihood that a target can be modulated by a therapeutic molecule, ligandability as the ability to identify compounds that bind to that target, and assayability as the ability to reliably measure the target’s biological activity. The paper argues that while druggability and ligandability are often assessed early, assayability is frequently treated as a downstream consideration, creating avoidable bottlenecks in screening and lead optimization. By evaluating assayability in parallel with the other two pillars, organizations can identify technical risks sooner, accelerate decision-making, and improve the overall efficiency and success rate of discovery programs.

Mass Appeal: Disrupting Drug Discovery Research from Assay Development to Lead Compound using Mass Spectrometry

In this white paper, we explore important aspects to consider when choosing a mass spectrometry (MS) approach for small molecule high-throughput screening applications, with a focus on different strategies for sample preparation to maximize the benefits of MS analysis. We highlight the value of combining polymeric enrichment arrays with matrix assisted laser desorption ionization (MALDI) MS, which offers unique solutions for measuring biochemical activities and binding interactions to accelerate and advance small molecule drug discovery research from assay development to lead compound.