Bioactivity assessment is an integral part of the in-depth characterization and understanding of the bioactive molecules following a high-throughput screening (HTS) campaign. Establishing structure-activity-relationship (SAR) and the mechanism-of-action (MoA) of lead compounds during medicinal chemistry-guided optimization is essential to progress candidate molecules from hit to lead and propel them forward in the drug development pipeline. Our broadly tuned portfolio of industry-grade assay technologies enables concentration-response experiments (dose-response analyses) to determine potency, efficacy, selectivity, and mode-of-action. Additionally, these technologies enable early preclinical assessment of cytotoxicity and undesirable off-target effects.

Assay.Works conducts HTS campaigns using either target-based screening for bioactive compounds or phenotypic high-content screening (HCS) using automated microscopy and imaging analysis. Both approaches deliver new hits and leads, however, they require different follow-up strategies to fully assess the bioactivity of candidate molecules. Quantitative systems biology solutions help refine and further characterize identified hit and lead compounds. Genome-wide siRNA loss-of-function analyses facilitates the deconvolution of complex pathways and the mapping of phenotypic observations to the therapeutic target of hits and leads. Moreover, siRNA screening can assist in discovering synthetic lethality as well as genetic and pharmacological interaction and predicting potential combinatorial therapies.