Lead Discovery
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Powerful lead discovery tools for pharma and biopharma drug characterisation

Lead discovery involves the identification of small molecule and biologic drug leads, for the discovery and development of innovative medicines and treatments. The rapid screening of drug candidates meets the short turn-around times required in the drug discovery arena.

After a drug target has been identified and validated, multiple drug candidates are developed through lead discovery. Active compounds are discovered using different screening techniques, and are selected as leads based on their activity on specific drug targets. Such “hits” are further optimised to elucidate the specific chemical groups responsible for eliciting the desired biological effect.

The screening stage is complex and time consuming, as libraries containing vast numbers of compounds must be sifted through in order to identify hits which act on specific drug targets.  

High throughput screening (HTS) and ultra high throughput screening (UHTS) can be used to identify promising candidates for drug leads, and enable the use of automated workflows for pharma and biopharma drug discovery in R&D laboratories. Unprecedented screening capabilities for HTS biochemical assays are available for lead discovery.

Fragment-based screening (FBS) and mass-based screening are other powerful techniques which enable the rapid screening of samples, to facilitate fast-paced drug discovery.

Mass spectrometry (for HTS/UHTS) accelerates label-free hit finding in drug discovery, by rapidly screening through compound libraries of millions of substances. NMR-based fragment lead discovery identifies lead compounds at a superior hit rate, and allows the acquisition, analysis and reporting of screening data.

During lead evaluation – the next stage in the drug discovery workflow – drug candidates are examined for binding mechanisms, potency, in-vitro toxicity, selectivity and more. New lead-related candidates are then further evaluated during lead optimisation.