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Lead Optimization

Lead optimization is a complex, non-linear process. During this stage of drug discovery, the chemical structure of a confirmed hit is refined to improve its drug characteristics with the goal of producing a preclinical drug candidate.

Typically, confirmed hits are evaluated in secondary assays, and a set of related compounds, called analogs, are synthesized and screened. The testing of analog series results in quantitative information that correlates changes in chemical structure to biological and pharmacological data to establish structure-activity relationships (SARs).

Today, lead optimization often involves a series of standard assays to evaluate toxicity, including P450 inhibition, cytotoxicity assays, and hERG testing. Toxicity in these relatively simple in vitro assays flags hits or leads that could have potential safety concerns.

Another characteristic that lead optimization often evaluates is formulation. Formulation and delivery are closely linked. For example, a drug intended to be delivered via intramuscular injection might call for a different formulation than would one intended for oral delivery. Formulation problems and solutions feed back into the iterative lead optimization cycle.

Molecular Devices offers a range of products that are particularly well suited for lead optimization studies.


ImageXpress® High-Content Screening Systems

CellKey® Label-Free Cellular Analysis System

PatchXpress® 7000A Automated Parallel Patch Clamp System

SpectraMax® Multi-Mode Microplate Readers 

FLIPR® Tetra High Throughput Cellular Screening System

What's New?
ScanLater Western Blot Detection System

NEW ScanLater Western Blot Detection System - Enables western blot and ELISA detection on your microplate reader. Learn more.

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Throughput: We have the right system for your lab--from single-readout instruments to automated, multi-detection systems.