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Early Drug Discovery 2017-05-16T17:08:39+00:00

Early Drug Discovery Services

Target validation services are offered as a foundation to drug discovery. Custom readout systems can be developed for high throughput screening efforts along with accompanying biomarker assays to support hit validation and hit-to-lead optimization.

Target Validation

Our team is experienced in the validation of prospective targets for drug development. Using methods including shRNA and gene overexpression, cell lines can be developed around the prospective target and used to determine its role is a specific phenotype. Once established, these tools can serve as the basis for matched in vivo models allowing further validation of the target of interest.

Custom Assay Development

Our team is experienced in custom assay development to suit your needs. We will validate each kit/assay developed to ensure the reliability and reproducibility of the method. A validation report will be provided to summarize the procedures, intra- and inter- assay variations, recovery, linearity and limits of detection, and stability of the assay. Custom assays that can be developed include, but are not limited to, readout systems for drug discovery and ELISA-based methods for biomarker detection.

Hit Identification

High-throughput screening services are available. Please contact us for details.

Hit-to-Lead Optimization

Hit Validation

After hits are identified from a high throughput screen, they are validated and evaluated using the following methods:
• Confirmatory testing: compounds that were found active against the selected target in the initial screen are re-tested under the same HTS assay conditions to ensure the observed activity is reproducible.
• Dose-response: the hit compounds are tested over a range of concentrations to determine the effective concentration that results in half maximal binding or activity (for instance, EC50).
• Secondary screening: confirmed hits are tested in functional cellular assays to validate activity, determine specificity, and eliminate false positives.

Focused Library Screening

Once hits are validated, structural analogs are selected around the validated hits (parent compounds) from within large commercially available collections and screened according to primary screening conditions to identify more potent, advanced hits. Additional focused libraries can be generated around advanced hits by medicinal chemistry to improve pharmacological properties and composition of matter (intellectual property).