Target engagement assays play a pivotal role in drug discovery and development. They enable researchers to understand the interaction between a drug candidate and its intended molecular target. Thereby increasing confidence in the specificity of that interaction.
In the early stages of the drug development cascade, monitoring the interaction between recombinantly expressed proteins and potential lead candidates can be done by using biophysical and biochemical assays. As confidence grows in a drug candidate during the later stages of a drug discovery project, target engagement can be measured within a more complex cellular environment.
Why are Target Engagement Assays Important?
The drug discovery pipeline faces a well-known problem with the very high attrition rate of potential drug candidates. A contributing factor to this is the lack of on-target engagement and target specificity, leading to potential off-target toxicity.
Thus, proving the target engagement of a lead compound early in a drug discovery project is imperative. This approach ensures that project resources are best utilized on the correct compounds, maximizing the chances of successful clinical progression.
How does Charnwood Discovery Confirm Target Engagement?
At Charnwood Discovery, we have extensive experience in identifying and executing the correct target engagement assays throughout a drug discovery project.
In the early stages of the project, such as hit identification, we may utilize biophysical assays (SPR, FTSA, NMR) or biochemical assays (fluorescence or luminescence-based microplate assays).
As the project progresses into lead optimization, target engagement may transition to more cell-based assays (NanoBRET, flow cytometry, high-content imaging).
At Charnwood Discovery we are very experienced in identifying and executing the correct target engagement assays throughout a drug discovery project.
At the early stages of the project, such as hit identification, this might take the form of biophysical assays (SPR, FTSA, NMR) or biochemical assays (fluorescence or luminescence-based microplate assays).
Further along the project as we enter lead optimisation, target engagement might take the form of assays that are more cell-based (NanoBRET, flow cytometry, high-content imaging).
