It is important in drug discovery to ensure that a chemical probe in development engages the intended target within a cellular environment. While in a biochemical or biophysical setting with recombinant proteins, it can provide critical insights around binding modes which is beneficial for SAR development from the hit series; however these don’t guarantee translation into phenotypic effects. The cellular environment includes state of the target, its concentration, and if it resides in complex with other proteins or co-factors. Therefore, in-cell target engagement studies provide a critical link bridging biochemical and phenotypic effects, offering direct evidence if the method of drugging is appropriate.
o2h offers different target engagement assays that can suggest compound permeability, quantitatively measure target occupancy, rank order compounds, study residence time, enable the assessment of compound efficacy and mode of action.
For new drug discovery programs and first-in-class chemical tools, academic exploration is necessary. This requires assessment of the target to first address target modulation, druggability, assayability, and potential to achieve differentiation from other strategies. Therefore, target validation can support in the technical evaluation, if the target has a key role in disease progression, and if pharmacological modulation is possible and effective in defined patient population. o2h can tailor assay development and offer a complementary suite to build strong evidence for your biological targets.
To know more about our biology services offering or to request our brochure, please reach out to us at discovery@o2h.com.
