Compound target assay
For supporting medical chemistry optimisation, we can provide mutational scanning of your drug target to help identify residuals that are required for the compound target interaction.
In the example shown, a cancer cell with a mutation is dependent on the drug target for survival - synthetic lethality. We can take advantage of this to identify which residuals are required for your drug target–compound interaction using our saturated mutagenesis service, supported by parallel drug target specific cell based reporter assays. Pettitt et al 2018,
Resistance to drugs often occurs via acquired mutations in the target, which may block drug binding or lead to constitutive activation. Screening for this early in the drug development process can help to optimise compounds and make developement of resistance less likely.