How Malvern Microcal ITC Adds Value In Drug Discovery With Applications From Assay Development To Lead Optimization

The goal of pharmaceutical research is to modulate the activity of a target such that atherapeutically beneficial response is evoked. A drug is normally only efficacious when bound to and modulating the activity of its physiological target(s). Consequently much early-phase drug discovery is focused on the optimization of a drug candidate’s target affinity and selectivity.

Isothermal titration calorimetry (ITC) is widely used for measuring thermodynamic binding parameters for interactions between small molecules and proteins. The simultaneous measurement of binding affinity (KD), stoichiometry (n), free energy (ΔG), enthalpy (ΔH), and entropy (ΔS) provides important information at many stages of the drug discovery process.

The following examples illustrate how the detailed binding information provided by the MicroCal iTC200 system contributes at different stages of drug discovery.