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  • Beside potency data (IC50 or Ki) obtained from screening experiments, data obtained from kinetic studies are very important for appropriate understanding and interpretation of drug-target interaction.
  • During lead optimization campaigns increased affinity of the compounds is very often driven by slow dissociation of the compounds from the target protein and consequently long residence time.
  • Classification of compounds as a fast or slow reversible or irreversible compounds contributes to improvement of pharmacodynamics effects and mitigation of toxicity.  
  • At Fidelta, we are using continuous enzymatic assays for studying enzyme kinetics of various protein families. With measurement of both, on- and off-rates, we are able to determine various parameters such as type of inhibition, reversibility, binding kinetics, kon, koff, t1/2, residence time (τ), Ki and IC50.
  • When it is technically feasible we can also develop displacement assays for determination of kinetic parameters (koff, t1/2, residence time (τ)).

Compound evaluation flowchart

Determination of kinetic parameters - examples


Copeland RA, Evaluation of enzyme inhibitors in drug discovery, 2nd ed., Wiley & Sons, 2013
Swinney DC, Biochemical mechanisms of drug action: what does it take for success, Nat Rev Drug Discov, 2004, 3(9):801-808
Copeland RA et al, Impact of enzyme concentration and residence time on apparent activity recovery in jump dilution analysis, Anal Biochem, 2011, 416:206-210

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