A Guide to Enzyme Kinetics in Early Drug discovery.

  title={A Guide to Enzyme Kinetics in Early Drug discovery.},
  author={Bharath Srinivasan},
  journal={The FEBS journal},
  • B. Srinivasan
  • Published 17 February 2022
  • Biology, Chemistry
  • The FEBS journal
Drugs interact with their target of interest to bring about the desired phenotypic outcome that results in disease alleviation. Traditionally, most lead optimization exercises were driven by affinity measures (like IC50 ) to inform structure-activity relationship (SAR)-guided medicinal chemistry. However, an IC50 value is a thermodynamic estimate measured under equilibrium conditions that can vary as a function of substrate concentration and/or time (the latter especially for non-equilibrium… 
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