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Determination of Half-Maximal Inhibitory Concentration of an Enzyme Inhibitor

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Targeting Enzymes for Pharmaceutical Development

Part of the book series: Methods in Molecular Biology ((MIMB,volume 2089))

Abstract

Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. Enzymes are one of the most important groups of drug targets; thus, enzyme inhibition is widely used for the treatment of certain disorders. The assessment of an inhibitor against an enzyme is predominantly based on two different parameters: the half-maximal inhibitory concentration (IC50) and the inhibition constant (Ki). This chapter describes an experimental procedure for the determination of the IC50 value of an enzyme inhibitor. The relationship between IC50 and Ki is also discussed.

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Acknowledgments

This work was supported by the Hellenic Foundation for Research and Innovation (HFRI) and the General Secretariat for Research and Technology (GSRT), under the HFRI PhD Fellowship grant (GA. No. 8904/22-09-2017).

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Authors and Affiliations

  1. Laboratory of Enzyme Technology, Department of Biotechnology, School of Applied Biology and Biotechnology, Agricultural University of Athens, Athens, Greece

    Nikolaos Georgakis, Elisavet Ioannou, Christina Varotsou, Georgios Premetis, Evangelia G. Chronopoulou & Nikolaos E. Labrou

Authors
  1. Nikolaos Georgakis
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  2. Elisavet Ioannou
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  3. Christina Varotsou
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  4. Georgios Premetis
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  5. Evangelia G. Chronopoulou
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  6. Nikolaos E. Labrou
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Corresponding author

Correspondence to Nikolaos E. Labrou .

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Editors and Affiliations

  1. Department of Biotechnology, Agricultural University of Athens, Athens, Greece

    Nikolaos E. Labrou

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Georgakis, N., Ioannou, E., Varotsou, C., Premetis, G., Chronopoulou, E.G., Labrou, N.E. (2020). Determination of Half-Maximal Inhibitory Concentration of an Enzyme Inhibitor. In: Labrou, N. (eds) Targeting Enzymes for Pharmaceutical Development. Methods in Molecular Biology, vol 2089. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-0163-1_3

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  • DOI: https://doi.org/10.1007/978-1-0716-0163-1_3

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  • Publisher Name: Humana, New York, NY

  • Print ISBN: 978-1-0716-0162-4

  • Online ISBN: 978-1-0716-0163-1

  • eBook Packages: Springer Protocols

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