Determination of Half-Maximal Inhibitory Concentration of an Enzyme Inhibitor

Nikolaos Georgakis; Elisavet Ioannou; Christina Varotsou; Georgios Premetis; Evangelia G Chronopoulou; Nikolaos E Labrou

doi:10.1007/978-1-0716-0163-1_3

Determination of Half-Maximal Inhibitory Concentration of an Enzyme Inhibitor

Methods Mol Biol. 2020:2089:41-46. doi: 10.1007/978-1-0716-0163-1_3.

Authors

Nikolaos Georgakis¹, Elisavet Ioannou¹, Christina Varotsou¹, Georgios Premetis¹, Evangelia G Chronopoulou¹, Nikolaos E Labrou²

Affiliations

¹ Laboratory of Enzyme Technology, Department of Biotechnology, School of Applied Biology and Biotechnology, Agricultural University of Athens, Athens, Greece.
² Laboratory of Enzyme Technology, Department of Biotechnology, School of Applied Biology and Biotechnology, Agricultural University of Athens, Athens, Greece. lambrou@aua.gr.

PMID: 31773646
DOI: 10.1007/978-1-0716-0163-1_3

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 (K_i). This chapter describes an experimental procedure for the determination of the IC₅₀ value of an enzyme inhibitor. The relationship between IC₅₀ and K_i is also discussed.

Keywords: Enzyme inhibitor; Enzyme kinetics; Half-maximal inhibitory concentration (IC50); Inhibition potency.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology*
Inhibitory Concentration 50*
Kinetics
Molecular Docking Simulation
Pharmaceutical Preparations / chemistry

Substances

Enzyme Inhibitors
Pharmaceutical Preparations