Binding kinetics is an important aspect of drug design and has been studied for many years. While all pharmaceutical drugs are unique, there are vast similarities between their binding kinetics.
Binding kinetics refers to the rate at which a compound binds to a target molecule and the speed at which it dissociates. Binding kinetics measure the on- and off-rate. However, this has been a challenging task for many years.
This article will discuss the fundamentals of binding kinetics and how they work.
The importance of binding affinity
Binding affinity refers to the level of drug needed to occupy 50% percent of a target molecule at equilibrium. This number, called the target occupancy, predicts in-vivo drug efficacy.
Another significant quantitative value that governs pharmaceutical drug efficacy is residence time. This value refers to the time it takes for drug receptors to reach target occupancy.
The importance of binding kinetics in affinity measurements
The time to reach equilibrium is dependent on the dissociation time. For this reason, binding kinetics are extremely important for binding affinity measurements. When the opposing rates are equal, a critical reaction is at equilibrium.
For dissociation to occur, the association must first take place. To effectively measure binding affinity, complete data on binding kinetics is required. A main advantage of using binding kinetics is that equilibrium does not need to be met, making it a much more rapid approach.
Binding kinetics in drug discovery
Incorrect dosing can cause undesired outcomes in patients. If binding affinity measurements are below the actual affinity, the risk of overdose in clinical trials is increased. If lower than the actual affinity, under-dosing of potentially life-saving drugs can occur.
There is an intrinsic link between binding kinetics and drug safety, efficacy, and the duration of response outcomes.
Measuring binding kinetics
Developing safe and efficacious drugs requires an in-depth understanding of a molecule’s binding kinetics. Equilibrium constants, such as koff, kon, and KD, must be established to understand kinetics.
koff is the dissociation constant in min-1. kon is the association constant in inverse minutes multiplied by inverse concentration. Calculating koff/ kon produces KD, which is expressed in Molar units.
Gator Bio provides biolayer interferometry (BLI) solutions for the measurement of kinetics, using real-time data and measuring kon and koff (binding kinetics) and KD (binding affinity.)
Insights into association/disassociation rates and binding affinity values aid the in-vivo prediction of biomolecular binding to target proteins/receptors. To explore the company’s full range of technical solutions for measuring binding kinetics and biomolecule activity, contact an expert at Gator Bio today
About Gator Bio, Inc.
Gator Bio is a world-leading biosensor company headquartered in Palo Alto, CA. At Gator Bio, we provide researchers the tools and instrumentation to advance their research. From antibody engineering to small molecule drug discovery to basic research, Gator Bio can be used to bring meaning to the unknown. From the original inventors of label-free biolayer interferometry (BLI), Gator Bio provides the next generation of BLI technology.
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