This review summarizes findings in the literature related to compound selection in the drug discovery process. By performing parallel optimizations of association and dissociation rates, compounds with desirable kinetic profiles for target binding may be generated. In addition, compound selection may also consider the kinetic properties of ADME marker binding profiles, further refining the quality of compounds early in the drug discovery process.

A “must read” for anyone doing small molecule assays. This paper illustrates applications of Biacore besides direct binding kinetics and affinity e.g. to measure the effect of binders on kinase activity and competition studies.

A comparison between Biacore results and those from a PAMPA (parallel artificial membrane permeability assay), which was in common usage, prior to Biacore, for determining lipid retention of small molecules.  The authors were able to use the Biacore data to discriminate structurally related compounds.

An approach for studying drug-lipid interactions in early in vitro ADME applications, using two types of immobilized liposomes for simultaneous resolution of lipid absorption characteristics. The paper provides a “how-to” guide and highlights the advantages for drug discovery applications compared to existing methods.

Experimental procedures are described in detail as well as the calculations required to obtain thermodynamic constants (ΔG, ΔS, ΔH).

Data are presented as on-rate/off-rate plots under different pH conditions. Includes a discussion on why biotinylation is better than amine coupling for ligands with low pI values. Also discusses the importance of on and off rates compared with affinity measurements alone.

How to mesaure binding of drugs to liposomes. Reproducibility of liposome capture, relative drug binding responses, kinetics of drug binding, liposome capture with lipids of various composition, effect of amount of captured liposome on drug binding, comparison of drug/lipid interactions under different experimental conditions