Application Note: Multiparameter profiling of a Structure Activity Relationship (SAR) library for immunological activity in human PBMCs

We describe a no-wash, high throughput screen that provides a multiparametric activity profile for a structure activity relationship (SAR) library derived from immunomodulatory compounds…

The success of immunomodulatory approaches for the treatment of disease has generated tremendous interest in discovery of new immunotherapy based therapeutics. Immunotherapy has the potential of affecting – positively and negatively – the myriad interactions among cells and signaling molecules regulating the immune system, and projects should include high throughput screening campaigns aimed at profiling the effects of compounds on these complex interactions.

We describe a no-wash, high throughput screen that provides a multiparametric activity profile for a structure activity relationship (SAR) library derived from immunomodulatory compounds.

Methods

Seven known immunomodulatory compounds were used as templates to generate an SAR expansion library of 1438 compounds. The selection utilised a combination of various substructure and similarity search methods combined with the generation of virtual templates.