Synthesis coupled to scintillation proximity affinity screening

The rapidly changing developments in genomics and combinatorial chemistry, generating new drug targets and large numbers of compounds, are beginning t o push the limits of screening efficiently. Thus, there is a need for novel tools and strategies to improve high throughput screening. A novel approac h is to couple synthesis and screening on a common platform, rather than to increase the rate at which traditional screening methods can be implemente d, We have developed a proprietary grafted polymer with special fluorescenc e characteristics referred to as Electronically Encoded Fluorescence matriX (EFX(TM)), which has the sturdiness and required functionality for direct chemical synthesis as well as suitable surface characteristics for measurin g interactions in aqueous solution. This matrix is fabricated into a MicroT ube reactor, and each tube is associated with an electronically encoded tag , The system follows a homogenous assay protocol and is based on the scinti llation proximity principle, Using solid-phase chemistry, a variety of smal l molecules may be synthesized onto the EFX, A simple binding assay can be conducted by combining a collection of MicroTubes with any radiolabeled acc eptor molecule. The MicroTubes that carry active compounds are selected bas ed on the photon mission or fluorescence characteristics. We validated this approach by evaluating the interactions of biotin with radiolabeled strept avidin.