Hit Validation: Surface Plasmon Resonance (Biacore)

SPR is a powerful, industry accepted ligand discovery technology that is orthogonal to NMR. In particular, TINS and SPR are highly complementary since both require target immobilization, while TINS provides extraordinary sensitivity to weak interactions and SPR is highly quantitative. We have shown that the combination of TINS screening with Biacore fragment characterization forms a powerful workflow for drug discovery (Kobayashi et al, J. Biomol. Screening, 2010, 15, p.978). ZoBio has a unique, highly integrated platform of TINS and SPR (Biacore T200) that allows us to further leverage our unparalleled expertise in protein immobilization for the benefit of our customers.

The sensorgrams on the left show the titrations of three fairly potent HSP90 fragment hits that were identified by TINS screening. The KD determined by Biacore, varying from double digit µM to a few hundred µM, is in extremely good correspondence with the values determined via an orthogonal method, protein observed NMR using HSQC experiment