Tools for fragment based drug discovery

Fragment Screening

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TINS_aniTINS is a powerful method that identifies fragments that preferentially bind to a target or reference protein, even with very low affinity. Fragments to be assayed for binding are injected as mixtures of 3 – 7 compounds. Binding is detected by a reduction in the height of the NMR signals of a compound that specifically binds to the target. Comparison of the NMR spectra of the fragments in the presence of the target and reference proteins directly reveals the identity of the binding ligand(s). The TINS technology has been validated against more than 70 targets.

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The orthogonal and quantitative nature has made SPR a powerful complement to our TINS fragment screening technology. Whereas TINS is capable of identifying fragments that bind to a target with very low affinity, SPR screening is well suited for molecules that potentially bind with higher affinity and is highly quantitative.

SPR screening makes use of our expertise, obtained from TINS screening, in immobilizing functional targets. Our Biacore™ 4000 has sufficient throughput to screen our in-house or our customers library in a timely fashion.




ZoBio can implement a client’s assay or develop target specific biochemical assays optimized for fragment screening purposes. Biochemical assays can be implemented in a variety of formats. We have experience with enzyme inhibition assays and protein binding assays for e.g. protein-protein interaction targets using tr-FRET or alpha-screen technologies. Quantitative data demonstrating the efficacy and reproducibility of the assay are always provided to the customer as part of a Go / No Go decision.

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