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The identification, characterization, and validation of small molecule compounds with therapeutic potential is a core activity of CDoT, and one that taps into the expertise of all of our functional groups. Our experienced drug discovery scientists collaborate with ӳ����ý researchers to design and develop a variety of biochemical and biophysical assays. Our automation laboratory can perform high-throughput screening on tens of thousands of compounds from our distinct libraries selected from the ӳ����ý’s collection of 350,000+ compounds, or we can leverage larger compound libraries through CROs. We can support a variety of assay formats and readouts, including plate-reader based assays and high-content imaging.

We have significant experience developing assay funnels that are used to orthogonally validate hits identified from high-throughput screening and support medicinal chemistry optimization of hits. We can characterize a compound's biochemical activity, binding kinetics, binding thermodynamics, as well as impacts on cellular growth, signaling, and morphology.

We collaborate closely with ӳ����ý investigators and the other groups within CDoT to identify the most appropriate reagents and assays for identification of small molecules with the desired biological activity. Working alongside the Compound Management and Informatics groups, our team can track and analyze experimental data. We are tightly connected to the Medicinal Chemistry team, leveraging the in vitro data generated to effectively validate hits and progress compounds into hit to lead.

To find and then validate small molecule “hits”, we employ a wide variety of biochemical and biophysical capabilities including:

• 600 MHz NMR with cryo probe suitable for both protein and ligand-observe experiments; with autosampler ideal for rapidly performing fragment screens with in-house library
• Multiple high throughput surface plasmon resonance (SPR) instruments
• Isothermal titration calorimetry (ITC) and differential scanning calorimetry (DSC) instrumentation
• Microscale thermophoresis (MST) instrumentation