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Small molecule drug discovery

SINTEF has long expertise in identifcation of small-molecule drug discovery for compounds that can inhibit enzymatic activity, or bind or block proteins, with high potential for drug discovery or new chemical tools.

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Small-molecule drug discovery begins with screening compounds against purified enzymes or proteins to identify binders and inhibitors. Bioactive hits are characterized, validated, and optimized to generate chemical tools and drug leads for research, diagnostics, and therapeutics.

Through participation in national and international screening consortia, we have access to large compound collections comprising clinically approved drugs, targeted inhibitors, activators, and bioactive compounds, metabolites, natural products from, e.g. marine bioprospecting, and vast collections of chemically diverse compound libraires.

Using our high-throughput screening laboratory infrastructure we can identify compounds that can modulate the biological activity or behavior of medically relevant or scientifically interesting biological processes. These compounds can then serve as chemical tool compounds, or as starting points for drug discovery and -development campaigns. These large datasets coupling biological activity to molecular structures also enable and are being used for both training and validation of in silico-models based on machine learning and AI.


How we create value

SINTEF provides integrated expertise in assay development, high-throughput screening, hit validation, biophysical characterization, and lead discovery. We design robust screening campaigns, identify high-quality hit compounds, and help de-risk projects through rigorous validation of target engagement and mechanism of action studies. SINTEF also provides expertise downstream in the drug discovery pipeline, such as evaluating safety and efficacy, drug combination effects, formulation, and drug metabolism and pharmacokinetics.

Our early drug discovery expertise supports both academic and industrial partners in translating biological insights into valuable research tools, drug candidates, and future therapeutic opportunities.

We provide expertise in discovering chemical compounds to inhibit or bind biological macromolecules such as proteins, or that block proteins from binding to each other. Our state-of-the-art research infrastructure includes most detection modalities, with a capacity of tens of thousands of assays per day. 

a high-throughput screen of ~80,000 compounds for RNAseH2 inhibition
An example of a high-throughput screen of ~80,000 compounds for RNAseH2 inhibition. Photo by Torkild Visnes/SINTEF.

Caption header image: Torkild Visnes/SINTEF.

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