High Throughput Screening (HTS) is one of the first phases of the drug discovery process, performed just after the conception of the idea of new drug development. Selvita supports HTS activities by employing an automated screening platform and handling internal and external libraries. We offer custom assay development, miniaturization, and adaptation for high-throughput screening/profiling services up to 1536-well plate format. With a throughput of 10,000 compounds a day we can efficiently screen different size libraries.

The HTS campaigns consist of several phases and could be adjusted on customer demand:

  • Assay development / miniaturisation / HTS adaptation
  • Pilot screen
  • Primary screen
  • Confirmation assay
  • Dose-response analysis
  • Re-ordering of solid compounds and quality check with LC-MS and NMR
  • Dose-response confirmation
  • Counterscreens / orthogonal assays
  • Hit selection and final report

Each step of the cascade is supported by the Computational Chemistry unit processing the HTS data, performing statistical and chemoinformatic triaging. The analysis based on REOS, PAINS, Eli Lilly rules, and more, could detect false positive molecules and exclude compounds without drug-likeness properties. Together with the AI approach Selvita increases customers’ chance of a successful HTS campaign.

To aid customers’ needs Selvita has initiated the design and construction of a new HTS library which will be grown and developed to provide an excellent resource for hit identification. This compound collection is supplemented by unique AnalytiCon the FideltaMacro™ libraries to further expand Selvita’s HTS capabilities (learn more here). Our Compound Management unit supports HTS activities by taking care of libraries and performing plate reformatting including the generation of Echo source plates and cherry-picking. With that support, Selvita can conduct HTS campaigns based on internal as well as external libraries, and by having capabilities for MatrixTM and FluidXTM compounds storage systems Selvita can handle customers’ compounds collections.

Our fully automated HTS platform is based on Beckman Coulter (Labcyte) Access Workstation composed of state-of-the-art devices:

  • Echo 650 acoustic dispenser
  • Certus Flex reagent dispenser
  • PHERAstar FSX multimode plate reader
  • Ancillary devices: sealer, peeler, de-lidder, centrifuge, shaker, plate hotels, barcode readers

HTS activities are furthermore supported by additional modern equipment:

  • D300e digital compounds dispensers
  • MultiFlo FX reagents and cells dispensers with washing module
  • Mantis liquid handler
  • CyBio Selma 384-well plate replicator
  • Hamilton STARlet pipetting station for plate reformatting

With Selvita’s HTS team expertise and equipment, the following readouts and corresponding assay technologies are available:

Biochemical assays:

  • binding studies (Fluorescence Polarisation, HTRF)
  • enzymatic inhibition (TR-FRET based: LanthaScreen, HTRF; luminescence-based: ADP-Glo)
  • phosphorylation studies (AlphaScreen, HTRF)
  • protease assays (FRET)
  • absorbance based assays

Cell-based assays:

  • protein receptors (e.g. GPCR) – binding and cAMP/IP level (HTRF)
  • binding in living cells (NanoBRET)
  • cytotoxicity/proliferation (luminescence-, fluorescence-, absorbance-based)
  • intra- and extracellular metabolites, protein biomarkers (AlphaLISA, HTRF)

We constantly develop our equipment and assays to meet the requirements of our customers. With our HTS capabilities and efforts, Selvita supports your drug discovery programs in the hit identification stage bringing you closer to the final drug product.

Iterative Chem Space Exploration

We offer a unique approach for building custom screening libraries by using Artificial Intelligence-enhanced chemical space exploration. This approach allows us to focus our search on those regions of chem space that are relevant to a given biological target, which increases our odds of finding good hits’​

  • A subset of our diverse, high-quality lead-like compounds library (around 25 000 compounds) is screened to obtain initial data​
  • An AI model is trained on the data to generate enriched compound set for another round of screening​
  • The process is repeated several times to yield better model (reusable in the future!) and more enriched library