Hit Identification

Screening services for the hit identification of lead series to start your research program towards success

The screening of drug targets against compound libraries is now a validated approach to identify the chemical starting points of drugs. There are broadly two main screening types, namely phenotypic (often systems-based and target-agnostic) and target-based (using hypothesis-driven) approaches.​

At Oncodesign, we can screen for the identification of hit compounds using our own libraries (Nanocyclix®) or those of our clients. Off-the-shelf or in-house developed robust and sensitive screening assays can be proposed for the identification of molecules with activity at the drug target.​ Simultaneously, early ADME properties can be evaluated.

Once the hit compounds have been identified, the aim of the next stage is to understand and refine the structure activity relationship (SAR) of each hit series by generating more potent and selective compounds that possess drug-like properties suitable for testing in any in vivo models. ​

Our integrated team can support your research programs from hit identification, lead optimization up to IND. We have developed offers based on your needs.

  • INPACT: integrated service in preclinical pharmacology
  • DRIVE-IDDS: integrated drug discovery solutions to generate novel drug candidates
  • SOLO: stand alone offers from our innovative technical platforms

Let’s talk about your project to know how we can best assist you.

DRIVE SM from hit identification to IND

Assay development of 3D cell culture system

Three-dimensional (3D) cell culture systems are a functionally relevant in vitro experimental approach to model human disease for a broad range of research applications. 3D cell cultures possess several in vivo features of tumors such as cell-cell interaction, hypoxia, drug penetration, response, resistance and production/deposition of extracellular matrix making them an attractive alternative to conventional 2D model systems. 3D culture systems thus have a potential to link between traditional 2D culture and animal experiments ultimately increasing the predictive value of pre-clinical drug research and bridging the gap towards anticipating clinical outcome of proposed treatments.

At Oncodesign, we have the ability and expertise to perform up to medium throughput spheroid screens in a variety of disease relevant 3D models (human and mouse cancer cell lines).

 

Screening on HCT116 with reference compound Staurosporine

In this example, HCT116 cells were grown in ultra-low attachment microplates to allow spheroid formation. Three-day old spheroids were treated with increasing concentrations of staurosporine for 72h. The spheroid growth and effect of
staurosporine were monitored using Operetta High Content Imaging System. At 72h, cell viability was assessed to determine the GI50.

Screening assay, profile of HCT116 spheroids treated with staurosporine

Legend: Profile of HCT116 spheroids treated with staurosporine

Staurosporine treatment resulted in a decreased spheroid cell viability. The GI50 was established at 32 nM.

To support your research efforts in oncology and immuno-oncology, our integrated and customized package INPACT PoC Oncology contains all the requirement for a successful preclinical program.

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