Pre-clinical Drug Evaluation

A major part in the field of drug discovery is to understand how the action of a drug is controlled at the physiological level. Information about the action of drugs and the exploration of potential drug safety issues is required. The dynamic real-time monitoring of the behavior of different cell types from various origins during the drug exposure enables the researcher to investigate adverse drug reactions. The Bionas DiscoveryTM 2500 system provides a valued tool for

  • Lead/hit profiling: verify hits from a primary screen using an independent/orthogonal assay
  • Drug profiling: beyond mere hit validation provide information potentiall indicative for mode of action, onset of action and even estimation of effective doselevel/exposure time in animal efficacy models 
  • Target validation: to confirm target-specific cellular actions and signaling of specific compounds

The on-line and long-term monitoring of compound actions in vitro with the Bionas DiscoveryTM 2500 system can be included in all stages of drug discovery from the initial target finding to the final characterization of leads.

Effect of compound/gold complexes on MCF-7 cells

Fig. drug 1:

Effects of gold (I) complexes with benzimidazole derived N-heterocyclic carbine (NHC) ligands (compound 2a) on MCF-7 cells on impedance (1A), respiration rate (1B) and acidification (glycolysis, 1C). The non-gold-containing compound (2) triggers only minor effects at higher concentrations on cell impedance and was almost inactive otherwise while Compound 2a shows concentration-dependent reduction in impedance, with no recovery of the cellular metabolism (Journal of Med. Chemistry, 53(24):8608-8618)

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Fig. drug 1B:

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Fig. drug 1C:

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