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  Graffinity's Fragment Based Drug Discovery Process – RAISE
Graffinity has pioneered RAISE (Rapid Array Informed Structure Evolution), an efficient fragment based drug discovery paradigm that enables the rapid hit identification and development of diverse novel quality leads and drug candidates.
Our Technology team has developed this unique fragment based drug discovery platform which is in routine use since 2003 for both external clients as well as In-house programs.
Our partners as well as our in house projects hereby enjoy a highly professional project management.
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  RAISE Process – Rapid Array Informed Structure Evolution
Design & Synthesis Array Production Fingerprinting / fragment screening Data Analysis Hit Evolution
1. Design & Synthesis 2. Array Production 3. Fingerprinting /
    fragment screening
4. Data Analysis 5. Hit Evolution

The 5 elements of RAISE
1. Design & Synthesis Design of fragment and leadlike molecules and high throughput synthesis followed by rigorous QC of the
    final compounds.
2. Array production Highly parallel production of chemical microarrays using proprietary, highly defined surface chemistry
3. Fingerprinting / fragment screening Simultaneous detection of Protein interactions to 10,000 small molecules via SPR
    Imaging
4. Data analysis Interaction data are combined with physicochemical compound data to interprete array results and to guide hit
    evolution chemistry
5. Hit evolution Soluble, untagged compounds are synthesized and further optimized by Medchem approaches

More Information:
For details of the process see separate document: External Link Elements of technology
 
  Paradigm     Answers
Graffinity’s paradigm provides answers to crucial questions at the earliest possible stage of the drug discovery process:
• Is the biological target druggable?
• How rich is the selection of novel molecules?
• Do our fragments give us novelty?
• Can we mix-and-match novel fragments with known compounds to rapidly develop SAR to get faster to the clinic?

In other words – the Graffinity process allows for early and cost-effective go/no-go decisions.
The complete process integrates in vitro biochemistry with in vivo pharmacology and pharmacokinetics at the earliest possible stage, and harnesses structural biology, computational chemistry, and medicinal chemistry in a powerfully synergistic drug discovery cycle. Our fragment based drug discovery process has worked with remarkable success for our partnerships as well as in our in house diabetes (DPP-IV inhibitor) and thrombosis (direct thrombin inhibitor) programs.
 
Paradigm | Process
Graffinity process
 
 
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