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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 |
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| 1. Design &
Synthesis |
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2. Array Production |
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3. Fingerprinting /
fragment screening |
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4. Data Analysis |
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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:  Elements of technology |
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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. |
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