The Chemetics® Platform
Nuevolution’s Chemetics® technology brings a quantum leap to small-molecule lead discovery.
Today, several technologies including HTS, HCS and fragment based screening, are applied both simultaneously and consecutively world wide by big pharma and biotech companies to offer medicinal chemists a better strategy for identification of leads with optimal properties.
Fragment based small molecule lead discovery has found its place alongside high-throughput and high-content screening, influencing the mindset of medicinal chemists for what a good lead is and how to find it. Current fragment based methods apply NMR and crystallography, which represent low throughput and target material consuming methods. Typically, only hundreds to a few thousands of fragments are screened against a target of interest. All leads for potential development must be developed through evolution of fragments identified from this small subset. Furthermore, the evolution process of very low affinity fragments into high affinity ligands is often a time consuming, complex and costly affair.
In contrast, Nuevolution’s Chemetics® technology unifies the best of high throughput screening and fragment-based screening, in a simple setting, sampling millions to billions of fragments, some of which have already been evolved synthetically by use of organic synthesis.
Nuevolution’s Chemetics® technology brings fragment based lead discovery to the billion scale in number of compounds combined with efficient screening, using standard laboratory equipment.
In only 2-3 days, more than 100 million molecules may be screened by one person against a given target using only micrograms of target material and nanograms of library material.
In the screening process the target of interest is exposed to a mixture of 100 million molecules. From this mixture, the target will select those molecules with the appropriate ligand characteristics based on Nature’s evolutionary principles: The better properties – The higher chance of survival.
As in Nature, DNA embody the enabling vehicle allowing Nuevolution to work in nano scale using multi-millions of compounds in complex mixtures. Each compound within a Chemetics® library is linked to a strand of DNA encoding the synthetic history and chemical structure of the small molecule produced from a split-and-mix synthesis process. The use of DNA offers a unique opportunity for storage of chemical information. The DNA-tag provides essentially single-molecule detection by allowing amplification and sequencing for hit/lead identification from in vitro affinity screening of compound libraries of immense complexity.
Nuevolution has invented this patented technique, which is applied to biological targets of pharmaceutical importance in partnerships and internal research.
During summer of 2009, Nuevolutions fragment based library space passed the ONE BILLION small molecule compound mark.