Drug Discovery and Development
The number of pharmaceutical compounds derived from natural products is immense. Searching for new lead structures is increasingly causing a bottleneck in the pharmaceutical industry’s drug discovery operations.
Natural products are biologically validated and provide a rich resource of structural diversity. Natural products develop from their interaction with enzymes/proteins - which are to an extent highly specific – their high potential for biological activity.
AnalytiCon has carried out innovations in the field of screening natural product-based compounds!
Efficient screening of natural product-based compounds from reliable access to the natural resources through to the selection of candidates for development places particular demands in terms of expertise and technological equipment! Thanks to new technologies, the use of chemoinformatic tools and a lean NP-specific organization, natural product-based compound screening is different at AnalytiCon – but not necessarily more complicated. Only a few teams worldwide have the critical mass to efficiently execute all steps in-house. These range from fermentation to complex syntheses and development work. AnalytiCon Discovery with its 60 employees belongs to the top five global natural product drug discovery teams.
AnalytiCon’s unique track record
- AnalytiCon is the worldwide leading supplier of natural product-based drug discovery concepts. The company is backed by 20 years’ successful co-operation with 60 companies from the pharmaceutical industry, including Johnson & Johnson, GlaxoSmithKline, Pfizer, Merck, Boehringer Ingelheim, Sanofi-Aventis, Wyeth, Genentech, Amgen and Takeda.
- In 200 screening campaigns to date, natural products and natural product-based semi-synthetic substance libraries have so far produced hit rates of between 0.01 and 5.1%, the average currently being 1.3%. More than 90% of the primary hits were confirmed in confirmatory assays on de novo produced substances. Nowadays NATx and MEGx are a part of every well-organized industrial compound repository. This is also a result of the huge diversity of structures from AnalytiCon available.
- 20 employees are working on the synthetic optimization of natural products from early SAR libraries up to complete hit-to-lead programmes to optimize their effects, their stability, their pharmacology and their IP positions. This is taking place at a speed which is breath-taking for natural product-based compound research. In several cases up to 50g of a compound optimized over several cycles could be supplied for initial in vivo experiments in less than 9 months after the first hit.
- In several projects, some of which have been published* (!), AnalytiCon has not only realized the successful interactive of natural-product chemistry and synthetic chemistry, but has proved the symbiosis of natural product and computer chemistry. This includes the use of virtual screenings for efficient compound searches and the use of initial hits to open up new structure options using scaffold-hopping strategies.
