The advent of genomics, high throughput screening and combinatorial chemistry has dramatically changed the dynamics of the drug discovery process.
Nowhere are these changes more apparent than in medicinal chemistry where the application of high throughput technologies is now well established. The combinatorial science is an emerging and fast-moving field. It is driven by profound expansion in our awareness of the molecular components of biology, the thirst to identity antagonists and mimetics of these biomolecules for use in biotechnology. The early emphasis on mixtures of compounds and very large numbers has largely given way to a more measured approach based on arrays of single, well characterised compounds, albeit still in significant numbers. Central is the need to increase efficiency and enhance the ability of chemists to respond rapidly to hits from high throughput screening, and this response should include the generation of broader structure-activity relationship earlier in the discovery process. Where possible we also need to extend the application of high throughput technologies, and efficient automated methods, more widely in medicinal chemistry. Key to the success of all these objectives is the development of a flexible science, integrated with medicinal chemistry and medicinal chemists.

The number of compounds in the screening collections at pharmaceutical companies has been increased dramatically with the major contribution coming from the core Combinatorial Chemistry.
High throughput compound production will without doubt continue to play an integral part in drug discovery and the use of automation in Medicinal Chemistry will see further expansion.

Pioneering work on polymer-supported reactions began in Israel in the mid-60's.
The field has found gradual acceptance in chemistry, culminating in the Nobel Prize work of Prof. Bruce Merrifield in 1984.
Combinatorial chemistry emerged from the field of polymer-supported reactions, and has become the most important method for drug discovery today. More than 3000 publications on the topic have appeared in scientific journals in the last three years.
Medium and large pharmaceutical companies have adopted combinatorial methodology as the main tool for drug discovery. To date, over 30% of bioactive leads are developed by combinatorial chemistry, and this number grows permanently. Over 25, 000 new biological targets will derive from the human genome project, a fact that points to the cardinal role of combinatorial methodology in producing drugs of the future.

In Israeli biotech companies, due to significant progress in biotechnology, the need of applying combinatorial technologies for lead discovery process apparently comes out. Currently, they perches thousands of molecules for screening, lacking their own infrastructure for generation of leads. Together with the scientists from Israel and abroad we can raise the awareness of importance of combinatorial technologies in academy and industry and assist the biotech companies to establish there own high throughput production process. The initiative has been taken at the first combinatorial conference held on May 25, 2000 in Ramat Gan, where over 100 participants attended, and 12 international companies exhibited combinatorial chemical equipment.

Regarding the need for immediate action to promote and advance this extremely important science and technology, we have initiated the establishment of the Israeli Society for Combinatorial Technology (ISCT). Our aim is to make this society the leading scientific and technological forum for the advancement of combinatorial technology in Israel for advanced drug discovery and material discovery tools.
ISCT will link to similar interactive societies in the field, to discuss organization of international activity in the fields of computational and combinatorial chemistry, high throughput screening and automation, as well as pharmaceutical and material science.
The Society is planning to organize international and local conferences, workshops and seminars to engage the scientists from Israel with leading personalities in modern drug discovery world.
Due to the novelty and importance of the methodology we hope that scientists from academy and industry will subscript for the membership to ISCT and contribute to its implementation in Israel, regardless to degree and position. The extended participation is important for leading the Israeli drug related sciences into 21 century.


Wishing fruitful cooperation