21st EFMC Short Course on Medicinal Chemistry

Course Outline

How can thousands of compounds be designed, synthesized, and tested in weeks rather than months? Direct-to-Biology (D2B) is reshaping drug discovery by enabling rapid screening of crude or minimally purified reaction mixtures, dramatically accelerating the journey from idea to biological data.

This interactive course guides participants through the complete D2B workflow, from the origins and evolution of the field to state-of-the-art approaches used in modern discovery programs. Participants will learn how to design high-value libraries, select and manage building blocks, determine optimal library size, and leverage computational tools and AI to prioritize compounds and maximize information gain.

The course will examine the chemistry that enables D2B, including reaction selection, impurity management, and semi-purification strategies, while exploring the critical question: when is a reaction mixture “good enough” for biological testing? Participants will also learn how chemistry, impurities, and assay design interact to influence data quality, hit identification, and decision-making.

Finally, the course will cover analytical strategies for characterizing and quantifying target compounds in crude and semi-purified mixtures, translating complex chemical mixtures into reliable biological data. Through case studies and hands-on exercises, attendees will gain practical tools and decision frameworks to successfully implement D2B approaches in modern drug discovery.

Course Set-up

This intensive course is designed for scientists already active in the field and with a solid foundation, and will feature presentations by senior experts from both industry and academia. The number of participants is limited to 35, to allow in depth discussion. Should the number of applications exceed the maximum, preference will be given to applicants from EFMC adhering countries and employees of EFMC corporate members. Upon special request to the organisers, only based on financial conditions and supported by an argued recommendation of the head of the department of the applicant, up to 3 applicants from academia may be admitted at a reduced fee.