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Novel chemical modalities in drug discovery


Admission requirements

Master students of Bio-Pharmaceutical Sciences, Chemistry, Biology, Biomedical Sciences, Life Science & Technology, Molecular Science & Technology, and related.
Required background knowledge basic knowledge of Biochemistry and Organic Chemistry 1&2 (4011OCH15Y and 4052ORGC2 for BSc MST or equivalent).


In this course the students will learn about bioactive chemical modalities beyond classical small molecule drugs. These novel chemical modalities enable the targeting of challenging disease mechanisms that are inaccessible by traditional drugs. The course will give insights into the development of antisense oligonucleotide therapeutics, peptide based drugs, antibody drug conjugates, covalent inhibitors and molecular glues. Antisense oligos target specific RNA sequences and block the expression of disease related proteins. Peptide based drugs often are designed to target disease related protein-protein interactions. Antibody-drug conjugates are used to deliver cytotoxic payloads to degenerate cells with a high specificity. Covalent drugs achieve longer target inhibition then reversible ligands. Molecular glues can recruit the proteasomal degradation machinery to specific target, and break them down. For each chemical modality the course will cover the basic mechanisms and some examples, based on recent literature. Further the course will show some design and discovery strategies for each modality class. The chemical synthesis strategies for several novel chemical modalities will be studied (e.g., chemical oligonucleotide synthesis, peptide synthesis, bioconjugation reactions).

Course objectives

After following this course the participants will have good insights into the mechanisms and chemistry of novel chemical modalities in drug discovery. For chemical biologists, medicinal chemists and drug discovery scientists this knowledge will be essential and highly valuable, both for a career in academia and in industry. In detail the participants will:

  • Know which novel chemical modalities exist beyond classical small molecule drugs (e.g., antisense oligonucleotides, peptide based modalities and antibody drug conjugates)

  • Be able to understand and explain mechanisms and applications of novel chemical modalities

  • Explore discovery strategies for novel chemical modalities

  • Learn about the chemistry used to create novel chemical modalities

  • Be able to read and understand recent scientific literature


This course is scheduled for semester 1, period 2.

You will find the timetables for all courses and degree programmes of Leiden University in the tool MyTimetable (login). Any teaching activities that you have sucessfully registered for in MyStudyMap will automatically be displayed in MyTimeTable. Any timetables that you add manually, will be saved and automatically displayed the next time you sign in.

MyTimetable allows you to integrate your timetable with your calendar apps such as Outlook, Google Calendar, Apple Calendar and other calendar apps on your smartphone. Any timetable changes will be automatically synced with your calendar. If you wish, you can also receive an email notification of the change. You can turn notifications on in ‘Settings’ (after login).

For more information, watch the video or go the the 'help-page' in MyTimetable. Please note: Joint Degree students Leiden/Delft have to merge their two different timetables into one. This video explains how to do this.

A detailed course schedule will be published on Brightspace.

Mode of instruction

Lectures, tutorials, self-tuition, classroom exercises and presentations

Assessment method

The assessment will be based on an oral presentation (30%) and a written exam (70%).

The presentation will be on a scientific paper (related to the topics treated in the course). The paper will be assigned by the lecturer.

For each individual exam, the grade is expressed either with pass or fail, or by using a decimal integer between 1.0 and 10.0 that should be ≥ 5.5. The final grade is expressed using an integer between 1 and 10 and can be rounded off/up to a half integer, with the exception of the grade 5.5. Final grades between 5.50 and 5.99 will be rounded up to 6.0. The final grade should be 6.0 to successfully complete this course.

The time and manner of the inspection and of the feedback session on the examination are specified in the Brightspace module of the course.

Reading list

The list will be announced during the course. Will be mainly based on scripts of the course and scientific literature provided by the lecturer.


Every student has to register for courses with the enrollment tool MyStudyMap. There are two registration periods per year: registration for the fall semester opens in July and registration for the spring semester opens in December. Please see this page for more information.

Please note that it is compulsory to both preregister and confirm your participation for every exam and retake. Not being registered for a course means that you are not allowed to participate in the final exam of the course. If you want to retake of the exam of the course without following the lectures, you have to contact the coordinator of the course to see if this is possible (you would have to passed the other assignments of the course in the earlier year).
Confirming your exam participation is possible until ten days before the exam.

Extensive FAQ's on MyStudymap can be found here.


Dr. Sebastian Pomplun (e-mail: +31(0)71 527 4651


A minimum of 5 students and a maximum of 20 master students applies to this course. Placement is based on the registration date in MystudyMap.

This information is without prejudice. Alterations can be made for next year.

This information is without prejudice. Alterations can be made for next year.