Targets, Assays & Screening
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Targets, Assays & Screening
This course is part of Drug Hunting: The Science of Making New Medicines Specialization
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What you'll learn
Promising compounds used in the hunt for novel drugs. Types of assays & methods used to screen molecule libraries. Methods for hit validation.
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There are 3 modules in this course
This course focuses on the early stages of drug discovery and the identification of promising compounds with which to begin the hunt for a novel drug. Different types of assays and methods are reviewed that are used to screen libraries of molecules in the preliminary search for compounds with activity. Methods are discussed for validating that active molecules are indeed engaging a target associated with a predicted therapeutic benefit.
Target audience: This course is suitable for life scientists, clinicians, and individuals from fields that support drug discovery (e.g., patents, finance, licensing, etc.) interested in learning more about the pharmaceutical/biotechnology sector. Advanced undergraduate coursework or practical familiarity/working knowledge in biological sciences and organic chemistry is recommended.
Welcome, by the end of the course students will be able to: Recognize the differences between target-based and phenotypic drug discovery. Differentiate between common library types and screening approaches for identifying small molecule hits. Describe some of the assay types used in early screening and factors to consider in their design.
What's included
5 videos2 readings3 assignments
5 videos•Total 34 minutes
- Course Welcome•1 minute
- Interview with Scott Busby, Discovery Sciences•18 minutes
- Early Discovery Definitions•5 minutes
- Target-Based Drug Discovery•5 minutes
- Phenotypic Drug Discovery•6 minutes
2 readings•Total 20 minutes
- The complement system as an example of target selection•10 minutes
- Recent Advances in Phenotypic Drug Discovery•10 minutes
3 assignments•Total 90 minutes
- Assessment•30 minutes
- Knowledge Check•30 minutes
- Knowledge Check•30 minutes
What's included
5 videos3 readings6 assignments
5 videos•Total 26 minutes
- Factors in Assay Design•6 minutes
- Molecular Space•6 minutes
- Compound Libraries•5 minutes
- High-Throughput Screening and the Primary Assay•5 minutes
- Orthogonal Assays, Counterscreens, and PAINS•4 minutes
3 readings•Total 30 minutes
- IC50 and Ki•10 minutes
- Evolution of commercially available compounds for HTS•10 minutes
- Assay Interference by Aggregation•10 minutes
6 assignments•Total 190 minutes
- Assessment•40 minutes
- Knowledge Check•30 minutes
- Knowledge Check•30 minutes
- Knowledge Check•30 minutes
- Knowledge Check•30 minutes
- Knowledge Check•30 minutes
What's included
5 videos2 readings3 assignments
5 videos•Total 19 minutes
- Fragment-Based Drug Discovery•5 minutes
- In Silico Screening•4 minutes
- Hit Validation•4 minutes
- Future Directions for Screening•5 minutes
- Farewell •1 minute
2 readings•Total 20 minutes
- Improving potency of fragments•10 minutes
- Hit Validation Methods•10 minutes
3 assignments•Total 90 minutes
- Assessment•30 minutes
- Knowledge Check•30 minutes
- Knowledge Check•30 minutes
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Reviewed on Jun 24, 2025
this course is very well designed. it really cleared my concepts and equipped me with sufficient knowledge and guide about target and assays
Reviewed on Jun 22, 2025
Great course. Clear explanations and very easy to digest materials. Thanks to the entire team
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