This course covers the stages of drug discovery in which promising compounds (leads) are identified, their optimal and suboptimal characteristics determined, and the suboptimal characteristics optimized to create a candidate suitable for the clinic. The course is built around a case study on the discovery of an antimalarial therapy. Assays useful for screening new compounds are outlined, examples of selection criteria for leads are discussed - such as potency, efficacy, and pharmacokinetics - and the structure activity relationships that contribute to the optimization of a lead series are considered. The phenotypic approach used by the antimalarial program will be briefly contrasted with a target-based program on a different target.
Lead Selection & Optimization
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Lead Selection & Optimization
This course is part of Drug Hunting: The Science of Making New Medicines Specialization
Instructors: Erland Stevens, PhD
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Gain insight into a topic and learn the fundamentals.
5.0
(12 reviews)
Intermediate level
Recommended experience
8 hours to complete
3 weeks at 2 hours a week
Flexible schedule
Learn at your own pace
Skills you'll gain
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Shareable certificate
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Assessments
12 assignments
Taught in English
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This course is part of the Drug Hunting: The Science of Making New Medicines Specialization
When you enroll in this course, you'll also be enrolled in this Specialization.
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There are 3 modules in this course
Welcome, by the end of the course students will be able to: Recognize malaria as a neglected tropical disease and understand its significance as an unmet medical need. Identify and describe some of the characteristics an effective small molecule therapeutic should possess, and liabilities to avoid. Describe the principles and common approaches used in defining and optimizing a lead compound's pharmacophore.
What's included
3 videos2 assignments
What's included
6 videos3 readings6 assignments
What's included
6 videos1 reading4 assignments
Offered by
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The State University of New York
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Technical University of Denmark (DTU)
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