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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

2,665 already enrolled

Included with

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3 modules

Gain insight into a topic and learn the fundamentals.

31 reviews

Intermediate level

Recommended experience

8 hours to complete

Flexible schedule

Learn at your own pace

3 modules

Gain insight into a topic and learn the fundamentals.

31 reviews

Intermediate level

Recommended experience

8 hours to complete

Flexible schedule

Learn at your own pace

Skills you'll gain

Details to know

Shareable certificate

Add to your LinkedIn profile

Assessments

12 assignments

Taught in English

91% of learners achieved a positive career outcome

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Build your subject-matter expertise

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.

Learn new concepts from industry experts
Gain a foundational understanding of a subject or tool
Develop job-relevant skills with hands-on projects
Earn a shareable career certificate

There are 3 modules in this course

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.

Module details

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.