Lead Selection & Optimization

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.

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.

What's inside

Syllabus

Lead Selection & Optimization, part 1

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.

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Read about what's good

what should give you pause

and possible dealbreakers

Introduces learners to the fascinating field of drug discovery, empowering them to gain a deeper understanding of the processes behind bringing life-saving medications to patients

Led by renowned academic experts and distinguished scientists, this course offers unparalleled insights into the drug discovery landscape

Emphasizes the importance of optimizing suboptimal characteristics during drug discovery, enhancing the potential for successful clinical applications

Provides a comprehensive overview of the drug discovery process, covering key stages and methodologies

Delves into the specifics of lead selection, optimization, and structure activity relationships, equipping learners with practical knowledge and tools

Suitable for a diverse audience ranging from scientists and clinicians to professionals in supporting roles, fostering interdisciplinary collaborations

Reviews summary

In-depth drug lead optimization

According to students, this course offers an incredibly well-structured and deep dive into lead selection and optimization, particularly benefiting professionals in drug discovery. Learners praise the real-world insights provided by Novartis instructors and highlight the brilliant case study on antimalarial therapy. The course provides a solid foundation and helps solidify understanding of the drug discovery pipeline, with practical discussions on SAR, pharmacokinetics, potency, and efficacy. However, a few reviewers noted that the course assumes a strong background in biological sciences and organic chemistry, potentially making it challenging for those without extensive prior knowledge or mid-level scientists. It is definitively not for casual learners.

Pace is suitable for professionals, potentially slow for some.

"My only minor critique is that some of the earlier modules felt a bit slow if I already have a strong chemistry background."

"I found the pace just right as a professional looking to refresh or deepen my knowledge."

Benefits from industry expertise and a compelling case.

"The case study on antimalarial therapy was a brilliant way to illustrate complex concepts."

"The instructors from Novartis provided real-world insights that were invaluable."

"I found the real-world examples given by the instructors to be top-notch."

"The Novartis perspective added significant credibility and practical relevance for me."

Covers complex topics with real-world application.

"This course is incredibly well-structured and provides a deep dive into lead selection and optimization."

"The content on identifying and optimizing lead compounds was exactly what I needed for my role."

"I appreciated the focus on practical applications and the discussions on liabilities to avoid."

"The explanations of potency and efficacy were clear, and the overall structure made complex topics digestible."

Assumes deep prior knowledge, can be challenging otherwise.

"I found it quite challenging without a very strong background in organic chemistry. Some concepts were introduced quickly..."

"The material felt very dense and assumed a lot of prior knowledge, even with the prerequisites stated."

"It's likely great for highly experienced people, but for someone like me (mid-level scientist), it was a bit overwhelming."

"This course definitely requires commitment and the recommended background; it's not for casual learners."

Activities

Be better prepared before your course. Deepen your understanding during and after it. Supplement your coursework and achieve mastery of the topics covered in Lead Selection & Optimization with these activities:

Review prerequisite material

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Review foundational concepts in biological sciences and organic chemistry to establish a strong base for understanding drug discovery.

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Review textbooks and lecture notes from previous courses.
Complete practice problems and exercises to strengthen understanding.
Attend office hours or online discussion forums for clarification.

Find a Mentor in Drug Discovery

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Finding a mentor can provide insights and guidance to better navigate the complex field of drug discovery, the focus of this course.

Browse courses on Drug Discovery

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Identify potential mentors in your field of interest.
Reach out to potential mentors and express your interest in learning from them.
Meet with your mentors and discuss your career goals.

Review Drug Discovery Basics

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Reinforce the fundamentals of drug discovery through a thorough review of basic concepts.

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Review principles of target identification and validation.
Revisit methods for screening and identifying lead compounds.
Refresh knowledge of pharmacokinetics and pharmacodynamics.

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Volunteer as a mentor to assist other students in the course

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Strengthen understanding and reinforce concepts by actively helping other students in the course.

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Express interest in becoming a mentor through course forums or instructors
Provide guidance and support to mentees on course content, assignments, and study strategies
Attend mentor training sessions or webinars to enhance mentoring skills (optional)

Review Structure-Activity Relationships

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Refreshing your knowledge of Structure-Activity Relationships can improve your understanding of the descriptions of assays and lead optimization.

Browse courses on SAR

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Review the introduction to an organic chemistry textbook.
Review the principles of SAR in a book chapter.
Read a research paper on SAR in the Journal of Medicinal Chemistry.
Attend a virtual seminar on SAR and drug discovery.

Join a study group to discuss course concepts

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Engage with peers to clarify concepts, exchange perspectives, and enhance overall understanding of course material.

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Identify potential study partners or join existing groups
Schedule regular meetings and establish clear goals for each session
Review course materials together, discuss key concepts, and solve problems collaboratively

Explore online tutorials on drug discovery

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Enhance understanding of drug discovery concepts through guided tutorials provided by experts in the field.

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Identify relevant tutorials from reputable sources.
Follow the tutorials step-by-step, taking notes and asking questions.
Apply the knowledge gained to the course materials.

Practice Lead Selection Criteria

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Enhance your ability to evaluate and select lead compounds by engaging in targeted practice exercises.

Browse courses on Lead Selection

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Solve problems involving the application of potency, efficacy, and pharmacokinetic criteria.
Analyze case studies of successful lead selection processes.
Simulate the decision-making process involved in prioritizing lead compounds.

Learn about lead optimization techniques

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Explore resources and tutorials providing in-depth understanding of techniques used in lead optimization.

Browse courses on Lead Optimization

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Search online for tutorials on lead optimization
Follow video demonstrations and simulations
Complete practice exercises to reinforce concepts

Use the ChEMBL SAR Tool

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Gaining familiarity with the ChEMBL SAR Tool can provide insights to assist in the lead selection process, as described in the course.

Browse courses on Drug Discovery

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Visit the ChEMBL website and create an account.
Watch the 'Introduction to ChEMBL' tutorial.
Use the 'SAR Tool' to explore the structure and activity data of compounds.
Analyze the results and identify potential lead compounds.

Practice solving quantitative structure-activity relationship (QSAR) problems

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Engage in exercises that strengthen skills in applying QSAR principles and enhance understanding of structure-activity relationships.

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Find online resources or textbooks with QSAR practice problems
Solve practice problems and compare results with provided solutions
Analyze and interpret the outcomes of QSAR calculations

Solve Lead Selection and Optimization Problems

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Solving lead selection and optimization problems can clarify the lead selection criteria discussed in the course and refine your approach to optimizing leads.

Browse courses on Lead Selection

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Review the lecture on lead selection and optimization.
Find practice problems in a textbook or online.
Attempt to solve the problems independently.
Check your answers and identify areas for improvement.
Seek help from a tutor or instructor if needed.

Follow Tutorials on Structure Activity Relationships

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Deepen your understanding of structure activity relationships through guided tutorials and practical applications.

Browse courses on SAR

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Explore online tutorials and resources on SAR concepts.
Practice identifying structural features that influence drug activity.
Apply SAR principles to optimize lead compounds.

Create a presentation on a specific lead optimization technique

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Deepen understanding by researching and presenting on a specific lead optimization technique, fostering critical thinking and communication skills.

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Choose a lead optimization technique to research and present on
Gather information from scientific literature, textbooks, and online resources
Design and prepare a presentation that clearly explains the technique, its applications, and limitations
Practice delivering the presentation to improve communication skills

Create a Summary of Antimalarial Drug Discovery

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Enhance your comprehension and retention by creating a comprehensive summary of the case study on antimalarial therapy discovery.

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Consolidate key concepts and findings from the case study.
Synthesize information from various sources into a coherent summary.
Utilize visual aids or diagrams to illustrate key points.

Volunteer at a research laboratory or non-profit organization

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Gain practical experience and contribute to the field of drug discovery by volunteering at a research laboratory or non-profit organization.

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Identify research laboratories or non-profit organizations involved in drug discovery.
Contact the organization and inquire about volunteer opportunities.
Commit to a regular volunteering schedule and actively participate in research activities.
Network with researchers and gain insights into the drug discovery process.

Attend a workshop on drug discovery and development

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Enhance practical knowledge by participating in a workshop focused on drug discovery and development, gaining insights from industry experts.

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Research and identify upcoming workshops in the field
Register for and attend the workshop
Actively participate in sessions, ask questions, and network with professionals

Write a Literature Review on Lead Optimization

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Writing a literature review on lead optimization can significantly enhance your understanding of the concepts covered in the course.

Browse courses on Lead Optimization

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Choose a specific topic in lead optimization.
Search for and gather relevant research papers.
Read and analyze the papers.
Synthesize the information into a coherent narrative.
Write and submit your literature review.

Contribute to a Drug Discovery Project on GitHub

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Contributing to a drug discovery project on GitHub can provide practical experience in the field.

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Find a drug discovery project on GitHub that interests you.
Read the project documentation and understand the project goals.
Identify an area where you can contribute your skills.
Fork the project and make your changes.
Submit a pull request and discuss your changes with the project maintainers.

Volunteer at a Research Lab Focused on Drug Discovery

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Volunteering at a research lab focused on drug discovery is a great way to gain exposure to practical aspects of drug discovery.

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Identify research labs in your area that focus on drug discovery.
Contact the labs and inquire about volunteer opportunities.
Attend volunteer orientation and training.
Perform assigned tasks and assist with research projects.

Career center

Learners who complete Lead Selection & Optimization will develop knowledge and skills that may be useful to these careers:

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What's inside

Syllabus

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Reviews summary

In-depth drug lead optimization

Activities

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