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Lead Selection & Optimization
Stephanie Dodd, MSc. ,
Sabine Guth, PhD,
Thomas M. Smith, PhD,
Alan P. Brown, PhD, DABT ,
Erland Stevens, PhD,
W. Ross Tracey, PhD,
Sujal Deshmukh, PhD,
and
Douglas S. Auld, PhD
Stephanie Dodd, MSc. ,
Sabine Guth, PhD,
Thomas M. Smith, PhD,
Alan P. Brown, PhD, DABT ,
Erland Stevens, PhD,
W. Ross Tracey, PhD,
Sujal Deshmukh, PhD,
and
Douglas S. Auld, PhD
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.
Read more
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.
Read more
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.
Register for this course and see more details by visiting:
OpenCourser.com/course/hb2si7/lead
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.
Read more
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.
Read more
Lead Selection & Optimization, part 2
Lead Selection & Optimization, part 3
Good to know
Good to know
Know what's good ,
what to watch for , 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
Save this course
Save Lead Selection & Optimization to your list so you can find it easily later:
Save
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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
Show steps
Review foundational concepts in biological sciences and organic chemistry to establish a strong base for understanding drug discovery.
Show steps
-
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
Show steps
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
Show steps
-
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
Show steps
Reinforce the fundamentals of drug discovery through a thorough review of basic concepts.
Browse courses on
Drug Discovery
Show steps
-
Review principles of target identification and validation.
-
Revisit methods for screening and identifying lead compounds.
-
Refresh knowledge of pharmacokinetics and pharmacodynamics.
17 other activities
Expand to see all activities and additional details
Show all 20 activities
Volunteer as a mentor to assist other students in the course
Show steps
Strengthen understanding and reinforce concepts by actively helping other students in the course.
Show steps
-
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
Show steps
Refreshing your knowledge of Structure-Activity Relationships can improve your understanding of the descriptions of assays and lead optimization.
Browse courses on
SAR
Show steps
-
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
Show steps
Engage with peers to clarify concepts, exchange perspectives, and enhance overall understanding of course material.
Show steps
-
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
Show steps
Enhance understanding of drug discovery concepts through guided tutorials provided by experts in the field.
Show steps
-
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
Show steps
Enhance your ability to evaluate and select lead compounds by engaging in targeted practice exercises.
Browse courses on
Lead Selection
Show steps
-
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
Show steps
Explore resources and tutorials providing in-depth understanding of techniques used in lead optimization.
Browse courses on
Lead Optimization
Show steps
-
Search online for tutorials on lead optimization
-
Follow video demonstrations and simulations
-
Complete practice exercises to reinforce concepts
Use the ChEMBL SAR Tool
Show steps
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
Show steps
-
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
Show steps
Engage in exercises that strengthen skills in applying QSAR principles and enhance understanding of structure-activity relationships.
Show steps
-
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
Show steps
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
Show steps
-
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
Show steps
Deepen your understanding of structure activity relationships through guided tutorials and practical applications.
Browse courses on
SAR
Show steps
-
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
Show steps
Deepen understanding by researching and presenting on a specific lead optimization technique, fostering critical thinking and communication skills.
Show steps
-
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
Show steps
Enhance your comprehension and retention by creating a comprehensive summary of the case study on antimalarial therapy discovery.
Browse courses on
Drug Development
Show steps
-
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
Show steps
Gain practical experience and contribute to the field of drug discovery by volunteering at a research laboratory or non-profit organization.
Show steps
-
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
Show steps
Enhance practical knowledge by participating in a workshop focused on drug discovery and development, gaining insights from industry experts.
Browse courses on
Drug Discovery
Show steps
-
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
Show steps
Writing a literature review on lead optimization can significantly enhance your understanding of the concepts covered in the course.
Browse courses on
Lead Optimization
Show steps
-
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
Show steps
Contributing to a drug discovery project on GitHub can provide practical experience in the field.
Browse courses on
Drug Discovery
Show steps
-
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
Show steps
Volunteering at a research lab focused on drug discovery is a great way to gain exposure to practical aspects of drug discovery.
Browse courses on
Drug Discovery
Show steps
-
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.
Review prerequisite material
Show steps
Review foundational concepts in biological sciences and organic chemistry to establish a strong base for understanding drug discovery.
Show steps
Show steps
Show steps
- 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
Show steps
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
Show steps
Show steps
Show steps
- 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
Show steps
Reinforce the fundamentals of drug discovery through a thorough review of basic concepts.
Browse courses on
Drug Discovery
Show steps
Show steps
Show steps
- Review principles of target identification and validation.
- Revisit methods for screening and identifying lead compounds.
- Refresh knowledge of pharmacokinetics and pharmacodynamics.
17 other activities
Expand to see all activities and additional details
Show all 20 activities
Volunteer as a mentor to assist other students in the course
Show steps
Strengthen understanding and reinforce concepts by actively helping other students in the course.
Show steps
Show steps
Show steps
- 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
Show steps
Refreshing your knowledge of Structure-Activity Relationships can improve your understanding of the descriptions of assays and lead optimization.
Browse courses on
SAR
Show steps
Show steps
Show steps
- 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
Show steps
Engage with peers to clarify concepts, exchange perspectives, and enhance overall understanding of course material.
Show steps
Show steps
Show steps
- 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
Show steps
Enhance understanding of drug discovery concepts through guided tutorials provided by experts in the field.
Show steps
Show steps
Show steps
- 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
Show steps
Enhance your ability to evaluate and select lead compounds by engaging in targeted practice exercises.
Browse courses on
Lead Selection
Show steps
Show steps
Show steps
- 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
Show steps
Explore resources and tutorials providing in-depth understanding of techniques used in lead optimization.
Browse courses on
Lead Optimization
Show steps
Show steps
Show steps
- Search online for tutorials on lead optimization
- Follow video demonstrations and simulations
- Complete practice exercises to reinforce concepts
Use the ChEMBL SAR Tool
Show steps
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
Show steps
Show steps
Show steps
- 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
Show steps
Engage in exercises that strengthen skills in applying QSAR principles and enhance understanding of structure-activity relationships.
Show steps
Show steps
Show steps
- 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
Show steps
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
Show steps
Show steps
Show steps
- 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
Show steps
Deepen your understanding of structure activity relationships through guided tutorials and practical applications.
Browse courses on
SAR
Show steps
Show steps
Show steps
- 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
Show steps
Deepen understanding by researching and presenting on a specific lead optimization technique, fostering critical thinking and communication skills.
Show steps
Show steps
Show steps
- 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
Show steps
Enhance your comprehension and retention by creating a comprehensive summary of the case study on antimalarial therapy discovery.
Browse courses on
Drug Development
Show steps
Show steps
Show steps
- 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
Show steps
Gain practical experience and contribute to the field of drug discovery by volunteering at a research laboratory or non-profit organization.
Show steps
Show steps
Show steps
- 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
Show steps
Enhance practical knowledge by participating in a workshop focused on drug discovery and development, gaining insights from industry experts.
Browse courses on
Drug Discovery
Show steps
Show steps
Show steps
- 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
Show steps
Writing a literature review on lead optimization can significantly enhance your understanding of the concepts covered in the course.
Browse courses on
Lead Optimization
Show steps
Show steps
Show steps
- 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
Show steps
Contributing to a drug discovery project on GitHub can provide practical experience in the field.
Browse courses on
Drug Discovery
Show steps
Show steps
Show steps
- 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
Show steps
Volunteering at a research lab focused on drug discovery is a great way to gain exposure to practical aspects of drug discovery.
Browse courses on
Drug Discovery
Show steps
Show steps
Show steps
- 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:
For more career information including salaries, visit:
OpenCourser.com/course/hb2si7/lead
Reading list
We haven't picked any books for this reading list yet.
For more information about how these books relate to this course, visit:
OpenCourser.com/course/hb2si7/lead
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Level
Intermediate
Via
Coursera
Institution
Novartis
Instructors
Stephanie Dodd, MSc.
Sabine Guth, PhD
Thomas M. Smith, PhD
Alan P. Brown, PhD, DABT
Erland Stevens, PhD
W. Ross Tracey, PhD
Sujal Deshmukh, PhD
Douglas S. Auld, PhD
Session
August 12, 2024
- September 9, 2024
Language
English
Good to know
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
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