In this course about lead selection and lead optimization, students will learn methods for discovering and optimizing leads with the end goal of advancing a compound into the clinic. The three-week course starts with the processes for finding molecules with promising activity for initiation of a drug program. The second week covers the criteria used to select the best molecules as new leads for the optimization stage. In the final week, students will learn different methods for identifying structural changes that will optimize a lead’s efficacy and PK properties as well as reduce toxicity.
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In this course about lead selection and lead optimization, students will learn methods for discovering and optimizing leads with the end goal of advancing a compound into the clinic. The three-week course starts with the processes for finding molecules with promising activity for initiation of a drug program. The second week covers the criteria used to select the best molecules as new leads for the optimization stage. In the final week, students will learn different methods for identifying structural changes that will optimize a lead’s efficacy and PK properties as well as reduce toxicity.
In this course about lead selection and lead optimization, students will learn methods for discovering and optimizing leads with the end goal of advancing a compound into the clinic. The three-week course starts with the processes for finding molecules with promising activity for initiation of a drug program. The second week covers the criteria used to select the best molecules as new leads for the optimization stage. In the final week, students will learn different methods for identifying structural changes that will optimize a lead’s efficacy and PK properties as well as reduce toxicity.
Students in the course should understand pharmacodynamics, drug activity, pharmacokinetics, and preclinical safety. Students should also be comfortable with algebraic expressions, including logarithmic and exponential functions. A fundamental understanding of the structure of organic molecules and their functional groups is also required. The course is designed in modules. Each module opens with a short video on a selected topic. The module continues with a short reading or exercise with an assessment activity. Each module will require approximately 1 hour to complete, and the course includes 15 modules. Two approaches to the course are recommended. One, a student might spend an hour per day on the course and complete all 15 modules in approximately three weeks. Two, a student with additional available time may be able to work through the entire course in just a single week or over an extended weekend.
Students signed up for the Audit Track have access to the instructional video materials. Students enrolled through the Verified Track have access to the instructional videos, the readings and activities, the assessments, as well as selected additional videos related to the primary instructional videos.
What you'll learn
general approaches to finding compounds with activity on a drug target
methods for confirming target engagement by an active compound
techniques for communicating the pharmacophore of a series of active molecules
criteria that help priorities biologically active compounds as potential leads
types of information that are most often used to guide lead optimization decisions
different functional groups that are often used to improve PK properties without affecting on-target activity in a molecule
Good to know
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Activities
Pharmacodynamics and Drug Activity Review
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Solidify the understanding of pharmacodynamics and drug activity to strengthen the foundation for lead selection and optimization.
Browse courses on
pharmacodynamics
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Review lecture notes and textbooks on pharmacodynamics.
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Solve practice problems related to drug-receptor interactions.
Explore Lead Identification Strategies
Show steps
Understand the general approaches to finding compounds with activity on a drug target.
Show steps
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Access online tutorials on lead identification techniques.
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Practice applying these techniques to case studies.
Course Materials Compilation
Show steps
Organize and review course materials to enhance understanding and retention of key concepts.
Show steps
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Gather lecture notes, slides, and assignments.
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Create a structured system for organizing materials.
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Review materials regularly to reinforce learning.
Five other activities
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Show all eight activities
Lead Selection Criteria Project
Show steps
Apply the criteria used to select the best molecules as new leads for the optimization stage.
Show steps
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Gather a dataset of active compounds.
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Apply lead selection criteria to prioritize compounds.
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Analyze the results and justify the selection.
Lead Optimization Study Group
Show steps
Engage in peer-to-peer learning and reinforce understanding by mentoring others.
Show steps
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Form a study group with peers.
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Take turns presenting and discussing lead optimization concepts.
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Provide feedback and support to group members.
Lead Optimization Techniques Article
Show steps
Develop a deeper understanding of different methods for identifying structural changes that will optimize a lead’s efficacy.
Show steps
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Research lead optimization techniques.
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Summarize key concepts in a well-written article.
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Share the article with peers for feedback.
Lead Optimization Workshop
Show steps
Learn from experts and engage in hands-on exercises to refine lead optimization skills.
Show steps
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Attend a lead optimization workshop.
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Participate in group discussions and exercises.
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Apply learnings to optimize lead compounds.
Lead Optimization Code Contribution
Show steps
Gain practical experience and contribute to the field by participating in open-source lead optimization projects.
Show steps
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Identify open-source lead optimization projects.
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Contribute code or documentation to the project.
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Collaborate with other developers to enhance the project.
Pharmacodynamics and Drug Activity Review
Show steps
Solidify the understanding of pharmacodynamics and drug activity to strengthen the foundation for lead selection and optimization.
Browse courses on
pharmacodynamics
Show steps
- Review lecture notes and textbooks on pharmacodynamics.
- Solve practice problems related to drug-receptor interactions.
Explore Lead Identification Strategies
Show steps
Understand the general approaches to finding compounds with activity on a drug target.
Show steps
- Access online tutorials on lead identification techniques.
- Practice applying these techniques to case studies.
Course Materials Compilation
Show steps
Organize and review course materials to enhance understanding and retention of key concepts.
Show steps
- Gather lecture notes, slides, and assignments.
- Create a structured system for organizing materials.
- Review materials regularly to reinforce learning.
Lead Selection Criteria Project
Show steps
Apply the criteria used to select the best molecules as new leads for the optimization stage.
Show steps
- Gather a dataset of active compounds.
- Apply lead selection criteria to prioritize compounds.
- Analyze the results and justify the selection.
Lead Optimization Study Group
Show steps
Engage in peer-to-peer learning and reinforce understanding by mentoring others.
Show steps
- Form a study group with peers.
- Take turns presenting and discussing lead optimization concepts.
- Provide feedback and support to group members.
Lead Optimization Techniques Article
Show steps
Develop a deeper understanding of different methods for identifying structural changes that will optimize a lead’s efficacy.
Show steps
- Research lead optimization techniques.
- Summarize key concepts in a well-written article.
- Share the article with peers for feedback.
Lead Optimization Workshop
Show steps
Learn from experts and engage in hands-on exercises to refine lead optimization skills.
Show steps
- Attend a lead optimization workshop.
- Participate in group discussions and exercises.
- Apply learnings to optimize lead compounds.
Lead Optimization Code Contribution
Show steps
Gain practical experience and contribute to the field by participating in open-source lead optimization projects.
Show steps
- Identify open-source lead optimization projects.
- Contribute code or documentation to the project.
- Collaborate with other developers to enhance the project.
Career center
Pharmacologist
Discovery Biologist
Computational Pharmacologist
Preclinical Scientist
Research and Development Scientist
Safety Pharmacologist
Drug Metabolism Scientist
Pharmacokinetics Scientist
Pharmaceutical Scientist
Toxicologist
Investigational Toxicologist
Regulatory Affairs Specialist
Clinical Research Associate
Biostatistician
Medical Writer
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