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
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Activities
Review organic chemistry functional groups
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Ensure you have a strong foundation in organic chemistry concepts, especially functional groups, to support your understanding of lead optimization.
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Organic Chemistry
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Review your notes or a textbook on organic chemistry functional groups
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Practice identifying functional groups in molecules
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Complete practice problems or quizzes on functional group chemistry
Review basic concepts in pharmacodynamics and pharmacokinetics
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Strengthen your understanding of the basic principles of pharmacodynamics and pharmacokinetics to enhance your comprehension of lead optimization.
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pharmacodynamics
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Review your notes or a textbook on pharmacodynamics and pharmacokinetics
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Focus on concepts such as drug-receptor interactions, dose-response relationships, and drug distribution and elimination
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Complete practice problems or quizzes on these concepts to assess your understanding
Review Foye's Principles of Medicinal Chemistry
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Refresh your knowledge on general and medicinal chemistry concepts and principles.
View
Foye's Principles of Medicinal Chemistry
on Amazon
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Read the chapter on Lead Discovery and Optimization
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Take notes on the key concepts and definitions
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Complete the practice problems at the end of the chapter
Five other activities
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Join a study group to discuss lead optimization concepts
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Engage with your peers to clarify concepts, share insights, and enhance your understanding of lead optimization.
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Lead Optimization
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Find a study group or create your own with classmates or colleagues
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Meet regularly to discuss course concepts, case studies, and practice problems
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Take turns leading discussions and presenting your findings
Practice lead selection and optimization calculations
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Reinforce your understanding of the quantitative aspects of lead selection and optimization.
Browse courses on
Lead Selection
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Find a set of practice problems online or in a textbook
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Solve the problems using the formulas and concepts covered in the course
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Check your answers against the provided solutions
Create a presentation on a lead optimization case study
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Apply your knowledge of lead optimization to a real-world example and develop your communication skills.
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Lead Optimization
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Choose a lead optimization case study from a scientific journal or industry report
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Research the background and methodology of the case study
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Create a presentation that summarizes the key findings and conclusions of the case study
Mentor a junior student or colleague in lead optimization
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Solidify your understanding of lead optimization by teaching and guiding others.
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Lead Optimization
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-
Identify a junior student or colleague who is interested in learning about lead optimization
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Meet regularly to discuss course concepts, answer questions, and provide guidance on projects
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Provide feedback and support to help them achieve their learning goals
Create a comprehensive study guide for the course
Show steps
Enhance your understanding and retention of course material by organizing and summarizing key concepts in a comprehensive study guide.
Show steps
-
Compile notes, assignments, quizzes, and exams from the course
-
Organize the material into logical sections and subsections
-
Summarize key concepts, definitions, and formulas
Review organic chemistry functional groups
Show steps
Ensure you have a strong foundation in organic chemistry concepts, especially functional groups, to support your understanding of lead optimization.
Browse courses on
Organic Chemistry
Show steps
- Review your notes or a textbook on organic chemistry functional groups
- Practice identifying functional groups in molecules
- Complete practice problems or quizzes on functional group chemistry
Review basic concepts in pharmacodynamics and pharmacokinetics
Show steps
Strengthen your understanding of the basic principles of pharmacodynamics and pharmacokinetics to enhance your comprehension of lead optimization.
Browse courses on
pharmacodynamics
Show steps
- Review your notes or a textbook on pharmacodynamics and pharmacokinetics
- Focus on concepts such as drug-receptor interactions, dose-response relationships, and drug distribution and elimination
- Complete practice problems or quizzes on these concepts to assess your understanding
Review Foye's Principles of Medicinal Chemistry
Show steps
Refresh your knowledge on general and medicinal chemistry concepts and principles.
View
Foye's Principles of Medicinal Chemistry
on Amazon
Show steps
- Read the chapter on Lead Discovery and Optimization
- Take notes on the key concepts and definitions
- Complete the practice problems at the end of the chapter
Join a study group to discuss lead optimization concepts
Show steps
Engage with your peers to clarify concepts, share insights, and enhance your understanding of lead optimization.
Browse courses on
Lead Optimization
Show steps
- Find a study group or create your own with classmates or colleagues
- Meet regularly to discuss course concepts, case studies, and practice problems
- Take turns leading discussions and presenting your findings
Practice lead selection and optimization calculations
Show steps
Reinforce your understanding of the quantitative aspects of lead selection and optimization.
Browse courses on
Lead Selection
Show steps
- Find a set of practice problems online or in a textbook
- Solve the problems using the formulas and concepts covered in the course
- Check your answers against the provided solutions
Create a presentation on a lead optimization case study
Show steps
Apply your knowledge of lead optimization to a real-world example and develop your communication skills.
Browse courses on
Lead Optimization
Show steps
- Choose a lead optimization case study from a scientific journal or industry report
- Research the background and methodology of the case study
- Create a presentation that summarizes the key findings and conclusions of the case study
Mentor a junior student or colleague in lead optimization
Show steps
Solidify your understanding of lead optimization by teaching and guiding others.
Browse courses on
Lead Optimization
Show steps
- Identify a junior student or colleague who is interested in learning about lead optimization
- Meet regularly to discuss course concepts, answer questions, and provide guidance on projects
- Provide feedback and support to help them achieve their learning goals
Create a comprehensive study guide for the course
Show steps
Enhance your understanding and retention of course material by organizing and summarizing key concepts in a comprehensive study guide.
Show steps
- Compile notes, assignments, quizzes, and exams from the course
- Organize the material into logical sections and subsections
- Summarize key concepts, definitions, and formulas
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