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Erland Stevens
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.
Read more
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.
Read more
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
Register for this course and see more details by visiting:
OpenCourser.com/course/fa3eff/lead
Traffic lights
Traffic lights
Read about what's good
what should give you pause and
possible dealbreakers
Explores lead selection and lead optimization which are core processes in drug discovery
Introduces students to the principles of lead selection and lead optimization
Addresses various methods for lead optimization, including structural changes for improved efficacy, PK properties, and toxicity reduction
Requires familiarity with pharmacodynamics, drug activity, pharmacokinetics, preclinical safety, algebraic expressions, and organic molecules
Provides flexibility in course completion with options for hourly or extended study
Taught by Erland Stevens
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Reviews summary
Drug lead discovery & optimization
According to students, this course offers a largely positive experience, particularly for professionals in medicinal chemistry or drug discovery. Learners praise its ability to bridge theoretical knowledge with practical application, noting the crystal-clear instructor explanations and insightful modules on efficacy, PK, and safety. The course's well-structured content and manageable pace are frequently highlighted as strengths. While some students wished for more interactive exercises and deeper dives for advanced specialists, recent reviews indicate the course has undergone significant updates, adding practical examples and enhanced interactive elements, demonstrating the instructors' responsiveness to feedback.
Well-organized content delivered at an accessible pace.
"I spent about 1-2 hours a day and finished it in just under two weeks, which was perfect for my schedule."
"The modules on lead optimization, especially regarding PK properties, were incredibly insightful."
"A solid introduction to lead discovery and optimization for professionals."
Instructors actively update content based on student feedback.
"I took this course two years ago and retook it recently. They've really enhanced the interactive elements and added more practical examples..."
"The updated content on modern lead optimization techniques is a huge plus. This demonstrates clear improvement from the instructors."
Bridges theory to real-world drug discovery processes.
"This course was exactly what I needed to bridge the gap between theoretical knowledge and practical application in drug discovery."
"The instructor's explanations were crystal clear, making complex topics digestible."
"It definitely helped me understand the industry better and how concepts apply in real scenarios."
Could benefit from more interactive exercises and discussion opportunities.
"While the videos were excellent, I wished there were more interactive exercises beyond the basic assessments."
"It feels more like a series of lectures than an interactive course. There wasn't much opportunity for discussion or asking questions."
"The readings were helpful, but sometimes not enough to grasp everything without external resources."
Best suited for learners with strong prerequisite science background.
"Some parts felt a bit rushed, especially if you don't have a very strong background in the prerequisite organic chemistry."
"I struggled with some of the more advanced concepts, finding them not deep enough for a specialist."
"Good overview for someone starting out in this area or needing a refresher, but not for cutting-edge specialists."
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 Discovery & Optimization for Efficacy, PK, & Safety with these
activities:
Review Medicinal Chemistry Background
Show steps
Reviewing Medicinal Chemistry concepts provides a foundation for understanding lead selection and optimization.
Browse courses on
Medicinal Chemistry
Show steps
-
Review lecture notes and textbooks on Medicinal Chemistry.
-
Solve practice problems related to Medicinal Chemistry concepts.
-
Attend review sessions or workshops on Medicinal Chemistry.
Explore Lead Optimization Software Tutorials
Show steps
Learning specialized software enhances the ability to perform lead optimization tasks more efficiently.
Show steps
-
Identify software commonly used in lead optimization, such as ChemDraw or Schrödinger Suite.
-
Access online tutorials or workshops that provide guidance on using the software.
-
Follow the tutorials and practice using the software for lead optimization tasks.
Participate in a study group to discuss lead selection and optimization
Show steps
Participating in a study group will provide an opportunity to discuss the course material with other students and reinforce your understanding.
Browse courses on
Lead Selection
Show steps
-
Find a study group or form one with other students
-
Meet regularly to discuss the course material
-
Work together on practice problems and case studies
Eight other activities
Expand to see all activities and additional details
Show all 11 activities
Compile Lead Optimization Resources
Show steps
Gathering resources on lead optimization techniques enhances understanding and provides a reference point for future use.
Show steps
-
Search for articles, books, and online resources related to lead optimization.
-
Organize resources into a comprehensive collection.
-
Review the collected resources to gain insights into different lead optimization approaches.
Use online tutorials to learn about lead optimization techniques
Show steps
Following tutorials on lead optimization techniques will supplement the course material and provide additional practice.
Show steps
-
Find online tutorials on lead optimization techniques
-
Watch the tutorials and take notes
-
Complete any practice exercises associated with the tutorials
Practice Lead Selection Exercises
Show steps
Engaging in lead selection exercises reinforces the criteria and methods used in the course.
Show steps
-
Identify and analyze datasets containing potential lead compounds.
-
Apply lead selection criteria to evaluate compounds and prioritize leads.
-
Discuss and compare lead selection strategies with peers or mentors.
Lead Optimization Study Group
Show steps
Engaging in peer discussions deepens understanding and facilitates knowledge exchange in lead optimization.
Show steps
-
Form a study group with peers who share an interest in lead optimization.
-
Meet regularly to discuss course materials, research articles, and case studies.
-
Collaborate on lead optimization projects and provide peer feedback.
Attend Industry Conference on Lead Optimization
Show steps
Networking at conferences allows for exposure to cutting-edge research and industry trends in lead optimization.
Show steps
-
Identify and register for an industry conference focused on lead optimization.
-
Attend keynote speeches, research presentations, and panel discussions.
-
Network with researchers, industry professionals, and potential collaborators.
-
Gather information on new technologies and advancements in lead optimization.
Practice lead selection and optimization problems
Show steps
Practicing lead selection and optimization problems will help solidify the concepts learned in the course.
Browse courses on
Lead Selection
Show steps
-
Find practice problems on lead selection and optimization
-
Solve the practice problems
-
Review your answers and identify areas for improvement
Attend Lead Optimization Workshop
Show steps
Attending a workshop provides practical insights and networking opportunities to enhance lead optimization knowledge.
Show steps
-
Research and identify a relevant lead optimization workshop.
-
Register for the workshop and attend all sessions.
-
Participate actively in discussions and hands-on exercises.
-
Connect with experts and professionals in the field of lead optimization.
Develop Lead Optimization Strategy
Show steps
Creating a lead optimization strategy provides hands-on experience in applying the concepts learned in the course.
Show steps
-
Identify a target molecule and research its properties.
-
Design and synthesize potential lead compounds.
-
Evaluate lead compounds using appropriate assays and techniques.
-
Develop a comprehensive lead optimization strategy based on the evaluation results.
Review Medicinal Chemistry Background
Show steps
Reviewing Medicinal Chemistry concepts provides a foundation for understanding lead selection and optimization.
Browse courses on
Medicinal Chemistry
Show steps
Show steps
Show steps
- Review lecture notes and textbooks on Medicinal Chemistry.
- Solve practice problems related to Medicinal Chemistry concepts.
- Attend review sessions or workshops on Medicinal Chemistry.
Explore Lead Optimization Software Tutorials
Show steps
Learning specialized software enhances the ability to perform lead optimization tasks more efficiently.
Show steps
Show steps
Show steps
- Identify software commonly used in lead optimization, such as ChemDraw or Schrödinger Suite.
- Access online tutorials or workshops that provide guidance on using the software.
- Follow the tutorials and practice using the software for lead optimization tasks.
Participate in a study group to discuss lead selection and optimization
Show steps
Participating in a study group will provide an opportunity to discuss the course material with other students and reinforce your understanding.
Browse courses on
Lead Selection
Show steps
Show steps
Show steps
- Find a study group or form one with other students
- Meet regularly to discuss the course material
- Work together on practice problems and case studies
Eight other activities
Expand to see all activities and additional details
Show all 11 activities
Compile Lead Optimization Resources
Show steps
Gathering resources on lead optimization techniques enhances understanding and provides a reference point for future use.
Show steps
Show steps
Show steps
- Search for articles, books, and online resources related to lead optimization.
- Organize resources into a comprehensive collection.
- Review the collected resources to gain insights into different lead optimization approaches.
Use online tutorials to learn about lead optimization techniques
Show steps
Following tutorials on lead optimization techniques will supplement the course material and provide additional practice.
Show steps
Show steps
Show steps
- Find online tutorials on lead optimization techniques
- Watch the tutorials and take notes
- Complete any practice exercises associated with the tutorials
Practice Lead Selection Exercises
Show steps
Engaging in lead selection exercises reinforces the criteria and methods used in the course.
Show steps
Show steps
Show steps
- Identify and analyze datasets containing potential lead compounds.
- Apply lead selection criteria to evaluate compounds and prioritize leads.
- Discuss and compare lead selection strategies with peers or mentors.
Lead Optimization Study Group
Show steps
Engaging in peer discussions deepens understanding and facilitates knowledge exchange in lead optimization.
Show steps
Show steps
Show steps
- Form a study group with peers who share an interest in lead optimization.
- Meet regularly to discuss course materials, research articles, and case studies.
- Collaborate on lead optimization projects and provide peer feedback.
Attend Industry Conference on Lead Optimization
Show steps
Networking at conferences allows for exposure to cutting-edge research and industry trends in lead optimization.
Show steps
Show steps
Show steps
- Identify and register for an industry conference focused on lead optimization.
- Attend keynote speeches, research presentations, and panel discussions.
- Network with researchers, industry professionals, and potential collaborators.
- Gather information on new technologies and advancements in lead optimization.
Practice lead selection and optimization problems
Show steps
Practicing lead selection and optimization problems will help solidify the concepts learned in the course.
Browse courses on
Lead Selection
Show steps
Show steps
Show steps
- Find practice problems on lead selection and optimization
- Solve the practice problems
- Review your answers and identify areas for improvement
Attend Lead Optimization Workshop
Show steps
Attending a workshop provides practical insights and networking opportunities to enhance lead optimization knowledge.
Show steps
Show steps
Show steps
- Research and identify a relevant lead optimization workshop.
- Register for the workshop and attend all sessions.
- Participate actively in discussions and hands-on exercises.
- Connect with experts and professionals in the field of lead optimization.
Develop Lead Optimization Strategy
Show steps
Creating a lead optimization strategy provides hands-on experience in applying the concepts learned in the course.
Show steps
Show steps
Show steps
- Identify a target molecule and research its properties.
- Design and synthesize potential lead compounds.
- Evaluate lead compounds using appropriate assays and techniques.
- Develop a comprehensive lead optimization strategy based on the evaluation results.
Career center
Learners who complete Lead Discovery & Optimization for Efficacy, PK, & Safety will develop knowledge and skills
that may be useful to these careers:
Medicinal Chemist
Medicinal Chemist
Design and synthesize organic molecules to treat various diseases. Lead Discovery & Optimization for Efficacy, PK, & Safety can provide you with a strong foundation. The course covers methods for discovering and optimizing leads with the end goal of advancing a compound into the clinic. This knowledge is essential for medicinal chemists, who need to understand the principles of drug design and optimization in order to develop new and effective treatments.
Pharmacologist
Pharmacologist
Study the effects of drugs on living organisms. Lead Discovery & Optimization for Efficacy, PK, & Safety can help you build a foundation. The course covers the principles of drug action, including how drugs interact with receptors and other targets, and how they are transported and metabolized in the body.
Toxicologist
Toxicologist
Assess the safety of drugs and other chemicals. Lead Discovery & Optimization for Efficacy, PK, & Safety can be useful. The course covers methods for evaluating the toxicity of compounds, including both in vitro and in vivo studies.
Drug Safety Scientist
Drug Safety Scientist
Ensure the safety and efficacy of drugs throughout their development and lifecycle. Lead Discovery & Optimization for Efficacy, PK, & Safety can be useful. The course covers the principles of drug safety, including how to design and conduct clinical trials, and how to interpret and evaluate safety data.
Clinical Research Associate
Clinical Research Associate
Manage clinical trials and ensure that they are conducted in accordance with good clinical practice (GCP) guidelines. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of clinical trial design and conduct, as well as the regulatory requirements for clinical trials.
Biostatistician
Biostatistician
Design and analyze clinical trials and other biomedical studies. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of biostatistics, including how to design and conduct clinical trials, and how to analyze and interpret clinical data.
Data Scientist
Data Scientist
Collect, analyze, and interpret data to solve business problems. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of data science, including how to collect, clean, and analyze data, and how to interpret and communicate results.
Project Manager
Project Manager
Plan, manage, and execute projects. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of project management, including how to plan and scope projects, how to manage resources, and how to track and evaluate progress.
Business Analyst
Business Analyst
Analyze business processes and develop solutions to improve efficiency and effectiveness. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of business analysis, including how to gather and analyze business requirements, and how to develop and implement solutions.
Quality Assurance (QA) Analyst
Quality Assurance (QA) Analyst
Ensure that products and services meet quality standards. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of quality assurance, including how to develop and implement quality systems, and how to audit and assess compliance.
Regulatory Affairs Specialist
Regulatory Affairs Specialist
Ensure that drugs and other medical products comply with regulatory requirements. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of regulatory affairs, including how to develop and submit regulatory filings, and how to interpret and comply with regulatory decisions.
Healthcare Consultant
Healthcare Consultant
Provide consulting services to healthcare organizations. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of healthcare consulting, including how to assess healthcare needs, and how to develop and implement solutions.
Patent Attorney
Patent Attorney
Draft and prosecute patents for inventions. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of patent law, including how to search for and analyze prior art, and how to draft and file patent applications.
Science Writer
Science Writer
Write and edit scientific articles, reports, and other documents. Lead Discovery & Optimization for Efficacy, PK, & Safety may be useful. The course covers the principles of scientific writing, including how to structure and organize scientific documents, and how to write clearly and concisely.
Teacher
Teacher
Teach science courses at the high school or college level. Lead Discovery & Optimization for Efficacy, PK, & Safety can be useful. The course covers the principles of science education, including how to develop and deliver effective lessons, and how to assess student learning.
For more career information including salaries, visit:
OpenCourser.com/course/fa3eff/lead
Reading list
We've selected 14 books
that we think will supplement your
learning. Use these to
develop background knowledge, enrich your coursework, and gain a
deeper understanding of the topics covered in
Lead Discovery & Optimization for Efficacy, PK, & Safety.
This classic textbook provides a comprehensive overview of medicinal chemistry, covering topics such as drug discovery, pharmacokinetics, and drug metabolism. It valuable resource for students and researchers in the field.
This textbook provides a comprehensive overview of pharmacology, covering topics such as drug receptors, drug actions, and drug metabolism. It valuable resource for students and researchers in the field.
Save
Provides an overview of pharmacokinetics and pharmacodynamics, including the principles of drug absorption, distribution, metabolism, and excretion.
Save
This textbook provides a comprehensive overview of medicinal chemistry, covering topics such as drug discovery, drug design, and drug metabolism. It valuable resource for students and researchers in the field.
This textbook provides a comprehensive overview of pharmaceutical biotechnology, covering topics such as gene expression, protein production, and drug delivery. It valuable resource for students and researchers in the field.
Provides a comprehensive overview of current drug discovery technologies, covering topics such as high-throughput screening, combinatorial chemistry, and molecular modeling. It valuable resource for students and researchers in the field.
Provides a comprehensive overview of organic chemistry, including the principles of reaction mechanisms and synthesis.
Save
Provides a historical perspective on drug discovery, covering topics such as the history of drug discovery, the development of new drugs, and the challenges of drug discovery. It valuable resource for students and researchers in the field.
Provides an introduction to medicinal chemistry, covering topics such as drug discovery, drug design, and drug development. It valuable resource for students and researchers in the field.
Provides an overview of drug delivery and targeting, including the principles of drug absorption, distribution, and metabolism.
Save
Provides a comprehensive overview of biochemistry, covering topics such as the structure of proteins, the function of enzymes, and the metabolism of carbohydrates. It valuable resource for students and researchers in the field.
Provides a comprehensive overview of organic chemistry, covering topics such as the structure of organic molecules, the reactions of organic molecules, and the synthesis of organic molecules. It valuable resource for students and researchers in the field.
Save
Provides a comprehensive overview of general, organic, and biochemistry, covering topics such as the structure of matter, the properties of matter, and the reactions of matter. It valuable resource for students and researchers in the field.
Provides a comprehensive overview of the medicinal chemistry of anticancer drugs, including the principles of drug design and synthesis.
For more information about how these books relate to this course, visit:
OpenCourser.com/course/fa3eff/lead
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