Pharmacological Target Engagement, Validation, and In Vivo Translation

The most prevalent cause of new drug failure is lack of demonstration of target engagement and therapeutic effect. Students and early-career professionals need to acquire a basic understanding of how target engagement and validation “fits” into early drug development, techniques used, and how this allows for more complex MOA studies.

Drugs interact with living breathing physiology and can present different profiles of activity in organs of varying sensitivity; pharmacology furnishes scales of activity to turn 'descriptive data' (what we see in one experiment) to 'predictive data' (what will be seen under all conditions in vivo).

Who Should Attend
Biologists involved in drug discovery
Medicinal chemists
Pharmacology students
Academic pharmacologists

Course Benefits
Gain new insights into state-of-the-art ideas on drug targets and their association with therapeutic opportunities
Learn new tools to quantitatively assess molecular effects on drug targets
Learn how parameters from these methods can predict activity in all systems
Define new vistas around old targets to better define chemical targets for receptors

Course Topics
Systems- vs. target-based research
Target validation: eg.CCR5 HIV
Role of Knock outs
Drugging Targets, HTS, virtual screening
Drugging orphans (constitutive screening)
New chemical entities (esp. allosteric modulators)
50% efficacy failures: reasons why and ways forward
Target vs. pathway validation and biased signaling
Demonstrating target engagement in vitro
Demonstrating target engagement in vivo
Linking target engagement with therapeutic effect

Key:

Complete
Failed
Available
Locked
Target Identification, Validation and Drugability
Target Identification, Validation and Drugability
Open to view video.
Open to view video. This lecture discusses systems- vs target-based discovery, choosing drug targets, validating drug targets and 'drugging' targets (i.e. finding small drug like molecules that can modify target behavior for therapeutic advantage).
Target Identification, Validation and Drugability Quiz
6 Questions  |  Unlimited attempts  |  4/6 points to pass
6 Questions  |  Unlimited attempts  |  4/6 points to pass
Quiz 1 Discussion
Open to view video.
Open to view video.
In Vitro Demonstration of Target Engagement
In Vitro Demonstration of Target Engagement
Open to view video.
Open to view video. This lecture completes target 'drugability' (virtual, constitutive screening) and then discusses methods to verify that a molecule engages the target in vitro.
In Vitro Demonstration of Target Engagement Quiz
5 Questions  |  Unlimited attempts  |  4/5 points to pass
5 Questions  |  Unlimited attempts  |  4/5 points to pass
Quiz 2 Discussion
Open to view video.
Open to view video.
In Vivo Demonstration of Target Engagement / Candidate Profiling
In Vivo Demonstration of Target Engagement / Candidate Profiling
Open to view video.
Open to view video. This lecture extends target engagement to in vivo conditions and also discusses the detailed characterization of candidate properties to better predict therapeutic utility.
In Vivo Demonstration of Target Engagement / Candidate Profiling Quiz
6 Questions  |  Unlimited attempts  |  4/6 points to pass
6 Questions  |  Unlimited attempts  |  4/6 points to pass
Quiz 3 Discussion
Open to view video.
Open to view video.
Evaluation and Certificate
Pharmacological Target Engagement, Validation, and In Vivo Translation Participant Evaluation
6 Questions
6 Questions Thank you for participation in the SLAS Pharmacological Target Engagement, Validation, and In Vivo Translation course. Your candid feedback on this new program is very important. Please take a few minutes to help us make our micro-credential program valuable for all. The topics for the Pharmacological Target Engagement, Validation, and In Vivo Translation course were: Systems- vs. target-based research Target validation: eg.CCR5 HIV Role of Knock outs Drugging Targets, HTS, virtual screening Drugging orphans (constitutive screening) New chemical entities (esp. allosteric modulators) 50% efficacy failures: reasons why and ways forward Target vs. pathway validation and biased signaling Demonstrating target engagement in vitro Demonstrating target engagement in vivo Linking target engagement with therapeutic effect
Pharmacological Target Engagement, Validation, and In Vivo Translation Certificate
Live Viewing: No credits available and certificate available
Live Viewing: No credits available and certificate available