How Fast Does a Drug Work?
- Terry's Desk
- Jul 22
- 3 min read
Updated: Aug 11
Kenakin’s latest lecture delivers exclusive, real-world insight designed to equip you to move beyond surface-level affinity data and make faster, more confident decisions in your drug discovery pipeline.
In this session, you’ll gain:
✅ A practical framework for understanding when a drug’s rate of binding onset and offset matter most for in vivo success, and when static equilibrium affinity won’t tell the full story
✅ Guidance on interpreting kinetic binding experiments that enable operational clarity and avoid wasted effort
✅ The ability to reduce cycle times by recognizing when your data truly reflects equilibrium—and when it doesn’t
This is practical kinetic expertise—crafted to help drug hunters reduce wasted effort and move faster from data to decision.
Why Faster, Smarter Decisions Require More Than Kd
In drug discovery today, the clock is always ticking. Your pipeline depends on early, well-informed decisions that move promising candidates forward while de-prioritizing those unlikely to succeed.
Yet most discovery teams still rely on classic affinity metrics alone, often overlooking how kinetic profiles (onset and offset rates) fundamentally shape how a drug behaves in vivo.
Two compounds can show identical affinities on paper, but their biological outcomes can differ dramatically if their kinetic profiles diverge.
Every day spent misunderstanding what your assays are truly showing you can lead to costly missteps—wasted SAR iterations, false positives, and slower time-to-milestone.
Kenakin’s kinetic insights help you translate assay readouts into actionable knowledge that keeps your programs focused and moving efficiently toward clinical relevance.
Why the Myth of “Potency = Affinity” Could Be Slowing Your Pipeline
Many workflows still operate on the assumption that equilibrium potency (Kd) alone is sufficient to predict in vivo efficacy.
But as Kenakin shows in this lecture, the reality is more nuanced, and mastering drug binding kinetics is essential for pipeline efficiency:
How fast a ligand binds (k₁) and how long it stays bound (k₂) can alter therapeutic profiles dramatically, even if two candidates share the same affinity at equilibrium.
Competitive conditions—such as the presence of endogenous ligands—change kinetic behavior, and ignoring this can lead to wrong prioritization decisions.
Kinetic measurements reveal hidden liabilities or advantages that static affinity numbers cannot.
Understanding these dynamics empowers drug hunters to separate what matters from what misleads, cutting through noise to focus only on compounds with genuine in vivo promise.
Kinetics Reveal What Static Numbers Can’t
If your workflow stops at “potency = Kd,” you’re missing a critical layer of actionable insight.
Kenakin’s lecture guides you through key questions that should shape your decision-making process:
Are you measuring equilibrium, or could early-time-point artifacts be skewing your interpretation?
How do competing ligands slow or alter binding rates, and what does this tell you about real-world pharmacology?
When does onset rate dictate therapeutic onset, and when does offset rate predict duration?
These aren’t theoretical questions—they directly impact your ability to advance the best candidates faster, while eliminating wasted cycles on compounds that look good on paper but won’t deliver.
Don’t Let Outdated Models Slow Your Next Program
The analytical tools that shaped traditional affinity assays were built for simpler systems. Without appreciating their limitations, it’s easy to misinterpret key kinetic signals that matter for decision-making in modern drug discovery.
Missteps at this level can delay optimization, generate unnecessary SAR work, or cause your team to miss subtle but critical liabilities—all of which slow your pipeline’s forward momentum.
Dr. Kenakin gives you clear, practical guidance on when to look deeper and how to extract meaningful, operational insight from your kinetic data.
Reach key milestones sooner, with fewer false starts.
You’ll gain clarity that accelerates your path from discovery to clinic:
Know when your assays truly reflect binding equilibrium
Interpret competition experiments with confidence
Recognize how kinetic rate constants can reveal hidden liabilities, or identify true best-in-class candidates faster
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