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It can redirect chemistry strategy, distort translational assumptions, and conceal liabilities that emerge Integrating Chemistry and Kinetics Early Biological activity alone does not define a viable series. Chemical tractability, early safety screens (e.g., hERG), ADME properties, and residence time often determine Strategic discipline means: Screening liabilities early Integrating chemistry insights immediately Avoiding

The math checks out.

Terry Kenakin walks through the core early assays that protect your chemistry, budget, and timeline.

robust toxicology In Silico Toxic Signals Advancements in computational screening enable teams to avoid chemotypes acknowledges the increasing utility of in silico alerts in early decision-making, arming medicinal chemists

and tell us what you need ➤ Terry’s Corner—Basic Pharmacokinetics Pharmacokinetics isn’t a late-stage checkbox—it

Too often, fundamentals are undervalued: in vitro assays are treated as routine checkboxes, and ADME demonstrates how CYP450 liabilities were mitigated without compromising efficacy This independence empowers chemists PK without sacrificing target engagement Optimization should be modular, not monolithic Medicinal chemistry points Early property mapping accelerates the design–test–learn cycle Drug discovery is faster when chemistry Designed for pharmacologists, medicinal chemists, and discovery leaders who refuse to rely on assumptions

The moment when clarity is cheapest, alignment is easiest, and impact is highest .

When priorities are explicit, execution accelerates because teams no longer need constant alignment checks

Intellectual property is not a checkbox.

When teams adopt structured decision cycles, consistent narrative checkpoints, and predictable timeline repeatable communication rhythm: internal alignment weekly cross-functional integration biweekly investor check-ins

Kenakin outlines a pragmatic checklist for producing reliable orthosteric binding measurements: Cell

✅ FDA approval is not a documentation checkpoint. It’s a strategic filter. However, that sequence conceals a significant flaw; it treats FDA approval as the  final checkpoint , But approval is not a checkpoint. ✅ It’s a strategic mirror.

conformations, and non-specific interactions introduce noise at precisely the stage where medicinal chemistry SCRAs—although often known for their undesired toxicological profile—offer a chemically diverse set of Furthermore, image-based data provide an additional check against off-target cytotoxicity or morphological Ki values were then calculated using the Cheng–Prusoff equation, with CELT-331 parameters fully reported European Journal of Medicinal Chemistry, 46(2), 547–555.

GPCR Podcast: Chemical Probes for GPCR Imaging with Dr. His work shows why chemical design can outperform antibodies and how rigorous assay validation bridges chemistry and biology effectively.

But behind the polite nods, your audience is checking out.

Kenakin  drew a sharp contrast between chemically reactive irreversible inhibitors and pseudo-irreversible Ranking Partial Agonists Without Losing Meaning Chemists want a single number. These GPCR pharmacology insights are essential for directing chemistry toward the property that actually

automated microscopy, multiplexed imaging, and computational analysis to evaluate cellular responses under chemical

Episode #177 The Experiment That Was Never Meant to Succeed When David Hodson’s lab teamed up with chemist Hodson: physiology, disease context, and imaging logic JB: chemistry, ligand engineering, mechanistic Collaboration, Chemistry, and the Pivot That Changed the Project Goal:  Develop a photo-switchable GPCR

Enter a long-term collaboration with chemist Dr.

Here, the Schild plot becomes a diagnostic tool  rather than a checkbox test: Slopes >1  often mean incomplete

David Hodson walks through how his team uses fluorescence tools and chemically engineered ligands to listen Researchers navigating complex datasets, balancing innovation with assay rigor, or working across chemistry–pharmacology–physiology

Here are three questions to help you check in with yourself: 1️⃣ Do you delay or dilute decisions while

GPCRs demanded something different: the integration of modeling, medicinal chemistry, and pharmacology Predictions from modeling inform chemistry. Chemistry fuels assays. Chemists understand why certain molecules are worth the effort to synthesize. Medicinal chemists can synthesize molecules, but must choose carefully from infinite possibilities. in mind, chemistry connected to assays, and assay data cycling back to refine predictions.

Modern real-time assays can deliver these insights earlier, faster, and cheaper than most teams assume Programs aren’t killed because of bad ideas—they’re paused when the chemical matter isn’t compelling

assays in drug discovery October 2024 | Biologics US 2024   October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry

Collaborating with chemists, biologists, and pharmacologists not only made his predictions more useful Today, his group includes around ten computational chemists and one in-house medicinal chemist. This is when the synthetic expertise of the chemist becomes essential. Carlsson notes that it’s easier to find pharmacologists to run assays than it is to persuade chemists

It was the result of chemistry, collaboration, and relentless effort until the signal finally confirmed The Chemistry That Almost Didn’t Work Designing pH-sensitive rare-earth complexes was not an obvious The chemistry involved is notoriously complex. Solubility poses significant challenges. The chemistry originated from Parker’s lab. What started as a chemistry problem has evolved into a discovery platform.

cell function Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry

GPCR-targeted drug development, incorporating machine learning, innovative biophysical methods, and medicinal chemistry The full agenda is now available; check it here ! Discovery on Target October 2024 | Biologics US 2024   October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry function NEW Protein Biochemist/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry (5-HT2A) GPCRs in Oncology and Immunology The power of many: Multilevel targeting of representative chemokine

This partnership aims to bring advanced chemical probe strategies to the forefront.