It’s important to lay strong foundations for successful drug discovery at this first stage of the process. Our integrated target identification and validation platform combines AI with expert insights, and rigorous lab validation to guide targets through robust evaluation, ready for hit discovery.
Validated, high-quality hits, delivered through integrated technologies and expert collaboration, give you a confident starting point for faster drug discovery.
Turning promising leads into clinical candidates with speed, precision, and the scientific expertise to generate high-quality data and deliver real patient impact.
Delivering integrated, modality-agnostic drug discovery to tackle complex biology, accelerate development, and advance innovative therapies with confidence.
Advancing next-generation ADCs through payload-focused design, integrated expertise, and collaborative innovation to deliver safer, more selective therapies.
Driving biologics innovation through integrated design, structural biology, and multidisciplinary expertise to accelerate next-generation therapies from concept to clinic.
Combining deep therapeutic expertise with translational insight to design strategies, reduce risk, and accelerate discovery programs toward clinical success.
Accelerating oncology drug discovery through integrated expertise, innovative modalities, and translational insight to deliver candidates with real clinical impact.
Driving immunology and inflammation drug discovery through tailored assays, translational models, and integrated expertise for faster clinical success.
Advancing CNS drug discovery through integrated models, translational biomarkers, and multidisciplinary expertise to overcome complexity and accelerate therapeutic innovation.
Designing and advancing differentiated small-molecule therapies for obesity and diabetes through integrated expertise, mechanistic insight, and translational strategies.
Inobrodib, an exciting, first-in-class oral anti-cancer drug in clinical development by CellCentric, was collaboratively designed, synthesised and supported on its pre-clinical journey by an integrated project team at Sygnature Discovery. Inobrodib is now showing promising results in Phase I and II trials for multiple myeloma and other cancer types.
It’s important to lay strong foundations for successful drug discovery at this first stage of the process. Our integrated target identification and validation platform combines AI with expert insights, and rigorous lab validation to guide targets through robust evaluation, ready for hit discovery.
Validated, high-quality hits, delivered through integrated technologies and expert collaboration, give you a confident starting point for faster drug discovery.
Turning promising leads into clinical candidates with speed, precision, and the scientific expertise to generate high-quality data and deliver real patient impact.
Delivering integrated, modality-agnostic drug discovery to tackle complex biology, accelerate development, and advance innovative therapies with confidence.
Advancing next-generation ADCs through payload-focused design, integrated expertise, and collaborative innovation to deliver safer, more selective therapies.
Driving biologics innovation through integrated design, structural biology, and multidisciplinary expertise to accelerate next-generation therapies from concept to clinic.
Combining deep therapeutic expertise with translational insight to design strategies, reduce risk, and accelerate discovery programs toward clinical success.
Accelerating oncology drug discovery through integrated expertise, innovative modalities, and translational insight to deliver candidates with real clinical impact.
Driving immunology and inflammation drug discovery through tailored assays, translational models, and integrated expertise for faster clinical success.
Advancing CNS drug discovery through integrated models, translational biomarkers, and multidisciplinary expertise to overcome complexity and accelerate therapeutic innovation.
Designing and advancing differentiated small-molecule therapies for obesity and diabetes through integrated expertise, mechanistic insight, and translational strategies.
Inobrodib, an exciting, first-in-class oral anti-cancer drug in clinical development by CellCentric, was collaboratively designed, synthesised and supported on its pre-clinical journey by an integrated project team at Sygnature Discovery. Inobrodib is now showing promising results in Phase I and II trials for multiple myeloma and other cancer types.
At Sygnature Discovery, we provide advanced tissue binding assays that reveal how drugs behave in the body. By focusing on unbound drug, the fraction that truly drives therapeutic effect, we deliver insights that improve pharmacokinetic predictions, guide dosing strategies, and accelerate candidate optimization.
Drug binding to plasma proteins and tissue components is reversible and shaped by properties such as lipophilicity and ionizable groups.
Differences in protein and lipid composition between plasma and tissue influence binding under physiological conditions. These interactions determine the volume of distribution (Vd), a key parameter for understanding drug disposition and systemic exposure.
Our assays quantify free drug concentrations across plasma, blood, and tissue compartments, giving you the clarity needed for smarter decisions. Our assays quantify free drug concentrations across plasma, blood, and tissue compartments, giving you the clarity needed for smarter decisions.
Our Tissue Binding Expertise
Plasma Protein Binding
Plasma proteins such as albumin and alpha 1 acid glycoprotein act as high-capacity carriers for drugs. Binding is typically reversible and non saturable at therapeutic concentrations. Acidic drugs often show strong plasma protein binding due to ionic inter actions with albumin. Understanding these dynamics is essential for predicting free drug concentration and pharmacokinetic behavior.
The blood-to-plasma partitioning (BPP) assay measures compound distribution between whole blood and plasma, reflecting affinity for cellular components like red blood cells (RBCs). Significant RBC binding can lower unbound plasma concentration, impacting pharmacokinetics and pharmacodynamics. For compounds that favor RBC partitioning, whole blood assays ensure accurate exposure assessment.
Tissue distribution and binding shape drug exposure and efficacy by modulating unbound drug available for target engagement. Basic compounds often exhibit high tissue affinity due to ionic interactions with negatively charged phospholipid head groups. For CNS targeted drugs, measuring fu, brain and calculating Kp, uu, the unbound brain-to-plasma ratio, are essential for assessing CNS penetration and pharmacodynamic relevance.
Cell and Media Binding
Non-specific binding during in vitro incubations can significantly reduce free drug concentration, confounding clearance (CLint) and potency data. Correcting for the fraction unbound in incubation (fu,inc) enables accurate comparisons across chemical series, supporting meaningful structure-activity relationship (SAR) decisions and improving translational relevance.
Bifunctional degraders bind and degrade proteins via ubiquitin ligase, despite breaking bRo5 rules. Translating in vitro DMPK data to in vivo performance remains a challenge. At Sygnature Discovery, we provide tailored assays and expertise to support projects involving these compounds. Read more in the poster.
Posters
Related Solutions
We bring together a dynamic blend of new talent and experienced pharmaceutical industry experts from a round the world, delivering excellence across every stage of discovery.
Integrated solid form and formulation strategies reduce risk, improve stability and solubility, and accelerate progression from candidate selection to clinic.
Validated in vivo models deliver clinically relevant data across therapeutic areas, accelerating confident decisions and reducing risk in drug development.
