Enzymlogic is a contract research organization that represents scientific excellence in binding kinetics analysis for small molecule drug discovery programmes.
Enzymlogic’s pioneering approach in Binding Kinetics and Kinetic Selectivity assays enables faster and cost-effective kinetic profiling, lead optimization, Structure-Activity Relationship (SAR) and Structure-Kinetic Relationship (SKR) campaigns. Our unique methodology provides predictive tools that deliver physiologically relevant insights earlier in the drug discovery process.
Our services give you the data you need to make smart decisions sooner and help you to optimize drugs with higher development potential and reduced risk of failure:
• Perform kinetic selectivity to find new therapeutic uses and explore the conformational space of the targets.
• Perform a kinetic profiling to get access to more diverse chemical space.
• Perform a kinetic profiling to identify novel drug-target interactions not captured by IC50 profiling.
• Generate SAR and SKR for reversible and irreversible compounds.
• Determine kinetic selectivity to assess physiologically relevant off-target risks.
• Determine accurate kinetic values to identify slow binding compounds or compounds that induce conformational changes.
We offer expertise and services in the area of small molecule interaction analysis in order to:
• Improve decision-making
• Drive chemical diversity and promote IP
• Enhance drug’s clinical efficacy
• Improve drug safety
• Help you to identify new therapeutic uses
The efficacy of target inhibition depends on the rate constant of both the association and dissociation of a drug molecule to and from the target. The onset of the drug action is influenced by the association rate: the faster a drug binds to the target, the faster the inactivation will occur. Conversely, the duration of drug action is dependent of the dissociation rate: the longer the duration of binding, the longer the pharmacodynamic effect.
Compounds with identical affinity for a given target can exhibit very different kinetic profiles which may result in the differentiation of the clinical responses.
Enzymlogic determines the kinetic binding profile of your compounds to your kinase of interest to provide competitive advantage when it comes to identifying and improving novel therapeutic agents.
We use a fast and simple method to measure the affinity constant (Kd), the association rate constant (kon), the dissociation rate constant (koff) and the residence time of your compounds.
Features & benefits:
Evaluating the dynamic behaviour of your drugs
Dynamism and specificity: a complete picture of the in vivo behavior of your drugs
Selectivity is highly dynamic in human body and evolves over the course of treatment as a function of the temporal binding between the drug and the main and secondary targets.
The early assessment of kinetic selectivity is crucial to select drugs with the suitable safety profiles.
A drug showing long residence time when bound to its main target and short residence times for secondary targets exhibits temporal target selectivity. Safety and tolerability will considerably improve if the intrinsic toxicity of the drug is minimal. In contrast, a drug that display a long residence time against a secondary toxicity-mediating target will result in safety issues.
Enzymlogic determines the residence time of your compounds when bound to the kinase panel of your choice to evaluate their pharmacological behavior.
Features & benefits:
Enzymlogic provides its expertise in enzymology and drug discovery to develop customized biochemical assays aimed at:
We apply mechanistic principles to assay design:
We use the most suitable detection methods for a given target and screening needs:
Our services encompass assay development as well as scientific advice and the establishment of close relationships with our customers to suit their needs.
Biochemistry & Molecular Biology Services
Enzymlogic has not received any endorsements.