As our understanding of conformational chemistry advances, we can explore a variety of strategies beyond cyclization to restrict the number of low-energy conformations accessible to ligands. These alternative approaches offer the potential to optimize binding affinity and enhance the overall pharmacological profile of ligands, facilitating more efficient drug design and discovery.
In this comprehensive review we highlighted the essential role of conformational drivers in drug design, exploring how molecular conformation influences key drug properties with real-world examples.
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Medicinal Chemistry,
Articles & Whitepapers,
ADME/DMPK
Diverse modalities are typically defined as those molecules which sit outside the rule of five characteristics for small molecules. These diverse modalities are often termed beyond the rule of five molecules, and include peptides, targeted protein degraders, oligonucleotides including ASOs, siRNAs and oligoconjugates, and proteins and monoclonal antibodies. Due to their characteristics, diverse modalities may require specialist assay design or analytical methods.
Cyprotex has expertise in assessing the ADME-Tox for various different types of diverse modalities to ensure robust data are generated.
Read our fact sheet to learn more about our services for assessing diverse modalities.
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Fact Sheets,
ADME/DMPK,
Toxicology & Safety,
Cyprotex
Pharmacological activity is often driven by free (unbound) concentration. Blood and plasma protein binding is important for understanding the pharmacokinetics of a molecule. These measurements along with others such as tissue binding, hepatocyte binding and microsomal binding can provide an insight into distribution and elimination from the body.
Read our fact sheet to learn more about our matrix binding services.
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Fact Sheets,
ADME/DMPK,
Cyprotex
Physicochemical properties provide an insight into the structure of a molecule and its physical behavior within a system, and they can influence its dissolution, absorption, distribution, metabolism, elimination, protein affinity and toxicity. Early assessment of a molecule's physicochemical properties supports rational compound design within drug discovery.
Read our fact sheet to learn more about our physicochemical profiling services.
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Fact Sheets,
ADME/DMPK,
Cyprotex,
Modelling and Simulation
Membrane permeability plays an important role in oral absorption. Cyprotex offers a range of in vitro permeability assays to understand passive permeability or transporter-mediated effects.
Read our fact sheet to learn more about our in vitro permeability services.
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Fact Sheets,
ADME/DMPK,
Cyprotex
Understand if your investigational drug has the potential to be a perpetrator (precipitant) of transporter-mediated drug-drug interactions by evaluating if it is an inhibitor of drug transporters.
Read our fact sheet to learn more about our transporter inhibition service.
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Fact Sheets,
ADME/DMPK,
IND Enabling Studies/Preclinical Development,
Cyprotex
Understand if your investigational drug is a potential victim (object) of transporter-mediated drug-drug interactions by evaluating if it is a substrate of drug transporters.
Read our fact sheet to learn more about our transporter substrate identification service.
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Fact Sheets,
ADME/DMPK,
IND Enabling Studies/Preclinical Development,
Cyprotex
Learn more about how Cyprotex can support you in the design, implementation and interpretation of drug-drug interaction (DDI) studies according to regulatory guidance including the ICH M12 harmonized guideline.
Read our DDI fact sheet to find out more.
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Fact Sheets,
ADME/DMPK,
IND Enabling Studies/Preclinical Development
Learn more about how Cyprotex can support you in discovery bioanalysis for small molecules and biotherapeutics (including peptides, oligonucleotides and protein degraders).
Read our fact sheet to find out more about our non-regulatory bioanalysis service.
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Drug Discovery,
Fact Sheets,
ADME/DMPK,
Cyprotex
Learn more about how Cyprotex can support you in understanding the metabolism of your compounds by identifying which metabolites are formed during in vitro and in vivo studies.
Read our fact sheet to learn more about our metabolite profiling and identification service.
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Fact Sheets,
ADME/DMPK,
IND Enabling Studies/Preclinical Development,
Cyprotex
