Our unique approach to Integrated Drug Discovery

Experienced Integrated Drug Discovery Team

Our experience will guide your drug discovery research programme successfully and cost effectively. We offer wide ranging expertise and pre-validated industry leading assays for ion channels.

Bringing experts together

Our highly experienced interdisciplinary team provides customers with a fully integrated drug discovery service by bringing together experts in:

• Ion channel biology
• Medicinal chemistry
• Specialist chemistry
• Translational biology
• ADMET and DMPK

Our integrated drug discovery service includes initial assay development, custom assay validation and high throughput screening in 384-well plate-based assays. It also comprises giga seal quality automated electrophysiology-based support for medicinal chemistry optimisation of compounds and highly experienced conventional electrophysiology services for profiling of lead compounds. We offer expert advice regarding translational assays such as microelectrode array and impedance measurement.

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Alongside our partners, Metrion Biosciences has the experience to steer your research programme to a successful and cost effective conclusion. Our suite of industry leading validated assays includes voltage-gated ion channels, ligand-gated ion channels multimodal transient receptor potential (TRP) channels, two-pore domain ‘leak channels, inward rectifier channels and hyperpolarisation-activated cyclic nucleotide gated ion channels.

Customised integrated drug discovery research programmes

Our extensive experience means we are very happy to discuss integrated drug discovery research programmes for all types of ion channels.

High Quality Small Molecule Library

Through Metrion Biosciences and our partners, customers can access a high quality library of 150,000 small molecules. This is in addition to a range of stable cell lines and validated assays, plus a choice of assay platforms to suit the requirements of individual customers during the hit identification stage of a discovery programme. Customers can access expert computational chemists for knowledge-based selection of a screening deck. Alternatively, we can perform diverse screens using the Assay.Works library alone or supplement this with customer molecules or libraries accessed via compound vendors.

Building appropriate screening cascades

Our team can provide advice and build appropriate screening cascades for customers who do not possess significant experience of the ion channel target class. Alternatively, we can work together with experienced customers to maximise their chances of success for this challenging target class.

Metrion’s Integrated Drug Discovery Service

Our integrated drug discovery service involves extensive interaction with customers to closely define the profile of compounds most appropriate to their therapeutic focus. This involves not only outlining individual drug-like properties to maximise efficacy or to limit side potential effects, but also to design each assay in the screening cascade to produce the most relevant biological data (such as block of a channel in a defined state).

High quality assays to drive enhancement of compound potency 

We also strive to maximise efficiency of the design and synthesis of new analogues to enable rapid structure-activity relationship (SAR) determination at an early stage, provide appropriate high quality assays to drive enhancement of compound potency and selectivity properties, we provide early assessment of ADME properties and rank hit compounds and/ or hit series for progression to lead optimization.

As each screening programme progresses through to lead optimisation, our collaborations provide access to expert toxicologists able to design and perform experiments to characterise potential (for example on-target) or observed toxicity issues. Through an understanding of mechanistic toxicology at this early research stage, we can generate information that informs molecule design, candidate selection and translational risk assessment. We can also provide advice regarding appropriate biomarker assays to provide reliable biological translation for the discovery programme.

Ion Channel Drug Discovery

For ion channel targets, our team has extensive experience supporting customer integrated research programmes and a track record of successful delivery of high quality assays, long term delivery of screening data to defined timelines to efficiently drive medicinal chemistry and has delivered clinical candidates for our customers. For an initial discussion please contact us.

Integrated Drug Discovery resource library