Experienced Intergrated Drug Discovery Team
Our highly experienced interdisciplinary team provides clients with a fully integrated drug discovery service by bringing together experts in ion channel biology, medicinal chemistry, specialist chemistry, translational biology, ADMET & DMPK. This integrated service spans initial assay development, custom assay validation and high throughput screening in 384-well plate-based assays, giga seal quality automated electrophysiology-based support for medicinal chemistry optimisation of compounds, highly experienced conventional electrophysiology services for profiling of lead compounds, plus expert advice regarding translational assays such as microelectrode array and impedance measurement. We also offer an industry leading suite of cardiac safety profiling assays.
Along with our partners, including Assay.Works, Metrion Biosciences has the experience to steer your research programme to a successful, and cost effective, conclusion. We offer wide ranging expertise and our suite of validated assays and an expert assay validation service includes industry leading assays for voltage-gated ion channels, ligand-gated ion channels and other gating class channels such as multimodal transient receptor potential (TRP) channels, two-pore domain ‘leak’ channels, inward rectifier channels and hyperpolarisation-activated cyclic nucleotide gated ion channels. 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, clients can access a high quality library of 150,000 small molecules, 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. Clients can access expert computational chemists for knowledge-based selection of a screening deck or we can perform diverse screens using the Assay.Works library alone or supplement this with client molecules or libraries accessed via compound vendors.
Our team can either provide advice and build appropriate screening cascades for clients who do not possess significant experience of the ion channel target class or work together with experienced clients 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 clients 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). 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 client 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 clients. For in initial discussion please contact us via the button below.