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## Media
### Title
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## Popup
### Body
htmlText_28171D44_38BB_4CEB_4187_918393CC78EF.html = Artificial Intellegence (AI) drug discovery methodologies and machine learning techniques can be applied to all stages of the discovery and optimization of chemical matter. Dedicated technologies are deployed for hit identification, hit-to-lead, and lead optimization to quickly explore novel chemical space and rapidly identify improved compounds.
Automating cellular assays enables increased throughput for complex assays and also enables more consistency across assays day-to-day, which is hugely important when the key drive of any assay is to measure differences in response to a given variable.
Characterization of a chemical series or drug candidate's ADME properties and pharmacokinetics is best when determined early. This helps to de-risk candidate molecules and improve project productivity through more targeted chemical synthesis and progression of the right compounds.
Experienced Charles River chemists gain maximum efficiency by combining the latest synthetic chemistry methodologies and technologies with innovative synthetic route designs. We offer rapid and efficient synthesis of molecules using the Synple automated synthesizers.
Generating a thorough physical characterization and pharmaceutical sciences data package provides crucial information to guide the selection of more robust candidates.
Human primary cell-based assays, such as cell proliferation assays, cell viability assays, and GPCR assays, were developed using cells derived from tissue, blood, or differentiated stem cells for high content analysis in more than 20 different disease area indications. These high-throughput assays accelerate drug discovery by delivering the right candidate in the most relevant biology.
In the webinar “Human iPSC-derived Cells for CNS Drug Discovery”, learn how scientists have manipulated induced pluripotent stem cells (iPSCs) to create a library of robust, reproducible neural cells suitable for high-throughput screening using the IN Cell and similar analyzers.
In this webinar “Enabling DMPK Science: Delivering In Vitro ADME Data Even Faster, ” learn how in vitro data are used for many purposes during the drug discovery and development stage to triage and prioritize NCEs to enable in vivo PK, PK/PD, efficacy and TK studies.
In vitro and in vivo DMPK ADME studies enable researchers to make go/no-go decisions on whether a compound should be selected as a drug candidate in the early medicinal chemistry and lead optimization phase of drug discovery.
Large scale analysis of specific proteomes, also known as proteomics, using protein mass spec platforms helps define protein diversity, and understand its biological consequences.
Medicinal and synthetic chemists, biologists, DMPK scientists, and pharmaceutical scientists at Charles River continually collaborate to build the most promising molecules, and they couldn’t do it without each other.
Molecular target identification, or target deconvolution, is essential for understanding compound mechanism, and further optimizing compounds of interest in the drug discovery pathway.
Multiple analytical and purification systems operate in parallel to create a flexible approach to accommodate standard and complex requirements from milligram to multigram scale. Once separated our Purification Sciences group utilise a range of drying processes to ensure the consistent safety and stability of your sample.
NMR at Charles River provides more insight in the chemical structure of test items and their chemical impurities and can also be used to quantify “hard to analyze” compounds.
Off-the-shelf or custom assays are available for screening and profiling ion channel targets, including major cardiac, central nervous system (CNS), and peripheral nervous system (PNS) channels.
Our chemists have deep expertise in synthetic chemistry; designing routes, troubleshooting, and optimizing multi-step synthetic sequences. We offer multi-stage synthesis from mg to kg scale, with expertise across non-classical small molecule areas e.g. macrocycles, PROTACs, pro-drugs, carbohydrates, natural products, peptidomimetics. We also have access to the latest technologies e.g. microwaves, H-cube, photochemistry, electrochemistry, flow chemistry, high-throughput experimentation, Synple synthesizer.
Our experienced medicinal chemists will use sophisticated structure-activity relationships (SAR) and multi-parameter optimizations (MPO) to develop compounds with the required profile; balancing potency, selectivity, physicochemical and ADME properties, in vivo pharmacokinetics, pharmacodynamics, efficacy, safety, tolerability and patentability.
Predictive models are used wherever possible to drive synthesis of the most promising compounds and overcome key issues.
Our medicinal chemistry team has experience in progressing small molecule drug discovery programs across a broad range of therapeutic areas and modalities. Together, they are cited as inventors on over 400 patents and 90 preclinical candidate compounds.
Our medicinal chemistry team has experience in progressing small molecule drug discovery programs across a broad range of therapeutic areas and modalities. Together, they are cited as inventors on over 400 patents and 90 preclinical candidate compounds.
Structural biology and biology protein structure services decipher the structure-function relationship of biological macromolecules.
Once the structure-function relationship has been defined, you can make changes to the ligands to improve potency and selectivity of your lead molecule.
The FLIPR® Penta High-Throughput Cellular Screening System allows us to perform fluorescence-based screens of up to 700,000 compounds.
The Incucyte® Live-Cell Analysis System are real-time quantitative live-cell imaging and analysis platforms that enable visualization and quantification of cell behavior over time, by automatically gathering and analyzing images around the clock.
This is an assay-ready workstation that enables rapid, hands-free processing, protecting sample integrity and high accuracy
Through a case study of ONO-8590580, you’ll discover how Charles River scientists took a metabolically unstable hit compound through lead optimization, improving functional selectivity, absorption, distribution, metabolism, and excretion (ADME), pharmacokinetics (PK) and brain receptor occupancy along the way.
Using multiplexing and techniques like cell painting, our disease-relevant cell-based assays allow you to measure and monitor phenotypic changes and optimize your early discovery efforts.
We have access to a 600 MHz Bruker AV3 spectrometer equipped with QCI cryoprobe. We cover many areas of biological NMR from 19F fragment screening to hit confirmation, characterization of proteins and RNA. NMR is also used as an orthogonal biophysical technique to SPR and HTS.
“Development and Validation NMDA Receptor Ligand Gated Ion Channel Assays Using Qube” describes the pharmacological assessment of modes of action on four members of the NMDA receptor family, NR1/NR2A, NR2B, NR2C and NR2D.
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