This article and associated images are based on a poster originally authored by Liana Bauer, Maximilian Seifermann, Julius Höpfner, Divya Varadharajan, Stefan Schmidt, Björn Fröhlich, Benjamin Wellenhofer, Charlotte Luchena, Carsten Hopf, Anna A. Popova, and Pavel A. Levkin, and presented at ELRIG Drug Discovery 2025 in affiliation with Karlsruhe Institute of Technology (KIT), Scivalon, Technische Hochschule Mannheim and Heidelberg University.
This poster is being hosted on this website in its raw form, without modifications. It has not undergone peer review but has been reviewed to meet AZoNetwork's editorial quality standards. The information contained is for informational purposes only and should not be considered validated by independent peer assessment.
The platform
Image Credit: Liana Bauer et al., in partnership with ELRIG (UK) Ltd.
Aim
- Discovery of novel MEK inhibitors
- Overactive kinase implicated in 30 % of all cancers
- Allosteric inhibition to circumvent acquired resistance
Image Credit: Liana Bauer et al., in partnership with ELRIG (UK) Ltd.
Library design
Image Credit: Liana Bauer et al., in partnership with ELRIG (UK) Ltd.
Workflow
Image Credit: Liana Bauer et al., in partnership with ELRIG (UK) Ltd.
Chemical analysis
- Stepwise quantification of each intermediate on droplet array with d = 2.83 mm
- Synthesis in total volume of 5 μl / spot
- Extraction from surface for analysis via LCMS
- Qualitative Analysis of all library compounds via MALDI-MS and MS Imaging
- Integration of synthesis and analysis without any transfer on spots with d = 900 μm
- Synthesis in total volume of 200 nl / spot
Image Credit: Liana Bauer et al., in partnership with ELRIG (UK) Ltd.
On-chip screening
- Direct on-chip screening on aroplet Array with d = 1.4 mm
- Screening of HT-29 cells, a human colorectal cancer cell line
- Optimization of compound release to an assay concentration of ~10 μM
- Comparison of the amount of dead cells after treatment with 10 μM mirdametinib (= positive control)
- 46 promising compounds with higher response in direct comparison
Image Credit: Liana Bauer et al., in partnership with ELRIG (UK) Ltd.
Summary
- Miniaturized platform for integration of synthesis, analysis, and screening
- Synthesis of 325 compounds using ~10 mg of reactants and ~250 μl solvent
- Identification of 46 primary hit compounds
- Synthesis and screening in only seven days
About Karlsruhe Institute of Technology
The Karlsruhe Institute of Technology (KIT), known as “The University in the Helmholtz Association,” is the only German university of excellence that integrates a national large-scale research sector. It offers students, researchers, and staff exceptional opportunities for learning, teaching, and collaboration. With origins dating back to 1825, KIT in its current form was established in 2009 through the merger of the Technical University of Karlsruhe and the Karlsruhe Research Center.
About ELRIG (UK) Ltd.
The European Laboratory Research & Innovation Group (ELRIG) is a leading European not-for-profit organization that exists to provide outstanding scientific content to the life science community. The foundation of the organization is based on the use and application of automation, robotics and instrumentation in life science laboratories, but over time, we have evolved to respond to the needs of biopharma by developing scientific programmes that focus on cutting-edge research areas that have the potential to revolutionize drug discovery.
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Our values
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Our purpose
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Last Updated: Nov 11, 2025