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To B or Not To B: Phenotypic Profiling BTK Inhibitors in BioMAP® Systems

To B or Not To B: Phenotypic Profiling BTK Inhibitors in BioMAP® Systems
File Name/Number:
Drug Dicovery Chemistry

Year:
2013

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Screening compounds in primary human cell BioMAP® systems designed to model diseased tissues reinstates a more physiological approach to drug discovery. Here, we present BioMAP® analysis of two BTK inhibitors revealing cell-selectivity, efficacy and safety related activities. Ibrutinib is broadly active on endothelial, epithelial, smooth muscle cells and fibroblast-based systems, while GDC-0834 is more selectively active in the BT system. Using these examples, we will show how BioMAP® can be used to guide pre-clinical development.