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05.10.2020 - Poster - Reliable Identification of hERG Liability in Drug Discovery

Reliable Identification of hERG Liability in Drug Discovery by Automated Patch Clamp

Introduction:

The Comprehensive in Vitro Proarrhythmia Assay (CiPA) was initiated in 2013 to improve pre-clinical drug safety paradigms. The aims of the initiative are not only to ensure that drugs which reach the market are safe, but also to reduce the number of false positives; thus ensuring that more potentially useful (and safe) drugs reach the market. As part of this initiative, compounds representing high, intermediate, and low proarrhythmic risk categories were tested across multiple sites and automated patch clamp (APC) platforms. Resulting IC50 values varied between platforms, which could be due to non-specific binding of compounds in well-based platforms (since they don’t maintain a constant flow of compound-containing solution to replenish losses to fluidics and well walls).

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