Development of a robust hNaV1.9 high-throughput screening assay on the Sophion Qube384 platform. This is complemented by a suite of ion channel selectivity assays and sensory neuron recordings to create a versatile screening cascade to support NaV1.9 drug discovery programmes.
We developed a high-throughput, electrophysiological assay of TREK-1 function to identify novel modulators. The assay was optimized to identify both activators and inhibitors, providing comprehensive mechanistic data for high value, limited supply screening libraries, such as the venom fraction library used in this study (Targeted Venom Discovery Array, T-VDA, Venomtech, UK).
Kv7 ion channels are highly relevant to epilepsy because they are voltage gated potassium ion channels that help regulate neuronal excitability and suppress excessive electrical firing in the brain.
Cardiac toxicity remains the leading cause of new drug safety side-effects. Current preclinical cardiac safety assays rely on in vitro cell-based ion channel assays and ex vivo and in vivo animal models⁽¹⁾. These assays provide an indication of acute risk but they do not always predict the effect of chronic compound exposure, as recently seen with oncology drugs. Therefore, new assays are required to characterise chronic structural and functional effects in human cells earlier in drug discovery. Impedance-based technology can provide more accurate chronic cardiotoxicity measurements in an efficient manner using human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs).
By accurately defining the drug exposure levels that affect QRS duration, researchers can establish safety margins, prioritise lower-risk compounds, and reduce the chance of late-stage failures due to cardiac toxicity
We demonstrate the generation and validation of a stable CHO-hHCN2 cell line used as a cellular tool in the successful development of hHCN2 automated electrophysiology screening assays.
Kv7 channels are a family of voltage gated potassium ion channels that play a key role in controlling cellular excitability.
Metrion and Sophion collaborated to determine whether other insoluble salts can act as seal enhancers, or whether this property is unique to CaF2.
CiPA logoThe International Council on Harmonization (ICH) S7B and E14 regulatory guidelines were introduced in 2005 to evaluate the proarrhythmic liability of new drugs.
Epilepsy is a chronic neurological disorder characterised by recurrent, unprovoked seizures caused by abnormal electrical activity in the brain. Seizures can vary widely in severity and presentation, ranging from brief lapses in awareness to widespread convulsions.