Quantitative Assays for Hemichannel Inhibitors in Living Cells

A screening of 2,242 approved drugs and compounds under development for their effect on connexin-based hemichannels. The dataset likely contains results from two automated cell-based assays measuring dye uptake and fluorescence quenching. The study was conducted by Emmanuelle Soleilhac of Inserm and identified 11 new hemichannel blockers.

Use Cases

• Identify potential drug repurposing candidates based on hemichannel inhibition activity.
• Compare drug effects on hemichannel versus gap junction activity based on the assay results.
• Validate automated fluorescence-based assays for high-throughput screening of membrane channel modulators.

Strengths

• Screens a substantial library of 2,242 compounds.
• Employs two distinct, automated cell-based assays for validation.
• Identifies 11 new hemichannel blockers, with 5 showing specificity over gap junction activity.

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• Data may reflect methodological bias inherent to the specific fluorescence assays described.

Provenance

Source

Inserm

Collection Method

Automated cell-based assays (Yo-Pro dye uptake and YFPQL quenching by iodide) used to screen a compound library.