ChanTest’s GPCR screening panel includes over 125 targets, and includes receptors from all major GPCR classes. All assays are fully validated and have been designed to provide high quality screening and profiling data for both drug discovery and safety assessments.

Instrumentation: FLIPR^TETRA®, FlexStation® 3

Readouts: cAMP, calcium, membrane potential, binding

GPCR Screening: Cell-based screens performed with calcium-sensitive or membrane-potential-sensitive dyes. Gs- and Gi-coupled GPCRs are assayed via cAMP determinations using either a cell-based real time cAMP assay or other validated cAMP assay platform. EC₅₀ / IC₅₀ determinations on confirmed actives are offered as a follow-up option. All screens include positive controls and a comprehensive report.

GPCR Profiling: Compound profiling against multiple receptors to determine specificity or off-target activity.

Mode of Action Studies: Full characterization of orthostatic and allosteric ligands.

GPCR Functional Selectivity: Measurement of GPCR functional selectivity and differentiation from assay format artefacts.

ChanTest Compound Library: Our diverse, custom-made compound library consists of 12,600 compounds (40 384-well plates). Library screen turnaround is one business week and includes EC₅₀ / IC₅₀ follow-up of confirmed actives identified in the screen.

To receive a quote or for additional information, please email inquiries@chantest.com or call 216-332-1665. Check back regularly for an updated listing of available targets.

Download: GPCR targets and assay readout pdf.