EDNRA Functional Cell-based Antagonist Assay for compound screening and profiling via fluorescence-based quantification of intracellular calcium.
Target Overview
CAT#
ENDRA Functional Antagonist
GPCR Target
Human EDNRA
Cell Line
CHO-K1/EDNRA
Scientific Information
EDNRA (https://www.uniprot.org/uniprotkb/P25101/entry)
Assay Properties
Protocol
30 min incubation with antagonist; EDNRA activation by agonist application using FLIPR Penta system cells treated with Calcium 6 dye; fluorescence kinetic measurement
Readout
Calcium 6 dye fluorescence tracking changes in intracellular calcium
Reference Compound IC50
| Compound IC50 (nM) | Agonist (nM) |
|---|---|
| Sparsentan (672) | Endothelin (100) |
| Sitaxentin (79.1) |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website In Vitro Safety Pharmacology Profiling
Reference compound inhibition of EDNRA
PDF