KOP Functional Cell-based Antagonist Assay for compound screening and profiling via fluorescence-based quantification of intracellular calcium.
Target Overview
CAT#
KOP Functional Antagonist
GPCR Target
Human KOP
Cell Line
CHO-K1/OPRK1/Gα15
Scientific Information
OPRK1 (https://www.uniprot.org/uniprotkb/P41145/entry)
Assay Properties
Protocol
30 min incubation with antagonist; KOP 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 EC50
| Compounds | IC50 (nM) |
|---|---|
| Naltrexone | 529 |
| Naltrindole | 1033 |
| Aticaprant | 8.5 |
Agonist = 200 nM Asimadoline
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website GPCR Assay and Profiling Services
Reference compound inhibition of KOP
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