H1 histaminergic Biochemical Binding Assay for compound screening and profiling via competitive radioligand binding.
Target Overview
CAT#
H1 Binding
GPCR Target
Human H1
Source
Membrane preparation from HEK293 cells stably transfected with human H1 receptor.
Scientific Information
HRH1 (https://www.uniprot.org/uniprotkb/P35367/entry)
Assay Properties
Protocol
Radioligand filter binding to H1 membrane preparation ± cold competing ligand; radiometric measurement on MicroBeta scintillation counter.
Readout
CPM representing 3H-disintegration detected using MicroScint-20
Radioligand
Pyrilamine, 5 nM
Reference Compound IC50
| Compound | IC50 (nM) |
|---|---|
| Mepyramine | 5.0 |
| Ranitidine | >10,000 |
| Cimetidine | >10,000 |
| Histamine | 3210 |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website GPCR Assay and Profiling Services
Reference compound binding data for H1
PDF