H2 histaminergic Biochemical Binding Assay for compound screening and profiling via competitive radioligand binding.
Target Overview
CAT#
H2 Binding
GPCR Target
Human H2
Source
Membrane preparation from CHO-K1 cells stably transfected with human H2 receptor.
Scientific Information
HRH2 (https://www.uniprot.org/uniprotkb/P25021/entry)
Assay Properties
Protocol
Radioligand filter binding to H2 membrane preparation ± cold competing ligand; radiometric measurement on MicroBeta scintillation counter
Readout
CPM representing 3H-disintegration detected using MicroScint-20
Radioligand
Famotidine, 20 nM
Reference Compound IC50
| Compound | IC50 (nM) |
|---|---|
| Ranitidine | 27.2 |
| Cimetidine | 1560 |
| Histamine | 4250 |
| Mepyramine | >10,000 |
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 H2
PDF