Fluorescence Polarization

Fluorescence polarization (FP), also known as Fluorescence anisotropy, is commonly used in early-phase drug discovery. When a fluorescent molecule is excited by polarized light, the polarization degree of the emitted wavelength is determined by the rate of molecular rotation. A fluorescently labeled small molecule rotates rapidly in solution, therefore the light emitted is depolarized. On the other hand, when a fluorescent probe is binding to a target protein, its rotation is slower, and the emission wavelength is polarized.

This method can be used to study molecular interactions (binding, kinetics, etc.) and enzyme activities in solution. The main advantage of fluorescence polarization is the possibility of performing anhomogenous assay, making it especially suitable for High Throughput Screening approaches.

We have validated several of our fluorescent ligands as optimal tools for FP, both on membrane preparations from cell cultures and on membrane extracts from baculovirus.

Celtarys Ligands validated for Fluorescence Polarization assays
  • CELT- 426 hD2 Dopamine receptor fluorescent antagonist (560/571)

    Our potent and partially selective hD2 Dopamine receptor fluorescent antagonist shows high affinity for hD2 receptor and partial selectivity over the other receptor subtypes (Ki =89.3 nM for hD2 receptor in radioligand binding assay). It has been validated in Fluorescence Polarization binding assays as a valid alternative to radioligand binding assays.It allows to perform cell visualization in fluorescence microscopy, confocal microscopy and high content system experiments. It is potentially suitable for other fluorescence-based assays.

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  • CELT- 419 hD3 Dopamine receptor fluorescent ligand (560/571)

    Our potent and partially selective hD3 Dopamine receptor fluorescent ligand shows high affinity for hD2 receptor and partial selectivity over the other receptor subtypes (Ki =65.6 nM for hD3 receptor in radioligand binding assay). It has been validated in Fluorescence Polarization binding assays as a valid alternative to radioligand binding assays.It allows to perform cell visualization in fluorescence microscopy, confocal microscopy and high content system experiments. It is potentially suitable for other fluorescence-based assays.

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  • CELT-228 hA3 Adenosine receptor fluorescent antagonist (560/671)

    Our potent and selective hA3 Adenosine receptor fluorescent antagonist shows high affinity for hA3 receptor and partial selectivity over the other receptor subtypes (Ki =52.7 nM for hA3 receptor in radioligand binding assay). It has been validated in Fluorescence Polarization binding assays as a valid alternative to radioligand binding assays.It allows to perform cell visualization in fluorescence microscopy, confocal microscopy and high content system experiments. It is potentially suitable for other fluorescence-based assays.

    More information and applications

    https://pubs.acs.org/doi/10.1021/acsmedchemlett.1c00598

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