High-content screening (HCS), also known as high-content analysis  (HCA), is a largely used methodology in drug discovery to identify compounds interacting with specific targets in whole cells. This assay is especially suited for high throughput screening with multi-well plates.

In a classical competition binding assay, cells are incubated with a fixed concentration of the fluorescent ligand followed by the addition of growing concentrations of the compound of interest (competitor). Fluorescence intensity is measured at each concentration to obtain a sigmoidal curve, suitable for affinity determination.

Celtarys Ligands validated for High Content Screening assays
  • CELT-335 hCB1/CB2 Cannabinoids receptors fluorescent ligand (646/662)

    10ug vial that allows to prepare 73ml of 100nM working solution to test CB1R/CB2R.

    Working concentration might differ among assay designs

    432,00

    Our CELT-335 product is a potent and selective hCB1/CB2 fluorescent ligand that shows a high affinity for CB1/CB2 receptors. It has a Ki value of 44.8 nM and 7.4 nM, respectively, in radioligand binding assay. CELT-335 has been validated in high-content screening assays and is also suitable for HTRF binding assays, providing a valid alternative to radioligand binding assays. It is available in a 10ug vial that allows for the preparation of 150ml of 100nM working solution to test CB1R/CB2R. CELT-335 is designed to allow for cell visualization in fluorescence microscopy and is potentially suitable for other fluorescence-based assays.

    More information and applications

    https://www.sciencedirect.com/science/article/pii/S1043661821005545?via%3Dihub

    https://www.mdpi.com/1420-3049/28/24/8107

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  • CELT-331 hCB2 Cannabinoids receptor fluorescent ligand (646/662)

    10ug vial that allows to prepare 76ml of 100nM working solution to test CB2R.

    Working concentration might differ among assay designs

    Our CELT-331 product is a potent and selective hCB2 fluorescent ligand that shows a high affinity for hCB2 receptors and selectivity over hCB1. It has a Ki value of 75.9 nM for hCB2 receptors in radioligand binding assay. CELT-331 is suitable for HTRF binding assays as a valid alternative to radioligand binding assays. It is available in a 10ug vial that allows for the preparation of 150ml of 100nM working solution to test CB2R. CELT-331 is designed to allow for cell visualization in fluorescence microscopy, confocal, and high-content system experiments and is potentially suitable for other fluorescence-based assays.

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Do you want more information?

If you want to know more about how to use fluorescent ligands to characterize receptors with pharmacological interest with this and other technologies, click on the button to download the article “Fluorescent ligands: A new method to label your GPCRs”

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