VHL binding assay - fluorescence polarization (FP) based service
Determine binding to VHL protein with our proprietary fluorescent probe CELT-504.
A service based on fluorescent polarization measurement that rapidly classifies and characterises your candidates, enabling the discovery and selection of promising compounds.
For full technical details, assay parameters and validation datasheets, see the VHL binding assay service brochure.
What is this service?
Celtarys’ VHL binding assay service is a fluorescent polarization-based assay that uses CELT-504 as the fluorescent tracer, alongside the ElonginB/ElonginC-VHL (VBC) complex to study the binding affinity of different ligands for the VHL E3 ligase. CELT-504 has been developed with FP in mind starting with its design. The affinity of this compound is in the low nanomolar range, allowing for the calculation of the binding affinity of a wide range of compounds. Indeed, both IC50 and Ki via Chen-Prusoff equation can be obtained.
Screening options
We offer a two-step screening strategy so you can quickly rank and thoroughly characterise only the best candidates:
Affinity binding screen (single point): qualitative detection of ligand binding based on fluorescence signal. 1 point readout at 1 µM (percent inhibition vs. tracer control).
Displacement curves to calculate IC50 and estimate Ki values for your compounds. You can choose which concentrations to test.
Compounds showing > 50 % inhibition at 1 µM proceed to a concentration-response displacement curve (choose 5 or 7 concentration points) for IC50 and estimate Ki estimation.Do you want more information?
We are ready to support your challenges