CRBN binding assay - fluorescence polarization (FP) based service
Determine binding to CRBN protein with our proprietary fluorescent probe CELT-077.
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 CRBN binding assay service brochure.
What is this service?
Celtarys’ CRBN binding assay service is a fluorescent polarization-based assay that uses CELT-077 as the fluorescent tracer, alongside the CUL4A/RBX1/DDB1/CRBN complex, to study the binding affinity of different ligands for CRBN. CELT-077 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 can be obtained using the Cheng–Prusoff equation.
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.Example / Case study (14‑compound cohort)
To illustrate output and decision flow, we completed a CRBN fluorescent polarization pilot assay in which fourteen candidate molecules were profiled through an affinity binding screen at 1 µM (percent inhibition vs. tracer control). The resulting report delivered rank‑ordering across the cohort and screen‑stage percent‑inhibition tables. To view the report and visualise the data sets from this validation, please refer to the quick study.
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