Our CRBN binding assay kit is a fluorescence polarization (FP)-based assay that enables quantitative evaluation of ligand binding to the CUL4A/RBX1/DDB1/CRBN complex.

This kit uses CELT-077 as a high-affinity fluorescent tracer (low nanomolar range), allowing the determination of IC₅₀ and Ki values through competitive binding experiments in a robust binary format.

The assay has been validated using reference compounds such as such as pomalidomide and thalidomide, providing affinity values consistent with reported data. (1)

The homogeneous FP format allows direct monitoring of binding events without washing steps, making it suitable for compound screening, profiling and PROTAC development workflows.

For more information on fluorescence polarization techniques, please refer to our blog article.

References

(1) Fischer, E. S., Böhm, K., Lydeard, J. R., Yang, H., Stadler, M. B., Cavadini, S., Nagel, J., Serluca, F., Acker, V., Lingaraju, G. M., Tichkule, R. B., Schebesta, M., Forrester, W. C., Schirle, M., Hassiepen, U., Ottl, J., Hild, M., Beckwith, R. E., Harper, J. W., Jenkins, J. L., … Thomä, N. H. (2014). Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide. Nature, 512(7512), 49–53.