| Assay Method Information | |
| | Lenalidomide Assay |
| Description: | Compounds in Atto565-Lenalidomide displacement assay were dispensed in a 384-well microplate (Corning, 4514) using D300e Digital Dispenser (HP) normalized to 1% DMSO into 10 nM Atto565-Leanlidomide, 100 nM DDB1deltaB-CRBN, 50 mM Tris pH 7.5, 200 mM NaCl, 0.1% Pluronic F-68 solution (Sigma). Compound titrations were incubated for 60 min at RT. The change in fluorescence polarization was monitored using a PHERAstar FS microplate reader (BMG Labtech) for 1 h in 120 s cycles. Data from three independent replicates (n=3) was used to estimate IC50 values using variable slope equation in GraphPad Prism 7. Compounds 9, 10, and 11 are potent binders of CRBN with IC50 comparable to FDA approved lenalidomide, while being inactive in degradation of IKZF1 |
| Affinity data for this assay | |
|---|---|
| If you find an error in this entry please send us an E-mail | |