Table 1. Validation of Initial Hit 1 as a Cbl-b Inhibitor.

^aIC₅₀ binding values for Cbl-b are based on a TR-FRET probe displacement assay and are the average of at least three determinations.

^blog D measured via shake-flask method in octanol and water at pH 7.4.

^cLLE: p(IC₅₀) – log D.

^dCompound 1 was measured by SPR to have a K_d of 0.40 μM. All SPR measurements are the average of at least two determinations.