Figure 5.

Profiling of representative FKBP ligands by competitive NanoBRET assays. (A) HEK293T cells stably over‐expressing FKBP12‐NLuc were treated with various FKBP ligands in the presence of 20 nM of tracer 2 b. (B) HEK293T cells stably over‐expressing FKBP51‐NLuc were treated with various FKBP ligands in the presence of 200 nM of tracer 2 c. Data points represent means±standard deviation from three independent cellular assays per concentration. Tables: Summary of the results obtained for different FKBPs. (a) compound numbers and K _D values were taken from Ponplum et al.,^[12] (b) compound numbers and K _D values were taken from Voll et al.,^[19] (c) K _D values were taken from Gaali et al.,^[17] (d) K _D values were taken from Kozany et al.,^[10] (e) K _D values were determined by fluorescence polarisation assay.^[12]