Compounds with reported binding affinity to FKBP12
| Compound | Literature values in FKPB12 assay (nM) | FKBP12 TR-FRET Kd (nM) | Dose-dependent rescue from tacrolimus in mouse T cells | Inhibition of mouse T cells by compound alone |
| Tacrolimus | – | 1.7* | – | – |
| Rapamycin | – | 1.0 | – | – |
| GPI-1046 | Ki 7.5 (PPI)33 IC50 1240 (FP)32 | 25.6% inhibition at 10 µM | – | – |
| V10-367 | Ki 0.5 (PPI)31 | 432 | No | Yes |
| VX-710, biricodar | IC50 17 (FP)32 | 180 | No (figure 2A) | Yes (figure 2A) |
| Q-2361 (L-685,818) | EC50 0.7 (3H-FK)30 | 2.0† | Yes (figure 2B) | No (figure 2B) |
*Mean of three experiments.
†Mean of two experiments.
FP, fluorescence polarization assay; 3H-FK, [3H]-dihydro-FK506 displacement assay; PPI, peptidyl-prolyl isomerase assay.