IC50 Values as Determined by Radioligand Displacement Studies for FAP (Using 177Lu-FAPI-04) and by Inhibition of DPP4 Enzyme Activity
| Compound | IC50 (FAP) MW ± SD (n = 3) | IC50 (DPP4) MW ± SD (n = 2) |
| FAPI-alkyne (11) | 109 ± 60 nM | 9.5 μM |
| FGlc-FAPI | 167 ± 110 nM | 26.6 μM |
| FAPI-04 | 49 ± 22 nM | 7.9 μM |
| Ga-FAPI-04 | 32 ± 7 nM* | Not determined |
↵* n = 2.