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. 2020 Jun 17;5(27):16318–16331. doi: 10.1021/acsomega.0c01058

Table 3. RTK Inhibitor-Based Radiotracers for Eph Receptor Imaging.

target lead compound skeleton IC50 enzyme IC50 cells developed by radiolabeling for imaging
EphB4 benzodioxolylpyrimidine (compound 1) n.d. 90 ± 50 nM Bardelle 201023 Mamat 201224 (fluorine-18)
EphB4 indazolylpyrimidine (compound 20) 1.3 nM 9 nM Bardelle 201023 Ebert 201525 (carbon-11)
Ebert 201525 (fluorine-18)
multi-Eph xanthine (compound 66) 1.6 (5) nM n.d. Lafleur 200926 Pretze 202027 (fluorine-18)