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[Preprint]. 2024 Feb 18:2024.02.18.580805. [Version 1] doi: 10.1101/2024.02.18.580805

Table 5.

Profiling of selected compounds.

Tm [K] SPR KD [nM] NanoBRET EC50 [nM]
EPHA2 GAK EPHA2 GAK EPHA2 EPHA4 GAK t1/2 [h] solubility [μg/mL]
6 6.7 4.9 307.0 ± 3.8 112.4 2800 N/A N/A N/A N/A
23 8.1 6.6 120.4 ± 4.6 7.7 470 ± 31 450 ± 140 20 ± 5.7 6.6 N/A
28 4.3 7.0 N/A 49.7 N/A N/A N/A N/A N/A
55 7.4 7.0 180.5 ± 3.5 19.2 260 ± 73 57 ± 23 27 ± 5.6 4.6 2.24 ± 0.12
75 6.5 7.5 95.3 ± 2.0 6.2 1600 ± 380 37 ± 12 24 ± 3.4 N/A N/A
79 8.1 8.7 126.1 ± 9.9 5.0 1400 ± 290 60 ± 13 31 ± 2.9 N/A N/A