Table 5.
Profiling of selected compounds by thermal shift assay ΔTm in kelvin; SPR KD in nM; NanoBRET EC50 in nM; metabolic stability in h and solubility in μg/mL; N/A = not applicable; n.d. = not determined.
| ΔTm [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.d. | n.d. | n.d. | n.d. |
| 23 | 8.1 | 6.6 | 120.4 ± 4.6 | 7.7 | 470 ± 31 | 450 ± 140 | 20 ± 5.7 | 6.6 | n.d. |
| 28 | 4.3 | 7.0 | N/A | 49.7 | n.d. | n.d. | n.d. | n.d. | n.d. |
| 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.d. | n.d. |
| 79 | 8.1 | 8.7 | 126.1 ± 9.9 | 5.0 | 1400 ± 290 | 60 ± 13 | 31 ± 2.9 | n.d. | n.d. |