Table 4.
EC50 values for prioritized compounds determined in a cellular NanoBRET target engagement assay. See Table S2 for complete data set.
| EC50 [nM] | ||||||
|---|---|---|---|---|---|---|
| cpd ID | EPHA2 | EPHA4 | GAK | ABL1 | FGFR1 | FLT1 |
| 23 | 470 ± 31 | 450 ± 140 | 20 ± 5.7 | 27000 ± 210 | 3100 ± 870 | 13000 ± 5400 |
| 54 | 370 ± 68 | 84 ± 32 | 160 ± 29 | 2700* | 1200 ± 230 | 13000 ± 130 |
| 55 | 260 ± 73 | 57 ± 23 | 27 ± 5.6 | >50000 | 18000 ± 1900 | 33000 ± 3600 |
| 56 | 440 ± 0.99 | 250 ± 57 | 40* | 30000 ± 2300 | 2000* | 7500* |
| 58 | 250* | 190 ± 45 | N/A. | 6400* | 470* | 1100* |
| 61 | 340 ± 81 | 37 ± 12 | 33 ± 4.9 | 8400* | 7600 ± 1100 | 17000 ± 2300 |
| 75 | 1600 ± 380 | 37 ± 12 | 24 ± 3.4 | >50000 | 34000 ± 11000 | 42000 ± 5700 |
| 78 | 470* | N/A | 30* | 17000* | N/A. | N/A |
| 79 | 1400 ± 290 | 60 ± 13 | 31 ± 2.9 | 32000* | 9800 ± 1900 | 23000 ± 2600 |
Mean of one experiment performed in technical duplicates