Table 2. IC50 (Rounded) and Selectivity of Ibrutinib Derivatives against Selected Ibrutinib Kinase Off-Targets.
| BTK | BLK |
BMX |
EGFR |
ERBB2 |
ITK |
||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| compound | IC50 (nM) | IC50 (nM) | BLK/BTK | IC50 (nM) | BMX/BTK | IC50 (nM) | EGFR/BTK | IC50 (nM) | ERBB2/BTK | IC50 (nM) | ITK/BTK |
| ibrutinib | 0.3 | 0.1 | 0 | 0.2 | 1 | 3 | 10 | 10 | 38 | 78 | 311 |
| 3c | 0.1 | 0.1 | 1 | 0.3 | 5 | 7 | 105 | 33 | 472 | 43 | 607 |
| 3h | 0.1 | 0.6 | 7 | 0.3 | 4 | 28 | 348 | 196 | 2400 | 295 | 3613 |
| 3e | 0.1 | 0.1 | 1 | 0.4 | 5 | 3 | 36 | 13 | 169 | 30 | 383 |
| 3i | 0.1 | 0.8 | 11 | 0.4 | 5 | 31 | 417 | 172 | 2292 | 232 | 3087 |