Table 4.
IC50 values were collected from data provided in Cortellis Drug Discovery Intelligence.
| Name (synonyms) | BTK | TEC | ITK | BMX | TXK | JAK3 | EGFR |
|---|---|---|---|---|---|---|---|
| Branebrutinib (BMS-986195) | 0.1 * | 0.9 | 100.0 | 1.5 | 5.0 | No data | 2,000.0 |
| BMS-986142 | 0.7 * | 21.2 * | 507.5 * | 85.0 * | 87.5 * | 1,000.0 | 1,000.0 |
| Tolebrutinib (SAR-442168, PRN2246) | 0.9 * | 1.0 | 365.0 | 1.1 | 1.7 | 1425.0 * | 4.1 |
| Poseltinib (LY-3337641, HM-71224) | 2.3 * | 4.5 | 103.0 | 0.6 | 4.6 | 18.8 * | 26.0 * |
| Ibrutinib (imbruvica, PCI-32765) | 2.4 * | 37.2 * | 91.9 * | 1.2 * | 4.5 * | 51.8 * | 30.2 * |
| Fenebrutinib (GDC-0853) | 5.3 * | >1000 | >1000 | 351.0 | >1000 | >1000 | >1000 |
| Remibrutinib (LOU064) | 5.5 * | No data | No data | No data | No data | No data | No data |
| Tirabrutinib (GSK-4059, ONO-4059) | 7.8 * | 29.0 * | >1000 | 21.7 * | 203.5 * | >1000 | >1000 |
| Acalabrutinib (calaquence, ACP-196) | 10.4 * | 142.1 * | >1000 | 91.6 * | 427.8 * | >1000 | >1000 |
| Spebrutinib (CC-292) | 15.4 * | 10.2 * | 674.7 * | 6.4 * | 93.7 * | 75.3 * | 436.0 * |
| Rilzabrutinib (PRN1008) | 33.4 * | 0.8 * | 440.0 | 1.0 * | 1.2 * | >5000 | 520.0 |
| Evobrutinib (M2951) | 47.7 * | ≤ 100 | ≤ 10000 | > 10 | >100 | 10,000.0 | 10,000.0 |
| Elsubrutinib (ABBV-105) | 175.0 * | 23,400.0 | 32,400.0 | No data | 9,180.0 | 8,640.0 | 14,400.0 |
Instances where multiple values were averaged together and noted with a *. For analysis, these values were binned together based on the strength of their nanomolar IC50s and colored as follows: low nanomolar (<10 nM) in red, low-mid nanomolar (10-100 nM) in orange, high-mid nanomolar (100-1000 nM) in yellow, and high nanomolar (>1000 nM) in green.