Selectivity of pirtobrutinib in cell-based assays
| Kinase . | n . | Pirtobrutinib IC50, mean ± SD, nM . | Fold selectivity vs BTK∗ . | Cell assay readout . |
|---|---|---|---|---|
| BTK | 3 | 0.66 ± 0.34 | 1 | Competitive displacement of tracer |
| TEC | 3 | 70.46 ± 20.30 | 106.8 | Competitive displacement of tracer |
| BRK/PTK6 | 3 | 360.47 ± 198.56 | 546.2 | Competitive displacement of tracer |
| TXK | 3 | >5000† | >7600 | Competitive displacement of tracer |
| YES1 | 3 | >5000† | >7600 | Competitive displacement of tracer |
| CSK | 3 | >5000† | >7600 | Competitive displacement of tracer |
| FYN | 3 | >5000† | >7600 | Competitive displacement of tracer |
| ERBB4 | 2 | >10 000† | N/D | Phosphorylation of C-terminal tail |
| MEK1/MEK2 | 3 | 12 600 ± 2400 | N/D | Phosphorylation of ERK1/2 (HCT116 cells) |
| MEK1/MEK2 | 3 | 3790 ± 1310 | N/D | Phosphorylation of ERK1/2 (A375 cells) |
| Kinase . | n . | Pirtobrutinib IC50, mean ± SD, nM . | Fold selectivity vs BTK∗ . | Cell assay readout . |
|---|---|---|---|---|
| BTK | 3 | 0.66 ± 0.34 | 1 | Competitive displacement of tracer |
| TEC | 3 | 70.46 ± 20.30 | 106.8 | Competitive displacement of tracer |
| BRK/PTK6 | 3 | 360.47 ± 198.56 | 546.2 | Competitive displacement of tracer |
| TXK | 3 | >5000† | >7600 | Competitive displacement of tracer |
| YES1 | 3 | >5000† | >7600 | Competitive displacement of tracer |
| CSK | 3 | >5000† | >7600 | Competitive displacement of tracer |
| FYN | 3 | >5000† | >7600 | Competitive displacement of tracer |
| ERBB4 | 2 | >10 000† | N/D | Phosphorylation of C-terminal tail |
| MEK1/MEK2 | 3 | 12 600 ± 2400 | N/D | Phosphorylation of ERK1/2 (HCT116 cells) |
| MEK1/MEK2 | 3 | 3790 ± 1310 | N/D | Phosphorylation of ERK1/2 (A375 cells) |