Table 3. In Vitro ADMET Profile of BMS-986242 (25).
| parameter | BMS-986242 (25) |
|---|---|
| met. stability CYP (T1/2 min) | 14 (H), 4 (M), 10 (R), 10 (D), 2 (C) |
| met. stability UGT (T1/2 min) | >120 (H), >120 (M), 93 (R), 33 (D), >120 (C) |
| PAMPA (pH 7.4) | 2830 nm/sec |
| Caco (a-b:b-a) | 88:55 nm/sec |
| human CYP IC50 (μM) | 2C8:1.39; 2C9:0.74; 2C19:3.37; others >15 |
| hERG patch clamp | 87% inh at 10 μM |
| Na+ patch clamp | <20% inh at 10 μM (1 and 4 Hz) |
| Ca2+ patch clamp IC50 | >25 μM |
| protein binding (% free): h, m | <0.3, <0.2 |
| PXR-TA EC50 | >50 μM |