Table 1.
Binding constants for compounds to CRBN measured by surface plasmon resonance and their ability to induce degradation of neo-substrates Aiolos and CK1α at 10 μM.
| Degradation | |||
|---|---|---|---|
| Compound | CRBN Kd / nM[a] | Aiolos | CK1α |
| Lenalidomide | 445 ± 19 | + | + |
| Pomalidomide | 264 ± 18 | + | - |
| 1 | >11000 | - | - |
| 2 | N.B. | - | - |
| 3 | N.D. | - | - |
| 4 | N.D. | - | - |
| 5 | N.D. | - | - |
| 6 | 1450 ± 49 | - | - |
| 7 | 1400 ± 375 | - | - |
| 8 | 55 ± 18 | - | - |
| 9 | N.B. | - | - |
| 10 | N.D. | - | - |
| 11 | 221 ± 52 | - | - |
| 12 | 111 ± 6 | - | - |
| 13 | 271 ± 110 | + | - |
| 14 | N.D. | - | - |
| 15 | N.D. | - | - |
| 16 | >11000 | - | - |
| 17 | 558 ± 51 | + | - |
| 18 | 2100 ± 400 | - | - |
| 19 | 325 ± 24 | + | - |
| 20 | 549 ± 66 | - | - |
N.B – no binding observed, N.D. – Not determined due to reference cell binding
[a]
Average of at least 2 experiments. Errors represent the standard error of the mean.