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Activity of KEAP1 PROTACs against the KEAP1-Kelch domain.
| Cmpd | Linker | X | IC50 (SD) μMa |
|---|---|---|---|
| 2 | – | – | 0.077 (0.003) |
| 3 |  |
NH | 0.150 (<0.001) |
| 4 |  |
NH | 0.267 (0.012) |
| 5 |  |
O | 0.223 (0.006) |
| 6 |  |
O | 0.147 (0.006) |
| 7 |  |
O | 0.143 (0.012) |
| 8 |  |
O | 0.066 (0.006) |
| 9 |  |
O | 0.086 (0.002) |
| 10 |  |
O | 0.127 (0.006) |
| 11 |  |
NH | 0.120 (<0.001) |
| 12 |  |
O | 0.563 (0.029) |
| 13 |  |
O | 0.059 (0.001) |
IC50 (SD) values represent 3 independent experiments against recombinant KEAP1-Kelch domain in a HTRF biochemical assay.
