Table 5.
The summary and comparison of PROTACs targeting BRD
| No. | PROTAC | Warhead | E3 ligase |
|---|---|---|---|
| 1 | HBL-4(118) | BI2536 | CRBN |
| 2 | MacroPROTAC-1(119) | JQ1 | VHL |
| 3 | 120 | Benzo[cd]indol-2(1H)-one) derivative | CRBN |
| 4 | 121 | JQ1 | VHL |
| 5 | 122 | Dihydroquinazolinone derivative | CRBN |
| 6 | 123 | ABBV-075 | CRBN |
| 7 | 124 | JQ1 | CRBN |
| 8 | pc-PROTAC1(125) | JQ1 | CRBN |
| 9 | N2(126) | JQ1 | CRBN |
| 10 | 127 | JQ1 | CRBN |
| 11 | 128 | JQ1 | VHL |
| 12 | KB02-JQ1(129) | JQ1 | DCAF16 |
| 13 | DP1(130) | JQ1 | DCAF15 |
| 14 | MS83(131) | (+)-JQ1 | KEAP1 |
| 15 | SJ995973(132) | JQ1 | CRBN |
| 16 | XY-06-007(133) | JQ1 | CRBN |
| 17 | AGB1(134) | JQ1 | VHL |
| 18 | SIAIS629048(135) | JQ1 | CRBN |
| 19 | SIAIS629049(136) | JQ1 | CRBN |
| 20 | WWL0245(137) | WNY0824 | CRBN |