Table 5 The summary and comparison of PROTACs targeting BRD
From: PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
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 |
