Table 2.
Deubiquitinating enzyme–targeted drug candidates.
| Name | Target(s) | Efficacy | References |
|---|---|---|---|
| PR-619 | ATXN3, BAP1, JOSD2, OTUD5, UCH-L1, UCH-L3, UCH-L5/UCH37, USP1, 2, 4, 5, 7, 8, 9X, 10, 14, 15, 16, 19, 20, 22, 24, 28, 47, 48, VCIP135, YOD1, PLpro, DEN1, SENP6 | EC50: 1–20 μM | (113) |
| P5091 (P005091) | USP7, 47 | EC50: 4.2 μM, 4.3 μM | (114, 115) |
| P22077 | USP7, 47 | EC50: 8 μM | (113, 116) |
| HBX41108 | USP7 | IC50: 0.27 μM | (117) |
| HBX19818 | USP7 | IC50: 28.1 μM | (118) |
| HBX28258 | USP7 | IC50: 22.6 μM | (118) |
| 9-oxo-9H-indeno [1,2-b]pyrazine-2,3-dicarbonitrile | USP7, USP8 | IC50: 3.5 μM, 0.29 μM | (119) |
| b-AP15 | UCHL5 | IC50: 2.1 μM | (120) |
| VLX1570 | USP14, UCHL5 | EC50: 29 nM | (121) |
| Degrasyn (WP1130) | USP5, USP9X, USP14, UCH37 | IC50: 1-5 μM | (122, 123) |
| IU1 | USP14 | IC50: 4.7 μM | (124) |
| pimozide | USP1/UAF1 | IC50: 2 μM | (125) |
| GW7647 | USP1/UAF1 | IC50: 5 μM | (125) |
| Isatin O-acyl oxime derivatives (30, 50, 51) | UCHL1, UCHL3 | IC50: 0.80-0.94 μM, 17-25 μM | (126) |
| AZ1 | USP25, USP28 | IC50: 0.62 μM, 0.7 μM | (127) |
| ML364 | USP2, USP8 | IC50: 1.1 μM, 0.95 μM | (128) |
| ML323 | USP1-UAF1 | IC50: 76 nM | (129) |
| TCID | UCH-L3 | IC50: 0.6 μM | (126) |
| Vialinin A | USP4, USP5 | IC50: 1–25 μM | (130) |
| XL188 | USP7 | IC50: 90–190 nM | (131) |
| Chalcone derivatives (AM146, RA-9, RA-14) | DUB | IC50: 1-13 μM | (132) |
| GRL0617 | PLpro | EC50: 10–15 μM | (133) |