Table 3.1.
Compounds 3.1–3.37: Chemical Class, Target, Developing Organization, Development Status
| Number | Chemical cpd./class | Target | Organization | Dev. status |
|---|---|---|---|---|
| 3.1a,b | Thioflavin S | Hsp70–BAG-1 | Cancer Research, UK | DD |
| 3.2 | Pifithrin-m, PES | Hsp70, plus others | University of Pennsylvania | LO |
| 3.3 | Gambogic acid, GA | Hsp70–, Hsp90–CHIP regulation | Jangsu University, China | TM |
| 3.4 | Methylene blue, MB | Hsp70–CHIP regulation | TauRX Therapeutics | Ph III |
| 3.5 | Apoptozole | Hsp70, ATPase inhib. | Yonsei University, South Korea | LO |
| 3.6 | Nutlin-3 | HDM2–p53 | Roche | Ph I |
| 3.7 | Serdemetan | HDM2–p53 | Johnson & Johnson | Ph I |
| 3.8 | AT-406 | IAPs | Ascenta | Ph I |
| 3.9 | GDC-0152 | IAPs | Genentech | Ph I |
| 3.10 | LCL-161 | IAPs | Novartis | Ph II |
| 3.11 | TL32711 | IAPs | Tetralogic | Ph II |
| 3.12 | Diamines, compound A | Skp2 | University of North Carolina | DD |
| 3.13 | Alkylidene thiazolidines, compound C1 | Skp2 | NY University | DD |
| 3.14 | Diacids, SKP-I2 | Cdc4 | Mount Sinai Hosp., Toronto, Canada | DD |
| 3.15 | Benzodiazepindiones, LS-101 | Synoviolin | Tokyo Medical Univ. | LO |
| 3.16 | Triazines, LS-102 | RING E3 ligases | Tokyo Medical Univ. | LO |
| 3.17 | Tetracycles, SMER3 | Met30 | UCLA | LO |
| 3.18 | Thalidomide | Cereblon | Tokyo Institute of Technology | Ph III |
| 3.19 | Curcumin | Pan-DUB inhibition | University of Utah | TM |
| 3.20 | Shikoccin | Pan-DUB inhibition | University of Utah | DD |
| 3.21 | Δ12-PGJ2 | Pan-DUB inhibition | Karolinska Institute | DD |
| 3.22 | Dienones, NSC 632839 | Pan-DUB inhibition | Progenra | DD |
| 3.23 | Bis-isothiocyanate, PR-419 | Pan-DUB inhibition | Oldenburg University, Germany | DD |
| 3.24a,b | Tricyclic dinitriles, HBX-41,108 (3.24a) | USP DUBs | Hybrigenics | LO |
| 3.25 | Gold complexes | Pan-DUB inhibition | University of Hong Kong | DD |
| 3.26 | Tyrposthin-like WP-1130 | USP5, USP9x, USP14, UCH-L1, UCH37 | University of Michigan | LO |
| 3.27 | Alkyliden-pyrazolidindiones, PYR41 | Cys DUBs | University of Michigan | DD |
| 3.28 | Betulinic acid | Pan-DUB inhibition | University of Miami | PE |
| 3.29 | Chalcones, RA-9 | UPS2, UPS5, UPS8, UCH-L1, UCH-L3 | University of Minnesota | DD |
| 3.30 | Phthalimide based, pimozide | UAF1, USP7 | University of Delaware | DD |
| 3.31 | Spautin-1 | USP10, USP13 | Chinese Academy of Sciences | DD |
| 3.32 | Thiophene based, P5091 | USP7, USP47 | Harvard Med. School | LO |
| 3.33 | Thiophene based | USP7, USP47 | Progenra | LO |
| 3.34 | Aminotetrahydroacridines, HBX-19,818 | USP7 | Hybrigenics | Ph I |
| 3.35 | Naphthylamides, GRL0617 | PLpro | University of Illinois | LO |
| 3.36 | Electrophilic dienones, NSC687852/b-AP15 | USP14 | Karolinska Institute | LO |
| 3.37 | Pyrrole based, IU1 | USP14 | Harvard Med. School | LO |
Not progressed, NP; early discovery, DD; lead optimization, LO; preclinical evaluation, PE; clinical Phase I-II-III, Ph I–Ph III; marketed, MKTD; traditional medicine, TM. Please note that the most advanced status for NDD-targeted experiments is listed: for example, candidates in clinical trials for non-CNS indications with early in vitro characterization against proteinopathies/tauopathies are classified as DD.