TABLE 3.
Focused compound selection (version 5)
| Target | Drug name | Clinical status |
|---|---|---|
| RNA transcription initiation | Triptolide | Phase I |
| HDAC‐pan | Panobinostat* | Phase III |
| 20S Proteasome | Bortezomib | Phase III |
| mTORC1,2 | INK128/sapanisertib/tak228 | Phase I/II |
| HDAC1/2/3/10, PI3K | Cudc907 | Phase I/II |
| CDK1/2/4/6/9 | At7519 | Phase I/II |
| Proteasome | Ixazomib | Phase III |
| STAT 4 | Napabucasin | Phase III |
| HSP90 | Cudc305 | Phase I |
| AKT, ERK | Onc201 | Phase I/II |
| ALK, BMP | Ldn‐212854 | preclinical |
| ATF1/CREB | 666‐15 | preclinical |
| ATR | Azd6738 | Phase I/II |
| Beta‐blocker | Propranolol HCL | Phase I/II |
| B‐Raf | Vemurafenib | Phase I/II |
| BRD2,3,4 and BRD‐T | Gsk525762/i‐bet‐762 | Phase I/II |
| BRD4, PI3k | Ly294002 | preclinical |
| BRD4, PLK1, TAF1, TAF1L, CBP, P300 | Bi2536 | Phase I/II |
| CDC25a; iron chelation | Ciclopirox | FDA approved |
| CDK 4/6 | Ribociclib | Phase III |
| CDK8/19, Wnt | Cct251545 | preclinical |
| CENP‐E | Gsk923295 | Phase I |
| CHK1/2 | Prexasertib/LY2606368 | Phase I/II |
| c‐MET, ALK | Crizotinib | Phase III |
| CPB, CREBBP/EP300 | Sgc‐cbp30 | preclinical |
| CRM‐1/XPO‐1 | Selinexor | Phase III |
| EGFR (allosteric inhibitor) | Eai045 | preclinical |
| EGFR‐PI3K | Mtx‐211 | preclinical |
| EZH2 | Tazemetostat | Phase I/II |
| FGFR1‐4 | Ly2874455 | Phase I |
| HDAC1/2, EGFR, HER2 | Cudc101 | Phase I |
| HDAC1/3 | Entinostat | Phase III |
| IAP | Cudc427 | preclinical |
| IGF1R | Bms‐754807 | Phase I/II |
| IKBKE | Amlexanox | Phase II |
| JAK1/2 | Ruxolitinib | Phase III |
| JMJD | Gsk‐j4 | preclinical |
| JAK1/2, TBK, IKKε | Cyt387 | Phase III |
| LSD1 | Sp‐2509 | preclinical |
| MCL‐1 | S63845 | preclinical |
| Mdm2 | Amg232 | Phase I/II |
| MEK1/2 | Cobimetinib | Phase III |
| MITF | Ml329 | preclinical |
| Mitochondrial energy metabolism | Cpi‐613 | Phase III |
| mTOR | Sirolimus/rapamycin | Phase 4 |
| mTOR, PI3K | BKM120/buparlisib | Phase I/II |
| Multiple RTK, PDGFR, SRC, EphB4 | Dasatinib | Phase I/II |
| Multiple RTK, VEGFR, PDGFR, RAF | Sorafenib | Phase III |
| p300 | C646 | preclinical |
| PI3Ka/d, NFkB | Pictilisib | Phase I/II |
| PIM 1‐2‐3‐ Kinase | Azd1208 | Phase I |
| Proton pump | Esomeprazole | FDA approved |
| ROCK | Fasudil | Phase III |
| S100A9; microenvironment | Tasquinimod | Phase III |
| S100B | Pentamidine | Phase I/II |
| TAR RNA‐binding protein 2 | Enoxacin/penetrex | FDA approved |
| TNFa induction | Dmxaa | Phase III |
| TP53 (mutant) | Apr‐246 | Phase III |
| pan‐TrkA/B/C, ROS1, ALK | Entrectinib | Phase II |
| TrkA, TrkB, TrkC | Larotrectinib | FDA approved |
| Wee1 | MK‐1775/adavosertib | Phase I/II |
*
is used a a positive control.