Hit compounds selected for DR assays and their corresponding IP
| Category . | Name . | Reported main target . | IP . |
|---|---|---|---|
| Kinases | Danusertib | Aurora | 0.3125 μM |
| TWS119 | GSK3 | 0.0390 μM | |
| SF2523r | PI3K/mTOR | 0.625 μM | |
| NCB-0846 | TNIK | 0.625 μM | |
| XMD16-5 | TNK2 | 2.5 μM | |
| Receptors | BNTX | δ₁-opioid | 2.5 μM |
| NVP-BVU972 | c-Met | 1.875 | |
| AMG 337 | c-Met | 5 μM | |
| Poziotinib | EGFR | 2.5 μM | |
| Naquotinib | EGFR | 5 μM | |
| LY2874455 | FGFR | 0.625 μM | |
| PD 161570 | FGFR | 0.3125 μM | |
| Gilteritinib | FLT3 and AXL | 1.25 μM | |
| BMS 536924 | IR and IGF1R | 0.1562 μM | |
| MGCD-265 | Met, FLT-1, FLT-4, FK-1, RON | 2.5 μM | |
| Tivozanib | VEGFR | 1.25 μM | |
| IMR-1 | Notch | 2.5 μM | |
| Others | WS3 | EBP1 | 2.5 μM |
| WS26 | EBP1 | 2.5 μM | |
| SBI-0640756 | eIF4G1 | 1.25 μM | |
| Edoxaban | Factor Xa | 1.25 μM | |
| Apixaban | Factor Xa | 0.625 μM | |
| 4μ8C | IRE1α | 2.5 μM | |
| MCB-613 | Steroid receptor coactivator | 2.5 μM | |
| Phosphodiesterases | Milrinone | PDE | 0.0781 μM |
| Anagrelide | PDE | 0.0195 μM | |
| Zardaverine | PDE | 0.1562 μM | |
| IBMX | PDE | 0.039 μM | |
| Ubiquitin pathway | PR 619 | DUB | 1.25 μM |
| Degrasyn (WP1130) | DUB | 0.1562 μM | |
| VLX1570 | DUB (USP14) | 1.25 μM | |
| NSC 697923 | E2 ubiquitin ligase (UBE2N) | 0.625 μM | |
| SMER 3 | E3 ubiquitin ligase | 0.1562 μM |
| Category . | Name . | Reported main target . | IP . |
|---|---|---|---|
| Kinases | Danusertib | Aurora | 0.3125 μM |
| TWS119 | GSK3 | 0.0390 μM | |
| SF2523r | PI3K/mTOR | 0.625 μM | |
| NCB-0846 | TNIK | 0.625 μM | |
| XMD16-5 | TNK2 | 2.5 μM | |
| Receptors | BNTX | δ₁-opioid | 2.5 μM |
| NVP-BVU972 | c-Met | 1.875 | |
| AMG 337 | c-Met | 5 μM | |
| Poziotinib | EGFR | 2.5 μM | |
| Naquotinib | EGFR | 5 μM | |
| LY2874455 | FGFR | 0.625 μM | |
| PD 161570 | FGFR | 0.3125 μM | |
| Gilteritinib | FLT3 and AXL | 1.25 μM | |
| BMS 536924 | IR and IGF1R | 0.1562 μM | |
| MGCD-265 | Met, FLT-1, FLT-4, FK-1, RON | 2.5 μM | |
| Tivozanib | VEGFR | 1.25 μM | |
| IMR-1 | Notch | 2.5 μM | |
| Others | WS3 | EBP1 | 2.5 μM |
| WS26 | EBP1 | 2.5 μM | |
| SBI-0640756 | eIF4G1 | 1.25 μM | |
| Edoxaban | Factor Xa | 1.25 μM | |
| Apixaban | Factor Xa | 0.625 μM | |
| 4μ8C | IRE1α | 2.5 μM | |
| MCB-613 | Steroid receptor coactivator | 2.5 μM | |
| Phosphodiesterases | Milrinone | PDE | 0.0781 μM |
| Anagrelide | PDE | 0.0195 μM | |
| Zardaverine | PDE | 0.1562 μM | |
| IBMX | PDE | 0.039 μM | |
| Ubiquitin pathway | PR 619 | DUB | 1.25 μM |
| Degrasyn (WP1130) | DUB | 0.1562 μM | |
| VLX1570 | DUB (USP14) | 1.25 μM | |
| NSC 697923 | E2 ubiquitin ligase (UBE2N) | 0.625 μM | |
| SMER 3 | E3 ubiquitin ligase | 0.1562 μM |
EBP1, ErbB3-binding protein 1; EGFR, epidermal growth factor receptor; FGFR, fibroblast growth factor receptor; FLT3, FMS-like tyrosine kinase 3.