Table 4.
Single Cell Line Selective Compounds with Nanomolar Potency
| Compound Name | FDA Approved | Compound Class | Target | Avg SI | Avg IC50 (μM) |
|---|---|---|---|---|---|
| PA-1 | |||||
| Mycophenolate mofetil | Yes; 2008 | Immunosuppressant; prodrug | Inosine monophosphate dehydrogenase | >100 | 0.631 |
| Pirarubicin | No; in clinical trials | Antineoplastic; anthracycline | DNA intercalater | 14.6 | 0.839 |
| Gimatecan | No; in clinical trials | Antineoplastic; quinolone akaloid | Topoisomerase I | 12.5 | 0.0337 |
| PHA-793887 | No; in clinical trials | Antineoplastic | CDK2/1/4/9; GSK3β | 12.3 | 0.194 |
| Doxorubicin | Yes; 1993 | Antineoplastic; anthracycline | DNA intercalater | 7.02 | 0.576 |
| TOV-21-G | |||||
| Neratinib | Yes; 2017 | Antineoplastic | EGFR/Her2/Her4; P-glycoprotein | >100 | 0.619 |
| Milciclib | No; in clinical trials | Antineoplastic | CDK; tropomyosin receptor kinase | 50.1 | 0.0897 |
| HeLa | |||||
| LY2874455 | No; in clinical trials | Antineoplastic | Pan-FGFR | 38.8 | 0.240 |
| AZD3463 | No | Antineoplastic | ALK/IGFR | 30.3 | 0.638 |
| NVP-TAE684 | No | Antineoplastic | ALK | 28.0 | 0.835 |
| TAK 901 | No; completed clinical trials | Antineoplastic | Aurora Kinase | 12.6 | 0.699 |
Table shows compound name, FDA approval status, compound class, target, average selectivity, and average IC50 (μM). IC50 values are the mean of the cell line shown. Selectivity >100 indicates drug was “inactive” in HEK293T cells with efficacy <50%.