Table I. Kinase inhibitors tested for HCMV inhibition. List of kinase inhibitors and their target(s). The stage of clinical testing is listed for those drugs currently in clinical trials. Inhibition of HCMV replication (IC50 values) was determined using the pp28-GFP assay (N.D. = drug does not reach 50% inhibition at concentrations tested). Cellular toxicity (LD50 values) was determined by LDH assay in uninfected primary human fibroblasts.
| Drug name | Target | Clinical stage | IC50 | LD50 |
|---|---|---|---|---|
| OTSSP167 | MELK | Phase I/II | 5.4 nm | 98 nm |
| Dinaciclib | CDK1, 2, 5, 9 | Phase 3 | 20 nm | >10 μm |
| OTX015 | BRD2,3,4 | Phase 1 | 8.4 μm | >10 μm |
| LY2603618 | Chk1 | 10 μm | >10 μm | |
| Tivantinib | c-Met | Phase 3 | >10 μm | >10 μm |
| Alisertib | AURKA | Phase 3 | >10 μm | >10 μm |
| Saracatinib | c-Src, v-Abl, lyn | Phase 1/2 | >10 μm | >10 μm |
| BMS-777607 | c-Met, Axl, Ron, TYRO3 | Phase 1/2 | >10 μm | >10 μm |
| Sotrastaurin | PKC (pan) | Phase 1/2 | >10 μm | >10 μm |
| TG003 | CLK1,2,4 | >10 μm | >10 μm | |
| SBI-0206965 | ULK1/2 | >10 μm | >10 μm | |
| PF-03814735 | AURKA, AURKB Flt1, FAK, TrkA | Phase 1 | N.D. | 1.7 μm |
| UNC2025 | MERTK | N.D. | 1.2 μm | |
| MRT67307 | IKK(epsilon), TBK1 | N.D. | 1.1 μm |