TABLE 4.
CHIKV inhibitors identified in in vitro biochemical assay/assays with purified proteina
| Compound | Viral target | Resistance mutation(s) | Confirmed in infected cells? |
In vitro efficacy |
In vivo efficacy |
Reference or source | |||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| CHIKV strain (genotype) | EC50 (μM) | CC50 (μM) | Cell line | CHIKV strain (genotype) | Efficacy | Mouse model | |||||
| 5-Iodotubercidin (NA) | nsP1 | — | Yes | Clinical isolate 119067 | 0.409 | >50 | Vero | — | — | — | 66 |
| lobaric acid | nsP1 | — | Yes | LR2006 OPY1 (ECSA) | 9.9 ± 2.6 | 76.3 ± 2.1 | BHK | — | — | — | 67 |
| Sinefungin | nsP1 | — | Yes | CHIKV LS3 | 184.9 ± 38.4 | >1,000 | VeroE6 | — | — | — | 66, 122; unpublished datab |
a
For compounds identified using in silico approaches, only those compounds for which the antiviral activity was demonstrated in cell culture using infectious CHIKV are reported; all other compounds for which activity was claimed against CHIKV from in silico screens, but for which no activity in cell-based assays was reported, are excluded from this table. —, not determined/not done (in vivo studies).
b
K. Kovacikova, M. G. Gonzalez, J. Reguera, Eric J. Snijder, Gerard J. P. van Westen, and Martijn J. van Hemert, unpublished data.