TABLE 1.
Discrimination values of nucleotide analogs by SARS-CoV-2 RdRp
| Nucleotide analog | Value (mean ± SD)a |
|
|---|---|---|
| D*analog | Dcalanalog | |
| ATP analogs | ||
| Remdesivir-TP | 0.78 ± 0.02 | |
| 6-Chloropurine-TP | 1 | 78.0 ± 3.5 |
| Clofarabine-TP | >1,439 | >112,242 |
| Ribavirin-TP | 320.5 ± 10.6 | 24,999 ± 828 |
| Tenofovir-DP | >1,439 | >112,242 |
| Favipiravir-TP | 94.1 ± 9.6 | 7,343 ± 752 |
| GTP | 111.3 ± 7.7 | 8,683 ± 600 |
| GTP analogs | ||
| 6-Thio-GTP | 10.6 ± 1.1 | |
| 2′-C-Methyl-GTP | 1 | 61.7 ± 9.0 |
| 6-Methylthio-GTP | 73.2 ± 14.3 | 4,516 ± 884 |
| Oxo-GTP | 37.6 ± 9.7 | 2,317 ± 600 |
| Remdesivir-TP | 1,786.4 ± 173.8 | 110,222 ± 10,726 |
| Favipiravir-TP | >2,319 | >143,089 |
| Ribavirin-TP | >2,319 | >143,089 |
| ATP | 55.5 ± 12.9 | 3,427 ± 797 |
| UTP analogs | ||
| 2′-Amino-UTP | 1 | 75 ± 5 |
| 2′-O-Methyl-UTP | 102.5 ± 5.1 | 7,688 ± 380 |
| 2′-Azido-UTP | 11.1 ± 0.5 | 831 ± 35 |
| ara-UTP | 8.3 ± 0.5 | 625 ± 40 |
| Stavudine-TP | 54.8 ± 6.7 | 4,109 ± 502 |
| Sofosbuvir-TP | 97.4 ± 4.9 | 7,307 ± 368 |
| Ribavirin-TP | 825.8 ± 131.2 | 61,933 ± 9,843 |
| CTP | 68.4 ± 8.6 | 5,131 ± 645 |
a
D*ATP analog = K1/2 ATP analog/K1/2, 6-chloropurine-TP; DcalATP analog = D*ATP analog × D6-chloropurine-TP; D*GTP analog = K1/2 GTP analog/K1/2, 2′-C-methyl-GTP; DcalGTP analog = D*GTP analog × D2′-C-methyl-GTP; D*UTP analog = K1/2 UTP analog/K1/2, 2′-amino-UTP; DcalUTP analog = D*UTP analog × D2′-amino-UTP. Data are from two independent experiments.