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. 2021 Apr 19;65(5):e02406-20. doi: 10.1128/AAC.02406-20

TABLE 1.

Structure and antiviral activity of INSTIs in the MT-2 cell line

INSTIa Structure Antiviral activity against HIV-1, EC50 (nM)b (fold change)
WT G140S+Q148H
BIC graphic file with name AAC.02406-20-f03a.jpg 1.5 ± 0.2 3.1 ± 0.8 (2.1)
DTG graphic file with name AAC.02406-20-f03b.jpg 1.5 ± 0.2 6.5 ± 1.2 (4.3)
RAL graphic file with name AAC.02406-20-f03c.jpg 9.4 ± 1.4 2,461 ± 323 (262)
EVG graphic file with name AAC.02406-20-f03d.jpg 2.1 ± 0.9 868 ± 138 (413)
Compound 1 graphic file with name AAC.02406-20-f03e.jpg 1.4 ± 0.5 4.5 ± 1.8 (3.2)
Compound 2 graphic file with name AAC.02406-20-f03f.jpg 1.5 ± 0.5 11.1 ± 0.5 (7.4)
a

All compounds were synthesized at Gilead Sciences, Inc.

b

EC50, 50% effective concentration.