Compound Strand Transfera 2LTR Circles in SupT1b Cytotoxicity in SupT1c Late RT in MT-2b Alu-LTR in MT-2b Cytotoxicity in MT-2c
IC50 (nM) MaximumFold-Change EC50 (nM) CC50 (nM) EC50 (nM) EC50 (nM) CC50 (nM)
GS-9224 55 ± 10 3.9 ↑ 9.5 2600 >100 2.8 1600
GS-9160 29 ± 3 2.3 ↑ 11 970 >100 1.8 4200
RAL 34 ± 5 2.4 ↑ 12 >100,000 >200 3.6 >100,000
EFV 0.2 ↓ 1.5 14000 3.5 1.3 >27,000
APV 1 ↔ 83000 >500 >500 >50,000
aMean ± SE of at least 4 independent experiments using IN enzyme.
b Mean of at least 2 independent experiments in HIV-1 infected SupT1 or MT-2 cells.
cMean of at least 4 independent experiments in uninfected SupT1 or MT-2 cells.
Table 3: Inhibition of Integrase Enzymatic Strand Transfer Activity and Integration in HIV-1 Infected SupT1 and MT-2 Cells.
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