TABLE 2.

Comparison of IC₅₀ and IC₉₀ values of novel IN inhibitors by using biochemical and cell-based assays^a

^aStructures of compounds L-731,688 and RDS 1607 and the parental structure of derivatives of RDS 1624 to RDS 2164 are shown above the table.

^bIn vitro IC₅₀ values in 3′-processing and strand transfer reactions for the indicated DKA derivatives.

^cFor PBMC infections, HIV-1 p24 antigen release in the supernatant was quantified using an enzyme-linked immunosorbent assay kit. The IC₅₀ and IC₉₀ of each drug were determined by the median effect equation (7). Each condition was tested in five replicates.

^dFor 293 cell infections, cell-associated luciferase activity was evaluated on a 96-well white plate with a clear bottom. The IC₅₀ and IC₉₀ of each drug were determined by the median effect equation. Each condition was tested in three replicates.