TABLE 1.

Some properties of the NNRTI used in this study

DrugIC50 (nM)aEC50 (nM)bType of inhibitionc
Clinical
    Nevirapine200 ± 4545 ± 10REI
    Delavirdine5.4 ± 0.42.8 ± 1.4REI
    Efavirenz7.7 ± 0.91.7 ± 0.2TBI
Experimental
    UC84117 ± 4240 ± 70REI
    UC7811.7 ± 1.210 ± 0.2TBI
    CSIC2.0 ± 0.21.2 ± 0.4TBI
  • a IC50 is the concentration of inhibitor that provides a 50% reduction in the RDDP activity of recombinant wild-type p51/p66 RT determined by measurement of this activity in the presence of various concentrations of inhibitor using [3H]dGTP and poly(rC)-oligo(dG)12-18 as described in Materials and Methods. Values are the means ± standard deviations of three independent measurements, each carried out in duplicate.

  • b EC50 is the concentration of inhibitor that provides a 50% reduction in HIV-1 infection of MT2 cells, assessed as described in Materials and Methods. Values are the means ± standard deviations of three independent measurements, each carried out in triplicate.

  • c Inhibition of HIV-1 RT in vitro: REI, rapid equilibrium inhibitor; TBI, tight-binding inhibitor.