MK-2048 is a potent inhibitor of HIV-1 integrase (IN) and IN mutant R263K with IC50 of 2.6 nM and 1.5 nM, respectively.
MK-2048 inhibits subtype B and subtype C integrase activities with IC50 of 75 nM and 80 nM, respectively.
MK-2048 inhibits S217H intasome with an IC50 of 900 nM, remains fully active against the N224H intasome with IC50 of 25 nM.
MK-2048 displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor.
