MK-0536

MK-0536 (0.6 nM-37 μM; 2 h) potently inhibits both strand transfer and 3'-processing activities of wild-type HIV-1 integrase in vitro, with an IC₅₀ of 33 nM for strand transfer and 5.8 μM for 3'-processing^[1].
MK-0536 (0.6 nM-37 μM; 2 h) is hypersensitive against HIV-1 integrase^Y143R, inhibiting strand transfer with an IC₅₀ of 9.5 nM and 3'-processing with an IC₅₀ of 1.4 μM^[1].
MK-0536 (0.6 nM-37 μM; 2 h) retains potent activity against HIV-1 integrase, inhibiting strand transfer with an IC₅₀ of 40 nM and 3'-processing with an IC₅₀ of 3.9 μM^[1].
MK-0536 (0.6 nM-37 μM; 2 h) exhibits reduced but still significant activity against HIV-1 integrase, inhibiting strand transfer with an IC₅₀ of 237 nM and 3'-processing with an IC₅₀ of 8.3 μM^[1].
MK-0536 inhibits wild-type HIV-1 replication in HOS cells with an EC₅₀ of 17 nM and is non-cytotoxic to HeLa cells at concentrations up to 333 μM^[1].

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