TABLE 2.

EC₅₀ fold changes for inhibition of recombinant HIV-1 virus replication by BI 224436^a

Test compound	EC50 fold change in inhibition of:
	Active-site integrase inhibitor-resistant mutant				NCINI-resistant mutant				NNRTI-resistant mutant
	N155S	G140S/Q148H	T66I/S153Y	E92Q	A128T	A128N	L102F	N222K	K103N/Y181C
BI 224436	1.0	1.2	0.5	1.0	2.9	64	61	2.8	0.9
Elvitegravir	77	NA	81	16	1.1	0.9	1.1	1.6	0.5
Raltegravir	8.5	290	0.4	3.1	0.9	1.0	1.0	1.0	0.7

^aShown are EC₅₀ fold changes for inhibition by BI 224436 of replication of recombinant HIV-1 viruses containing mutations that confer resistance to either NNRTIs or the active-site inhibitors raltegravir and elvitegravir. Single or double point mutations were introduced into the HXB2 integrase-containing virus, which was used to infect the C8166 LTR luciferase reporter cell line. The EC₅₀s were calculated in a minimum of three separate experiments with the mean fold shift in EC₅₀ calculated relative to the EC₅₀ of the wild-type virus.