Table 4.

Antiviral potencies in cell infected with HIV-1 containing wild-type or mutant integrase enzymes.^a

No.	CC50 (μM)b	EC50 (μM)c	SId	Integrase Mutantse
				Y143R	N155H	SHf
2	5.2	0.447	12	1x	2x	8x
5a-1	4.3	0.040	108	1x	19x	95x
5a-2	8.4	0.017	494	3x	57x	300x
5a-3	4.6	0.093	49	1x	68x	132x
5a-8	6.2	0.043	144	1x	44x	430x
5a-10	5.3	0.022	241	2x	23x	218x
5a-11	106.6	0.929	115	3x	ND	ND
5a-12	95.2	0.140	680	2x	272x	ND
5b-2	6.3	0.322	20	2x	12x	30x
5c-2	7.0	3.8	2	1x	4x	1x
5d-2	12.1	3.6	3	3x	2x	4x
5d-10	5.9	3.4	2	4x	2x	3x
5g-2	4.6	0.159	29	2x	10x	ND
5h-2	2.8	0.132	21	4x	16x	25x

^aAssays were performed as described in reference 25;

^bCytotoxic concentration resulting in 50% reduction in the level of ATP in human osteosarcoma (HOS) cells;

^cValues obtained from cells infected with lentiviral vector harboring WT IN;

^dSelectivity index calculated as the ration of CC₅₀ to EC₅₀;

^eCells were infected with viral constructs carrying IN mutantion as described in reference 25 and indicated values correspond to the fold-change in EC₅₀ relative to WT;

^fG140S-Q148H double mutant.