TABLE 5.

Antiviral activity of GSK’254 against SDMs in single-cycle and multiple-cycle assays

Assay type and virus	GSK’254			GSK’795
	Mean ± SD EC50, μM	FC-EC50	MPI, %	Mean ± SD EC50, μM	FC-EC50	MPI, %
Single-cycle assay
Wild type	0.003 ± 0.002	1.0	98	0.005 ± 0.003	1.0	94
V370A	0.002 ± 0.001	0.7	97	0.006 ± 0.000	1.2	84
V370M	0.002 ± 0.001	0.7	93	0.013 ± 0.011	2.6	78
ΔV370	0.008	2.7	96	0.110	2.2	60
T33N/V370A	0.003	1.0	94	0.030	6.0	70
V362I	0.003 ± 0.001	1.0	89	0.014 ± 0.006	2.8	68
M367V	0.015 ± 0.010	5.0	89	>3	>600	36
V362I/V370A	0.004 ± 0.001	1.3	91	>3	>600	31
V362I/V370M	0.004 ± 0.002	1.3	90	>3	>600	51
V362I/H219Q	0.007 ± 0.002	2.3	91	0.066	13.2	60
H358Y/ΔT371	0.035 ± 0.002	11.7	67	>3	>600	18
I333V/V370A	0.011 ± 0.001	3.7	86	>3	>600	10
I333V/V370	0.011 ± 0.001	3.7	86	>3	>600	−36
I333V/V362I	0.039 ± 0.005	13.0	65	>3	>600	−30
T332N/V370A	0.004 ± 0.001	2.2	94	0.030	7.6	70
T332S/V362I/prR41G	0.013 ± 0.009	4.3	88	>3	>600	−30
V362I/H219Q/T332S	0.008 ± 0.003	2.7	91	0.71	142	52
R361K/V362I/L363M	0.014 ± 0.002	4.7	89	>3	>600	36
A364V	>3	>1,000	45	>3	>600	8
A366V	>3	>1,000	−7.6	>3	>600	3
V362I/A366V	>3	>1,000	−96	>3	>600	−109
A366V/V370M	>3	>1,000	26	>3	>600	3
V362I/A366V/V370M	>3	>1,000	1	>3	>600	−62
Multiple-cycle assay
Wild type	0.003 ± 0.002	1.0	98	0.005 ± 0.003	1.0	94
V370A	0.002 ± 0.001	0.7	97	0.006	1.2	84
ΔV370	0.003 ± 0.001	1.0	96	0.006 ± 0.002	1.2	87
V362I/V370A	0.003 ± 0.001	1.0	91	>3	>600	31
T332S/V362I/prR41G	0.007 ± 0.004	2.3	97	0.704 ± 0.606	141	65
A326T/V362I/V370A	0.026 ± 0.070	8.7	69	>3	>600	6
R361K/V362I/L363M	0.003 ± 0.001	1.0	91	0.552 ± 0.971	110.4	68
A364V	0.274 ± 0.505	91	70	>3	>600	16
A366V-containing virusesa	>3	>1,000	−86 to 400	>3	>600	−13 to 408

^aIncludes genotypes A366V, V362I/A366V, V362I/A366V/V370M, and A366V/V370M.