TABLE 3.
Compound | R | IC50 (nM)a
|
Fold increase in IC50 | |
---|---|---|---|---|
Wild type | Mutant | |||
GS 4071 | 0.2 | 6,500 | 32,500 | |
GS 4047 | 0.7 | 8,500 | 12,145 | |
GS 4048 | 0.8 | 22,500 | 28,125 | |
GS 3768 | 60 | 14,000 | 235 | |
GS 4926 | 290 | 21,000 | 70 | |
GS 4993 | 750 | 44,500 | 60 | |
GS 4093 | 21 | 17,500 | 835 | |
GS 4383 | 0.09 | 6,500 | 72,220 | |
Data shown are average values from two independent experiments using 50 μM MUNANA as substrate.