Table 8.
Comparison of activity versus WT and A934T SLACK for selected inhibitors
| No. | WT | A934T | ||
|---|---|---|---|---|
| IC50 (μM)a | Efficacy (%)a,b | IC50 (μM)a | Efficacy (%)a,b | |
|
| ||||
| 5 | 2.1 | 102 | 0.82 | 72 |
| 27 | 3.7 | 103 | 1.1 | 109 |
| 43 | 3.2 | 105 | 1.0 | 110 |
| 58 | 2.1 | 95 | 2.0 | 95 |
| 60 | 4.8 | 105 | 0.97 | 103 |
| 76 | 4.9 | 105 | 4.3 | 129 |
| 109 | 5.4 | 100 | 2.3 | 83 |
| 113 | 8.8 | 91 | 2.5 | 72 |
| 119 | 8.7 | 93 | 2.6 | 104 |
| 121 | 7.4 | 98 | 1.5 | 112 |
| 122 | 1.1 | 99 | 0.67 | 72 |
a
CRC from Tl+ flux assay in HEK-293 cells expressing either WT or A934T SLACK
b
Amplitude of response in the presence of 30 μM test compound as a percentage of the maximum response for VU0606170