Table 2. EC50 and efficacy in yeast and HEK 293 cells for RXR variants.
| 9cRA
|
LG335
|
|||||||
|---|---|---|---|---|---|---|---|---|
| Yeast
|
HEK 293
|
Yeast
|
HEK 293
|
|||||
| Variant | EC50 | Eff | EC50 | Eff | EC50 | Eff | EC50 | Eff |
| WT | 500 | 100 | 220 | 100 | >10,000 | 10 | 300 | 10 |
| I268A;I310A;F313A;L436F | >10,000 | 0 | >10,000 | 0 | 220 | 70 | 30 | 50 |
| I268V;A272V;I310L;F313M | >10,000 | 10 | >1600 | 30 | 40 | 60 | 1 | 30 |
| I268A;I310S;F313V;L436F | >10,000 | 10 | — | — | 470 | 60 | — | — |
| I268A;I310S;F313A;L436F | >10,000 | 0 | >10,000 | 0 | 430 | 50 | 690 | 20 |
| I268V;A272V;I310M;F313S;L436M | >10,000 | 10 | >10,000 | 0 | 680 | 30 | 180 | 30 |
| I268A;A272V;I310A;F313A;L436F | >10,000 | 0 | — | — | 530 | 30 | — | — |
| I268L;A271V;I310L;F313L | >10,000 | 0 | — | — | 530 | 20 | — | — |
| I268A;I310M;F313A;L436T | >10,000 | 0 | >10,000 | 0 | 610 | 10 | 140 | 20 |
| I268V;A271V;I310L;F313V | >10,000 | 0 | — | — | 650 | 10 | — | — |
| I268L;I310V;F313I | >10,000 | 0 | — | — | >2000 | 10 | — | — |
| I268L;I310M;F313V | >10,000 | 20 | — | — | 610 | 20 | — | — |
| I268V;I310V;F313S | >10,000 | 0 | — | — | 440 | 10 | — | — |
EC50 values (given in nm) represent the averages of two screen experiments in quadruplicate for yeast and in triplicate for HEK 293. Efficacy (Eff; given as a percent) is the maximum increase in activation relative to the increase in activation of wild type with 10 μM 9cRA. Values represent the averages of two screen experiments in quadruplicate for yeast and in triplicate in HEK 293.