Characterization of the allosteric mechanism for hSERT mutants
| EC50 | Kd | |
|---|---|---|
| μM | nM | |
| hSERT WT | 7.0 (5.8–8.4) | 6.7 (5.4–8.0) |
| hSERT ALI/VFL | 45.2 (32–64) | N.D. |
| hSERT II/VT | 23.0 (19–27) | 5.1 (3.9–6.3) |
| hSERT MS/SN | 15.4 (14–17) | 4.6 (3.9–5.2) |
| hSERT SI/TT | 35.3 (26–48) | 6.8 (5.7–7.9) |
| hSERT VFL-II-SN-TT | 216.3 (126–372) | 11.3 (8.3–14.4) |
| hSERT ALI-VT-SN-TT | 396.5 (257–613) | 7.5 (4.3–10.8) |
| hSERT VFL-VT-SN-SI | 193.0 (146–255) | 6.6 (3.3–10.0) |
| hSERT VFL-VT-MS-TT | 532.3 (358–792) | N.D. |
| hSERT VFL-VT-SN-TT | 208.2 (169–256) | 16.9 (12.4–21.3) |
| hSERT VFL-II-SN-SI | 213.5 (176–259) | 10.2 (6.7–13.7) |
| hSERT ALI-VT-MS-TT | 207.7 (120–359) | 15.2 (12.3–17.7) |
| hSERT ALI-II-SN-TT | 47.1 (39–56) | 10.8 (8.4–13.2) |
| hSERT VFL-II-MS-TT | 483.8 (369–634) | 12.5 (6.5–18.5) |
| hSERT VFL-VT-MS-SI | 113.6 (89–145) | 14.1 (10.5–17.8) |
| hSERT A505V | 34.9 (24–51) | N.D. |
| hSERT L506F | 33.2 (20–56) | N.D. |
| hSERT I507I | 6.2 (5.2–7.3) | N.D. |
| hSERT I552V | 7.3 (5.8–9.4) | N.D. |
| hSERT I553T | 21.4 (14.6–31.4) | N.D. |
| hSERT M558S | 7.6 (6.5–8.8) | N.D. |
| hSERT S559N | 16.1 (11.6–22.4) | N.D. |
| hSERT S574T | 5.8 (4.3–7.8) | N.D. |
| hSERT I575T | 23.4 (19.7–27.9) | N.D. |
N.D., not determined.