Impact of 1-C linker to the indole, identifying SAR contributions.
| |||||||
|---|---|---|---|---|---|---|---|
| Compound # | X | Binding affinity | Activity | ||||
| Ki (nM) | EC50 (nM) | ||||||
| SST1 | SST2A | SST3 | SST4 | SST5 | SST4 | ||
| 213 | — | — | >10 000 | — | 99.4 | — | 401.9 |
| 180 | H | 1518 | >10 000 | >10 000 | 1.7 | >10 000 | 2.0 |
| 190 | 3,4-Cl2 | — | 3697 | — | 0.8 | — | 0.3 |
| 192 | 3,5-Cl2 | — | 5111 | — | 1.2 | — | 1.3 |
| 186 | 2-Cl | — | >10 000 | — | 2.6 | — | 3.1 |
| 187 | 3-Cl | 1235 | 4000 | 4398 | 0.5 | >10 000 | 0.1 |
| 189 | 4-Cl | 624.4 | 7693 | 4072 | 1.4 | >10 000 | 1.3 |
| 183 | 4-F | 1156 | >10 000 | >10 000 | 1.7 | >10 000 | 1.8 |
| 198 | 2-OCH3 | — | 6303 | — | 0.7 | — | 1.9 |
| 200 | 3-OCH3 | — | 9185 | — | 0.5 | — | 0.5 |
| 202 | 4-OCH3 | 2576 | >10 000 | >10 000 | 2.2 | >10 000 | 7.3 |
| 195 | 3-CF3 | 587.6 | >10 000 | 2335 | 0.8 | >10 000 | 0.6 |
| 205 | 3-CN | — | >10 000 | — | 7.1 | — | 10.7 |
| 207 | 3-SO2CH3 | 660.7 | >10 000 | >10 000 | 1.0 | >10 000 | 3.3 |
| 209 | 4-SO2CH3 | — | >10 000 | — | 58.8 | — | 169.2 |