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| |||||||
|---|---|---|---|---|---|---|---|
| Compound # | R | Binding affinity | Activity | ||||
| Ki (nM) | EC50 (nM) | ||||||
| SST1 | SST2A | SST3 | SST4 | SST5 | SST4 | ||
| 218 | (CH2)2NH2 | — | >10 000 | — | >10 000 | — | — |
| 221 a | (CH2)3NH2 | — | >10 000 | — | 2380a | — | — |
| 219 | (CH2)4NH2 | — | >10 000 | — | 653.4 | — | 1065 |
| 220 | (CH2)5NH2 | — | >10 000 | — | 3224 | — | — |
Ref. 58
