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Summary of binding affinity and inhibitory potency data for aminoethyl-substituted CBIs
| R | TR-FRET assay (µM) | Reporter gene assay (µM) | Mammalian 2-hybrid assay (µM) | |
|---|---|---|---|---|
| NR Box II 15mer | n/a | 0.23 | n/a | n/a |
| 3a | propyl | >50 | >50 | >50 |
| 3b | butyl | 1.8 | 8.2 | 10.1 |
| 3c | pentyl | 1.7 | 3.2 | 3.2 |
| 3d | hexyl | 2.0 | 3.6 | 3.4 |
| 3e | neo-hexyl | 2.1 | 3.8 | 2.2 |
