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Binding Affinities of Peptidomimetics Combining Favorable Groups at the Ala1 and Ala3 Positions
| ||||||
|---|---|---|---|---|---|---|
| Compound | R1 | R2 | R3 | R4 | IC50 ± SD (nM) | Ki ± SD (nM) |
| ARA |
|
−H | −H |
|
540 ± 30 | 120 ± 10 |
| 6a |
|
|
−H |
|
5 ± 1 | <1 |
| 6b |
|
|
|
36 ± 5 | 8 ± 2 | |
| 6c |
|
|
−H |
|
6 ± 0.4 | <1 |
| 6d |
|
−H |
|
5 ± 1 | <1 | |
| 6e |
|
|
32 ± 7 | 6 ± 2 | ||
| 6f |
|
−H |
|
9 ± 1 | 1 ± 0.3 | |
| 6g |
|
|
|
80 ± 14 | 16 ± 3 | |
