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Effect of substitution of Gln-NHBn with glutamine mimics on peptidomimetics 3b, 4b, 5b, and 6b.a
| Xxx |
||||
|---|---|---|---|---|
 |
 |
 |
||
| Compound | βMpCinn-Leu-Pro-Xxx | 8 | 9 | 10 |
| KI (nM) | 144 ± 9 | 203 ± 32 | 94 ± 7 | |
| Compound | βMpCinn-Leu-mPro- Xxx |
11 | 12 | 13 |
| KI (nM) | 83 ± 10 | 193 ± 38 | 39 ± 10 | |
| Compound | βMpCinn-Nle-mPro-Xxx | 14 | 15 | 16 |
| KI (nM) | 66 ± 13 | 114±14 | 46 ± 6 | |
| Compound | PMpCinn-Haic-Xxx | 17 | 18 | 19 |
| KI (nM) | 105 ± 22 | 188 ± 13 | 386 ± 41 | |
KI values were determined by fluorescence polarization.27
