Integrin affinities of alkyne-functionalized peptide monomers. Values are expressed as 50% inhibition constants (IC50), and were used to calculate the IC50-based selectivities. Data for FF and YY have been reported previously33 and are given for the objective of comparison.
| Compound | IC50 (95% confidence interval) [nM] | αvβ6-selectivity over | |||||
|---|---|---|---|---|---|---|---|
| αvβ6 | αvβ8 | αvβ3 | α5β1 | αvβ8 | αvβ3 | α5β1 | |
| FF (ref. 33) | 0.17 (0.09–0.33) | 32 (20–51) | 424 (270–670) | 226 (115–193) | 188 | 2494 | 1329 |
| YF | 3.3 (2.4–4.4) | 23 (16–32) | 630 (341–1162) | 114 (82–158) | 6.9 | 190 | 35 |
| FY | 2.8 (2.1–3.7) | 37 (27–51) | 732 (486–1104) | 177 (138–227) | 13.2 | 261 | 63 |
| YY (ref. 33) | 0.84 (0.56–1.2) | 26 (19–37) | 219 (88–540) | 150 (116–193) | 31 | 261 | 179 |