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Binding affinities of Smac mimetics to XIAP, cIAP-1 and cIAP-2, as determined in competitive, fluorescence-polarization based assays (assays details provided in SI). Data were obtained using 3-5 independent experiments.
| Cpds | Ki ± SD (nM) | ||
|---|---|---|---|
| XIAP | cIAP-1 | cIAP2 | |
| 1 | 26 ± 4 | 1.0 ± 0.3 | 1.8 ± 0.6 |
| 2 | 20.0 ± 14.5 | 1.2 ± 0.1 | 4.6 ± 1.5 |
| 3 | 341 ± 65.9 | 3.3 ± 1.3 | 17.5 ± 4.3 |
| 4 | 91.8 ± 30.4 | 3.7 ± 1.4 | 9.8 ± 4.1 |
| 5 | 5.4 ± 3.0 | 1.3 ± 0.3 | 1.9 ± 0.8 |
| 6 | 8.4 ± 1.6 | 1.5 ± 0.5 | 4.2 ± 0.6 |
