Table 2.
The Efficacy Scores of Compounds 142–181
| Compounds | % F.F. | P.S. | % F.F.ave | P.S.ave | Efficacy Scores | Compounds | % F.F. | P.S. | % F.F.ave | P.S.ave | Efficacy Scores |
|---|---|---|---|---|---|---|---|---|---|---|---|
| 142 | 12% | 0.13 | 7.8 | 0.66 | 0.510 | 162 | 80% | – | 33.3 | 0.40 | 0.312 |
| 143 | 17% | 0.11 | 163 | 44% | – | ||||||
| 144 | 1% | 0.98 | 164 | 8% | 0.31 | ||||||
| 145 | 1% | 1.41 | 165 | 1% | 1.30 | ||||||
| 146 | 28% | – | 11.5 | 0.87 | 0.492 | 166 | 77% | – | 42.8 | 0.25 | 0.238 |
| 147 | 15% | 0.10 | 167 | 9% | 0.02 | ||||||
| 148 | 2% | 1.10 | 168 | 79% | – | ||||||
| 149 | 1% | 1.47 | 169 | 6% | 0.96 | ||||||
| 150 | 71% | – | 22.0 | 0.73 | 0.450 | 170 | 83% | – | 55.0 | 0.30 | 0.195 |
| 151 | 14% | 0.30 | 171 | 41% | – | ||||||
| 152 | 2% | 0.84 | 172 | 85% | – | ||||||
| 153 | 1% | 1.78 | 173 | 11% | 1.19 | ||||||
| 154 | 70% | – | 30.0 | 0.62 | 0.377 | 174 | 88% | – | 80.3 | 0.15 | 0.152 |
| 155 | 48% | – | 175 | 70% | – | ||||||
| 156 | 3% | 0.88 | 176 | 81% | – | ||||||
| 157 | 1% | 1.58 | 177 | 2% | 0.58 | ||||||
| 158 | 47% | – | 29.5 | 0.41 | 0.331 | 178 | 89% | – | 62.5 | 0 | 0.125 |
| 159 | 8% | 0.13 | 179 | 43% | – | ||||||
| 160 | 61% | – | 180 | 92% | – | ||||||
| 161 | 2% | 1.51 | 181 | 26% | 0.41 |
Notes: Efficacy scores are calculated from % F.F.ave and P.S.ave. Compounds with % F.F. values of >20% fibril formation are exclusive in the plasma selectivity assay as they are assigned with P.S. values of 0. Higher efficacy scores correspond to more potent and selective linkers.