Table 3.
The Efficacy Scores of Compounds 178–258
| 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 |
|---|---|---|---|---|---|---|---|---|---|---|---|
| 183 | – | – | 2.5 | 1.43 | 0.789 | 223 | 4% | 1.56 | 17.0 | 0.94 | 0.538 |
| 184 | 1% | 1.67 | 224 | 2% | 1.39 | ||||||
| 185 | – | – | 225 | 5% | 1.29 | ||||||
| 186 | 3% | 1.73 | 226 | 4% | 1.30 | ||||||
| 187 | 3% | 1.69 | 227 | 10% | 1.02 | ||||||
| 188 | – | – | 228 | – | – | ||||||
| 189 | 3% | 0.62 | 229 | 24% | 0.05 | ||||||
| 190 | – | – | 230 | – | – | ||||||
| 191 | – | – | 231 | – | – | ||||||
| 192 | – | – | 232 | 70% | |||||||
| 193 | 1% | 1.01 | 1.3 | 1.27 | 0.748 | 233 | 9% | 1.40 | 18.6 | 0.63 | 0.443 |
| 194 | 0% | 1.70 | 234 | 8% | 1.09 | ||||||
| 195 | 1% | 1.40 | 235 | 8% | 0.95 | ||||||
| 196 | 1% | 1.46 | 236 | 12% | 0.85 | ||||||
| 197 | 0% | 1.73 | 237 | 13% | 0.68 | ||||||
| 198 | – | – | 238 | 25% | 1.21 | ||||||
| 199 | 1% | 1.57 | 239 | 29% | – | ||||||
| 200 | – | – | 240 | 34% | – | ||||||
| 201 | – | – | 241 | 11% | 0.16 | ||||||
| 202 | 5% | 0.05 | 242 | 37% | – | ||||||
| 203 | 2% | 1.14 | 8.2 | 1.40 | 0.734 | 243 | – | – | 25.0 | 0.65 | 0.413 |
| 204 | 2% | 1.48 | 244 | 9% | 1.48 | ||||||
| 205 | 1% | 1.56 | 245 | 10% | 1.13 | ||||||
| 206 | 2% | 1.56 | 246 | 36% | – | ||||||
| 207 | 2% | 1.39 | 247 | 45% | – | ||||||
| 208 | 3% | 1.58 | 248 | – | – | ||||||
| 209 | 2% | 1.88 | 249 | – | – | ||||||
| 210 | 3% | 1.82 | 250 | – | – | ||||||
| 211 | 64% | – | 251 | – | – | ||||||
| 212 | 1% | 1.62 | 252 | – | – | ||||||
| 213 | – | – | 3.0 | 1.16 | 0.697 | 253 | 21% | 1.33 | |||
| 214 | 3% | 0.94 | 254 | 53% | – | ||||||
| 215 | 2% | 0.87 | 255 | 53% | – | ||||||
| 216 | 3% | 1.70 | 256 | 49% | – | ||||||
| 217 | 4% | 1.11 | 257 | 45% | – | ||||||
| 218 | – | – | 258 | 27% | – | ||||||
| 219 | – | – | 259 | 54% | – | ||||||
| 220 | – | – | 260 | 50% | – | ||||||
| 221 | – | – | 261 | 11% | 0.49 | ||||||
| 222 | – | – | 262 | 83% | – |
Notes: Efficacy scores are calculated from % F.F.ave and P.S.ave. Compounds with % F.F. values of <25% fibril formation are included in the plasma selectivity assay as the P.S. values are lower than those of their parent compound 182 (% F.F. values of 26%). Higher efficacy scores correspond to more potent and selective inhibitors.