Table 6.
Binding affinities1 of 20, CJ-1639 and pramipexole for inhibiting radioligand binding to the indicated drug targets as determined in the PDSP screen.
| Target | Compound | Target | Compound | ||||
|---|---|---|---|---|---|---|---|
| 20 (Ki, nM) | CJ-1639 (Ki, nM) | Pramipexole (Ki, nM) | 20 (Ki, nM) | CJ-1639 (Ki, nM) | Pramipexole (Ki, nM) | ||
| 5HT1A | 2,108 | 708 | 6514 | D3 | 1240 | 30 | 0.9 |
| 5HT1B | NA | NA | 3508 | D4 | NA | 45 | 29 |
| 5HT1D | NA | NA | >10,000 | D5 | NA | NA | >10,000 |
| 5HT1E | NA | NA | >10,000 | DAT | NA | 205 | NA |
| 5HT2A | NA | 2,841 | NA | DOR | NA | NA | >10,000 |
| 5HT2B | 674 | 1,178 | NA | GABAA | NA | NA | ND |
| 5HT2C | 5,997 | 762 | NA | H1 | NA | 110 | NA |
| 5HT3 | NA | NA | >10,000 | H2 | NA | 224 | 2,683 |
| 5HT5A | NA | NA | >10,000 | H3 | NA | 893 | NA |
| 5HT6 | NA | NA | >10,000 | H4 | NA | NA | >10,000 |
| 5HT7 | NA | 770 | 1,188 | KOR | NA | >10,000 | NA |
| Alpha1A | NA | NA | >10,000 | M1 | NA | NA | >10,000 |
| Alpha1B | NA | 666 | NA | M2 | NA | NA | >10,000 |
| Alpha1D | NA | 1,184 | NA | M3 | NA | NA | >10,000 |
| Alpha2A | >10,000 | NA | 75.7 | M4 | NA | 2,279 | NA |
| Alpha2B | N/A | NA | 67.7 | M5 | NA | 2,297 | NA |
| Alpha2C | 2,841 | NA | 52.2 | MOR | NA | 745 | NA |
| Beta 1 | 77 | NA | NA | NET | NA | 436 | NA |
| Beta 2 | NA | ND | >10,000 | PBR | NA | NA | ND |
| Beta 3 | NA | NA | >10,000 | SERT | NA | 32 | NA |
| BZP site | NA | NA | ND | Sigma 1 | 383 | 531 | 4,446 |
| D1 | NA | NA | >10,000 | Sigma 2 | 2,750 | N/A | NA |
| D2 | NA | 3,902 | 743.7 | ||||
1
Ki (nM) values for the indicated compounds were determined as described in the Experimental Section.
NA indicates inhibition of binding was <50% in the primary assay conducted using a single 10 μM concentration.