Table 1.
Radioligand binding and functional activities of UNC9975, UNC0006, and UNC9994 at select GPCRs
| Binding affinity or potency, nM* | ||||
| Receptor/assay | Aripiprazole | UNC9975 | UNC0006 | UNC9994 |
| D2/binding (Ki) | 8.0 | 2.6 | 5.0 | 79 |
| D1/binding (Ki) | 895 | 1,040 | 825 | 4,000 |
| D3/binding (Ki) | 19 | 11 | 16 | 17 |
| D4/binding (Ki) | 251 | 178 | 200 | 138 |
| D5/binding (Ki) | 1,051 | 513 | 615 | >10,000 |
| 5HT2A/binding (Ki) | 40 | 7.4 | 16 | 140 |
| 5HT2A/FLIPR (pA2) | 417 | 102 | 331 | 6,600 |
| 5HT2B/binding (Ki) | 1.4 | 1.1 | 0.6 | 25 |
| 5HT2B/FLIPR (IC50) | 98 | 76 | 115 | 501 |
| 5HT2C/binding (Ki) | 250 | 99 | 115 | 512 |
| 5HT2C/FLIPR (EC50) | 1,900 | 324 | 363 | 1,550 |
| 5HT1A/binding (Ki) | 18 | 29 | 60 | 26 |
| 5HT1A/cAMP (EC50) | 450 | 1,800 | 2,500 | 933 |
| H1/binding (Ki) | 6.0 | 6.1 | 4.5 | 2.4 |
| H1/FLIPR (pA2) | 52 | 35 | 22 | 79 |
*Ki, IC50, pA2, or EC50 values are the average of at least two duplicate experiments with SD values that are threefold less than the average.