Table 1.
Sample | Ki (nM) (n =3) | EC50 (nM) (n = 3 and 4) | Emax(% of U50,488H) |
---|---|---|---|
3a | >1000 | — | — |
4a | >1000 | — | — |
5a | 422± 44 | 1966 ± 94 | 87 |
6a | 198 ± 43 | 648 ± 152 | 92 |
3b | 197 ± 14 | 539 ± 50 | 77 |
4b | 167 ± 6.5 | 673 ± 111 | 112 |
5b | 42.3 ± 3.3 | 282 ± 8.5 | 90 |
6b | 245 ± 14 | 239 ± 23 | 46 |
6c | 51.6 ± 0.9 | 266 ± 40 | 124 |
4c | 24.3 ± 0.9 | 83.3 ± 10.9 | 103 |
5c | >1000 | — | |
1 | 7.5 ± 1.7 | 106 | |
U50,488H | 1.2 ± 0.3 | 6.3 ± 0.7 | 100 |