EC50 | n | Fmut | IC50 | n | Fmut | ||
---|---|---|---|---|---|---|---|
nM | nM | ||||||
1 | rPKPfQwFwLL-NH2 | 18 ± 2 | 11 | 1.0 | 3.2 ± 0.7 | 4 | 1.0 |
2 | PKPfQwFwLL-NH2 | 25 ± 9 | 5 | 1.4 | 2.2 ± 0.4 | 3 | 0.7 |
3 | KPfQwFwLL-NH2 | 44 ± 3 | 4 | 2.4 | 17.0 ± 3 | 3 | 5.3 |
4 | PfQwFwLL-NH2 | 61 ± 23 | 3 | 3.4 | >1000.0 | 4 | >310 |
5 | fQwFwLL-NH2 | 29 ± 9 | 8 | 1.6 | 17.0 ± 4 | 3 | 5.3 |
6 | QwFwLL-NH2 | 990 ± 90 | 4 | 55.0 | 120.0 ± 30 | 4 | 38.0 |
7 | wFwLL-NH2 | >1000a | 5»55.0 | 530.0 ± 230 | 4 | 170.0 | |
8 | rPKPAQwFwLL-NH2 | 350 ± 50 | 3 | 19.0 | 68.0 ± 20 | 3 | 21.0 |
9 | rPKPfAwFwLL-NH2 | 32 ± 1 | 3 | 1.8 | 10.0 ± 3 | 3 | 3.1 |
10 | rPKPfQAFwLL-NH2 | >1000 | 3 | >55.0 | >1000 | 3 | >310 |
11 | rPKPfQwAwLL-NH2 | 310 ± 40 | 3 | 17.0 | 64.0 ± 5 | 3 | 20.0 |
12 | rPKPfQwFALL-NH2 | >1000 | 3 | >55.0 | >1000 | 3 | >310 |
13 | rPKPfQwFwAL-NH2 | >1000 | 3 | >55.0 | 110.0 ± 40 | 3 | 34.0 |
14 | rPKPfQwFwLA-NH2 | 31 ± 6 | 3 | 1.7 | 19.0 ± 3 | 4 | 5.9 |
15 | rPKPfQWFwLL-NH2 | 210 ± 6 | 3 | 12.0 | 97.0 ± 25 | 3 | 30.0 |
16 | rPKPfQwFWLL-NH2 | >1000 | 3 | >55.0 | 150.0 ± 19 | 3 | 47.0 |
17 | rPKPFQwFwLL-NH2 | 23 ± 5 | 4 | 1.3 | 4.3 ± 0.5 | 3 | 1.3 |
18 | rPKPyQwFwLL-NH2 | 12 ± 3 | 4 | 0.7 | 3.9 ± 1.8 | 3 | 1.2 |
19 | rPKPwQwFwLL-NH2 | 11 ± 4 | 3 | 0.6 | 11.0 ± 2 | 3 | 3.4 |
20 | rPKP QwFwLL-NH2 | 52 ± 14 | 4 | 2.9 | 26.0 ± 3.5 | 3 | 8.1 |
21 | KPfQwFwL -NH2 | >1000 | 3 | >55.0 | 38.0 ± 13 | 3 | 12.0 |
22 | KPfQwFw -NH2 | >1000 | 3 | >55.0 | 150.0 ± 30 | 3 | 47.0 |
↵ a The dose-responds curve is biphasic, composed of a partial agonist component at 10 nM concentration and after partial inverse agonism.