Table. 1 Calcium mobilization and PRESTO-Tango assay screening
From: Discovery of a β-arrestin-biased CCKBR agonist that blocks CCKBR-dependent long-term potentiation
Drug | Calcium signaling assay | PRESTO-Tango assay | Biased factor \(\beta\) | ||||
|---|---|---|---|---|---|---|---|
EC50(nM) | % CCK8s maximal response | N | EC50(nM) | % CCK8s maximal response | N | ||
CCK8s | 4.08 ± 2.09 | 100.00 ± 0.90 | 4 | 4.57 ± 0.46 | 100.00 ± 16.27 | 4 | 0 |
CCK8 | 4.55 ± 0.47 | 98.52 ± 3.40 | 4 | 1.56 ± 0.70 | 98.12 ± 12.11 | 3 | 0.51 |
CCK4 | 7.68 ± 1.37 | 101.70 ± 3.90 | 5 | 8.13 ± 1.35 | 112.55 ± 9.78 | 3 | 0.07 |
MF-1 | > 20000 | 83.34 ± 7.25 | 4 | 316.40 ± 31.68 | 76.49 ± 3.01 | 4 | Nil |
MF-2 | > 20000 | 34.26 ± 2.05 | 5 | 18748 ± 379.3 | 38.08 ± 4.28 | 4 | Nil |
MF-3 | > 20000 | 55.50 ± 5.41 | 4 | 7412.00 ± 234.80 | 46.09 ± 5.96 | 3 | Nil |
MF-4 | > 20000 | 71.63 ± 11.29 | 3 | 1209.00 ± 13.88 | 73.09 ± 5.80 | 4 | Nil |
MF-5 | 7741 ± 977.8 | 64.92 ± 12.44 | 4 | 1074.00 ± 77.41 | 101.9 ± 4.45 | 5 | Nil |
MF-6 | Nil | Nil | 6 | Nil | Nil | 3 | Nil |
MF-7 | 476.50 ± 97.50 | 108.60 ± 4.55 | 6 | 2.61 ± 0.11 | 102.10 ± 10.00 | 5 | 2.20 |
MF-8 | 516.00 ± 93.15 | 66.34 ± 1.91 | 5 | 4.54 ± 0.71 | 86.83 ± 5.20 | 4 | 2.27 |
MF-9 | 3470.00 ± 915.90 | 120.70 ± 6.83 | 6 | 80.35 ± 1.76 | 110.40 ± 10.48 | 4 | 1.84 |
MF-10 | 3628.00 ± 1098.99 | 81.54 ± 9.13 | 4 | 300.20 ± 10.57 | 95.46 ± 14.19 | 5 | 1.20 |
MF-11 | 337.70 ± 52.57 | 109.60 ± 12.42 | 7 | 82.83 ± 6.49 | 99.60 ± 9.04 | 4 | 0.77 |
MF-12 | 205.10 ± 25.46 | 108.10 ± 4.70 | 4 | 4.28 ± 0.02 | 114.10 ± 13.77 | 4 | 1.75 |
MF-13 | 124.20 ± 10.00 | 98.75 ± 10.50 | 6 | 6.84 ± 0.59 | 98.01 ± 4.46 | 5 | 1.30 |
