Table 5.
Initial concentrations (µM) | Relative amount of different IN forms in equilibriuma (%) | |||||||
---|---|---|---|---|---|---|---|---|
Ligand | E0 | S0 | E | ES | E2S | E2S2 | E4S4 | Activationb (%) |
ss A5 | 40.0 | 10.4 | 18.7 | 70.1 | 0.6 | 0.7 | 9.9 | (Inhibitor) |
39.0 | 24.6 | 8.9 | 76.5 | 0.7 | 0.9 | 13.0 | ||
34.0 | 48.9 | 4.5 | 79.0 | 1.2 | 1.3 | 14.0 | ||
29.0 | 83.2 | 3.8 | 78.4 | 1.3 | 1.5 | 15.0 | ||
ds A21 · T21 | 40.0 | 0.17 | 19.0 | 69.4 | 0.7 | 0.9 | 10.0 | (Inhibitor) |
38.0 | 0.41 | 8.9 | 75.1 | 0.9 | 1.1 | 14.0 | ||
34.0 | 0.76 | 5.0 | 75.9 | 1.4 | 1.7 | 16.0 | ||
29.0 | 1.30 | 3.0 | 75.1 | 1.6 | 2.0 | 18.3 | ||
ss GCAGT | 40.1 | 30.8 | 18.7 | 66.8 | 0.5 | 0.6 | 9.8 | 40 |
37.9 | 72.7 | 9.0 | 76.5 | 0.7 | 0.9 | 12.9 | ||
34.7 | 133.3 | 5.1 | 77.7 | 1.2 | 1.3 | 14.7 | ||
29.8 | 228.6 | 3.0 | 80.7 | 1.0 | 1.1 | 14.3 | ||
ss 19-CA | 59.62 | 39.5 | 39.00 | 47.46 | 8.42 | 4.85 | 0.27 | 225 |
55.78 | 92.1 | 0.90 | 84.15 | 0.32 | 14.30 | 0.39 | ||
51.71 | 169.1 | 0.24 | 85.25 | 0.079 | 13.56 | 0.89 | ||
45.05 | 289.6 | 0.11 | 86.60 | 0.033 | 12.19 | 1.09 | ||
ss 21-GT | 61.78 | 31.3 | 53.60 | 37.4 | 4.87 | 4.17 | 0.024 | 100 |
53.77 | 73.0 | 0.093 | 82.0 | 0.017 | 17.50 | 0.370 | ||
49.70 | 143.0 | 0.012 | 83.1 | 0.002 | 16.58 | 0.300 | ||
43.30 | 229.0 | 0.005 | 84.76 | 0.007 | 15.00 | 0.220 | ||
ds 19-CA | 64.20 | 14.0 | 79.38 | 15.69 | 3.82 | 3.82 | ∼0.0 | 250c |
57.15 | 32.6 | 49.35 | 49.35 | 5.30 | 5.30 | 0.005 | ||
48.10 | 59.9 | 0.89 | 77.83 | 0.16 | 21.10 | 0.050 | ||
41.85 | 102.6 | 0.036 | 80.34 | 0.0055 | 19.60 | 0.024 | ||
ds 21-GT | 62.92 | 15.1 | 77.23 | 15.76 | 5.78 | 1.23 | ∼0.0 | 210c |
55.47 | 35.3 | 43.80 | 41.20 | 7.53 | 7.43 | ∼0.0 | ||
47.67 | 64.7 | 0.13 | 77.37 | 0.036 | 22.47 | 0.0016 | ||
41.54 | 110.8 | 0.014 | 79.38 | 0.0034 | 20.60 | 0.0012 |