Table 1. Optimization of the Hinge and Ile regions.
Values for the TR-FRET, solubility, and permeability experiments are represented as means plus or minus standard deviation calculated from at least one experiment, run in triplicate. ND indicates values were not determined.
|
|
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|---|---|---|---|---|---|---|---|---|---|
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| |||||||||
| No | R1 | IC50 (μM) (TR-FRET) | Avg. Sol (μM) | Pampa (×10−6 cm/s) | No | R2 | IC50 (μM) (TR-FRET) | Avg. Sol (μM) | Pampa (×10−6 cm/s) |
| 1 |
|
7.6 ±1.0 | 32 ± 1.6 | 670 ± 100 | 23 |
|
>67 | 68 ± 3.4 | 1400 ± 250 |
| 13 |
|
4.0 ±0.18 | 44 ± 3.4 | 1200 ± 35 | 24 |
|
23 ±4.7 | ND | ND |
| 14 |
|
28 ±1.9 | 0.3 ±0.2 | 830 ± 1 | 25 |
|
>67 | 2.4 ± 0.1 | >2200 |
| 15 |
|
13 ±1.7 | 44 ± 1.4 | 1500 ± 1 | 26 |
|
44 ± 6.2 | ND | ND |
| 16 |
|
6.6 ± 0.32 | 35 ±8 | >2200 | 27 |
|
>67 | ND | ND |
| 17 |
|
33 ±0.11 | 0.7 ±0.6 | 1700 ± 1 | 28 |
|
>67 | ND | ND |
| 18 |
|
16 ±1.5 | 50 ± 2.7 | >2200 | 29 |
|
>67 | ND | ND |
| 19 |
|
19 ±1.9 | 14 ±0.7 | >2200 | 30 |
|
>67 | ND | ND |
| 20 |
|
25 ± 2.7 | 0.8 ±0.4 | 1300 ± 43 | 31 |
|
>67 | 1.0 ±0.6 | 930 ± 190 |
| 21 |
|
14 ±0.5 | 19 ± 1.2 | >2200 | 32 |
|
>67 | 78 ± 5.5 | >2200 |
| 22 |
|
>67 | 2.8 ± 0.8 | 910 ±290 | 33 |
|
>67 | 75 ± 0.6 | 220 ± 120 |