Table 1.
GSK1440115 and GSK1562590 binding affinities to recombinant and native mammalian UT
| pKi | nH | n | |||||
|---|---|---|---|---|---|---|---|
| UT orthologue | GSK1440115 | GSK1562590 | GSK1440115 | GSK1562590 | GSK1440115 | GSK1562590 | Relative affinity |
| Mouse (recombinant) | 7.34 ± 0.07 | 9.34 ± 0.02 | 0.93 ± 0.04 | 1.47 ± 0.05 | 4 | 13 | 101-fold |
| Rat (recombinant) | 8.49 ± 0.25 | 9.66 ± 0.04* | 0.70 ± 0.09 | 0.95 ± 0.05 | 4 | 10 | 25-fold |
| Cat (recombinant) | 8.45 ± 0.15 | 9.64 ± 0.03† | 0.78 ± 0.05 | 1.39 ± 0.03 | 4 | 13 | 22-fold |
| Monkey (recombinant) | 7.53 ± 0.12 | 9.14 ± 0.03 | 0.94 ± 0.05 | 1.05 ± 0.03 | 4 | 13 | 48-fold |
| Human (recombinant) | 8.64 ± 0.06 | 9.28 ± 0.0† | 0.88 ± 0.02 | 1.07 ± 0.02 | 12 | 33 | 5-fold |
| Human (native; SJRH30) | 8.38 ± 0.11 | 9.46 ± 0.06 | 0.81 ± 0.08 | 1.09 ± 0.15 | 4 | 4 | 15-fold |
*
pKi > 9.79 observed in n= 5 additional experiments.
†
pKi > 9.79 observed in n= 2 additional experiments.
GSK1440155 and GSK1562590 consistently displaced the radioligand [125I]hU-II by 100%. All values are expressed as mean ± SEM.