Table 4.
Inhibition of [3H]SB-657510 binding to monkey UT-HEK293 cell membranes by nonpeptide sulphonamide antagonists (SB-706375 and SB-657510) and native U-II isopeptides
KD (nM) | Bmax (fmol mg−1 protein) | |
---|---|---|
Saturation binding | ||
[3H]SB-657510 | 2.6±0.4 | 860±120 |
Ki (nM) | nH | |
Competition binding | ||
SB-706375 | 4.6±1.3 | 0.99±0.05 |
SB-657510 Ki | 17.6±5.4 | 0.89±0.03 |
Human U-II Ki | 11.4±3.3 | 1.16±0.15 |
Goby U-II Ki | 14.6±4.3 | 0.96±0.12 |
All values are represented as mean±s.e.m. (n=3–4, duplicate determinations).