Table 1.
Comparison of potency estimates in radioligand binding and functional studies
| Compound | Binding potency | Functional pIC50 | Reference |
|---|---|---|---|
| KN62 | 7.6 | 7.5 | Hibell et al. (2001) |
| OxATP | 3.8–4.8a | 5.4 | Hibell et al. (2001) |
| BBG | 6.2 | 6.9 | Hibell et al. (2001) |
| P2X7 mABb | 0.07 μg ml−1 | 0.1–0.2 μg ml−1 | Buell et al. (1998) |
| 0.03 μg ml−1 | Michel et al. (2000) | ||
| Decavanadate | 7.0 | 7.4 | Michel et al. (2006a) |
| PPADS | 5.6–6.2a | 7.3 | Hibell et al. (2001) |
| SB-203580 | 5.6 | 6.2–4.8 | Michel et al. (2006b) |
| SB-224435 | <5 | <5 | Michel et al. (2006b) |
The binding data are pIC50 values except for oxATP, PPADS and the P2X7 mAb.
a
For oxATP and PPADS, pEC50 values to reverse the inhibitory effect of various concentrations of ATP are shown. The functional data are pIC50 values from BzATP-stimulated ethidium bromide cellular accumulation studies conducted in the absence of NaCl and presence of sucrose buffer.
b
For the P2X7 mAb, the binding data are the IC50 values and the functional data an effective concentration range to block BzATP-induced interleukin-1β release from THP1 cells (Buell et al., 1998) or the IC50 to inhibit BzATP-induced ethidium bromide accumulation in HEK293-P2X7 cells (Michel et al., 2000).