Compound | Activity in Screena | Concentration Response Curves | ||||||||
---|---|---|---|---|---|---|---|---|---|---|
Yeast [pEC50 (IA)] | BIND [pEC50] | Aequorin [pEC50 (IA)] | SPA pIC50 | |||||||
hGPR55 | rGPR55 | CB1 | hGPR55 | hGPR55 | α1A | GlyT1 | ||||
X | Y | |||||||||
GSK494581Ab | 4-F-Ph | 123 ± 7 | 6.5 (1.1) | <4.5 | <4.5 | 6.5 | 6.8 (1.1) | NT | 7.7 | |
GSK598945Ab | 4-F-Ph | 64 ± 6 | 5.4 (0.8) | <4.5 | <4.5 | 5.5 | 5.5 (1.3) | <4.4 | 8.2 | |
GSK553224Ab | 4-F-Ph | 11 ± 1 | 5 (1.0) | <4.5 | <4.5 | 5.7 | 4.9 (0.8) | <4.4 | 7.9 | |
GSK522373Ab | 4-F-Ph | 98 ± 3 | 6.2 (1.0) | <4.5 | <4.5 | 5.7 | 5.8 (1.3) | <4.4 | 7.1 | |
GSK452334Ab | Ph | 30 ± 1 | 5.2 (0.4) | NT | <4.5 | 6.1 | 5.7 (0.9) | <4.4 | 8.1 | |
GSK319199Ac | 68 ± 4 | 5.5 (0.8) | NT | <4.5 | 5.7 | 5.1 (0.4) | <4.4 | 7.2 | ||
GSK575594Ab | 4-F-Ph | NT | 6.8 (0.9) | <4.5 | <4.5 | NT | NT | NT | 5.0 |
IA, intrinsic activity; NT, not tested.
↵a Percent effect ± S.D.;