Characterization of compounds in cyclase and FLIPR functional assays
Mean EC50 (nM)*, Emax Relative to CP 55,940; 95% Confidence Interval of EC50 (nM) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Cyclase Assays | FLIPR Assays | ||||||||||
| hCB2 | hCB1 | rCB2 | rCB1 | rCB2 | rCB1 | ||||||
| A-836339 | 0.42, 100% | 740, 100% | 0.42, 73% | 1200, 130% | 5.3, 60% | 440, 82% | |||||
| 0.14–1.3 | 430–1300 | 0.090–2.0 | 850–1600 | 3.1–9.2 | 83–2400 | ||||||
| A-796260 | 0.71, 78% | 980, 120% | 2.5, 70% | 290, 97% | 31, 39% | 1800, 78% | |||||
| 0.32–1.6 | 620–1600 | 0.86–7.2 | 210–400 | 7.9–120 | 880–3900 | ||||||
| JWH-015 | 46, 96% | 1100, 94% | 8.9, 63% | 500, 100% | 1100, 58% | 51% at 10,000 | |||||
| 30–72 | 450–2800 | 4.2–19 | 260–960 | 550–2000 | |||||||
| AM1241 | >1800 | 2700, 101% | >1000 | 2000, 81% | >10,000 | >22,000 | |||||
| 1700–4100 | 840–4600 | ||||||||||
| GW-842166X | 460, 96% | 4300, 89% | 100, 89% | >25000 | N.D. | >10,000 | |||||
| 120–1800 | 1600–12,000 | 48–217 | |||||||||
| L-768,242 (GW405833) | 29, –21% | 950, 80% | 2.9, –62% | 560, 76% | N.D. | >10,000 | |||||
|
| 9.5–86 | 580–1600 | 1.6–5.4 | 200–1600 |
|
| |||||
N.D., not determined; N.A., not applicable
↵* All EC50 values are derived from at least three studies performed in duplicate