LDK1229 binding to the T210A, wild-type, and T210I CB1 receptors using [3H]CP55,940 as a tracer
| Kia | ||||
|---|---|---|---|---|
| CP55,940 | Ki Ratiob | LDK1229 | Ki Ratiob | |
| nM | ||||
| CB1 T210A | 7.00 (2.59–18.9) | 1:3 | NB | — |
| CB1 wild type | 2.56 (1.45–4.51)c | 1:1 | 220 (106–457) | 1:1 |
| CB1 T210I | 0.835 (0.542–1.29) | 3:1 | 5831 (907–7510) | 1:27 |
NB, no binding using up to 32 μM of LDK compound.
↵a Data are the median and corresponding 95% confidence limits of three independent experiments performed in duplicate. Ki values were determined from competition binding assays using [3H]CP55,940 as tracer at its respective Kd values, as described in Results.
↵b Wild type:mutant.
↵c Binding values are from Ahn et al. (2009) for comparison.