TABLE 2.
Summary of in vitro Ki values for displacement of 3H-NMS binding from human recombinant M1–M5 mAChRs
Ki values for LSN3172176, xanomeline, and GSK1034702 were derived from IC50 values, as described in Materials and Methods, from the data shown in Fig. 3. Values in parentheses indicate the fold-selectivity vs. the M1 mAChR.
| Compound | mAChR Subtype, Ki (nM) |
||||
|---|---|---|---|---|---|
| M1 | M2 | M3 | M4 | M5 | |
| LSN3172176 | 8.9 | 63.8 (7.2) | 3031 (341) | 41.4 (4.7) | 55.6 (6.2) |
| Xanomeline | 23.1 | 54.8 (2.4) | 40.0 (1.7) | 16.1 (0.7) | 26.4 (1.1) |
| GSK1034702 | 959.9 | 5674 (5.9) | 61,570 (64) | 2261 (2.4) | 10,090 (10.5) |