Table 3.
| ||
---|---|---|
Compound | Ar | hM5 Percent inhibition |
4 (VU0549108) | 1,3,5-TriMe-1H-4-pyrazole | 88% (hM5 IC50 = 6.18 μM) |
9a | 1-Me-1H-4-pyrazole | 27% |
9b | 1,3-DiMe-1H-4-pyrazole | Inactive |
9c | 1,5-DiMe-1H-4-pyrazole | 83% |
9d | 3-Cl-4-F-phenyl | 83% |
9e | 3,5-DiF-phenyl | 62% |
9f | 3,4,5-TriF-phenyl | 55% |
9g | 3,5-DiMe-4-isoxazole | 40% |
9h | 1-Me-4-imidazole | Inactive |
Average of three determinations with hM5 cells with an EC80 of ACh as a single point % inhibition at 10 μM. If not IC50 reported, the IC50 was >10 μM.