Table 11. Functional mGlu5 Activity in the Nicotinamide Series.
entry | n | X | A | R | mGlu5 IC50 (nM) |
---|---|---|---|---|---|
171 | 1 | H | CH | Cl | 310 |
172 | 0 | H | CH | Cl | 5400 |
173 | 2 | H | CH | Cl | 250 |
174 | 3 | H | CH | Cl | 2300 |
175 | 1 | H | CH | H | ∼10 000 |
176 | 1 | H | CH | F | 2300 |
177 | 1 | H | CH | Me | 2300 |
178 | 1 | H | CH | OMe | 1800 |
179 | 1 | H | N | Me | 420 |
180 | 1 | Cl | CH | Cl | 95 |
181 | 1 | Cl | N | Me | 87 |