Table 2.
Compound | R1 | R2 | R3 | EC50 (μM) | Relative Vmax (%)* |
---|---|---|---|---|---|
D001 | OMe | H | 2-chlorobenzene | 15 | 90 |
D003 | OMe | H | 4-pyridine | >30 | 1 |
D010 | OMe | H | 4-fluorobenzene | 3.6 | 24 |
D012 | OMe | H | 3,4,5-trimethoxybenzene | >30 | 3 |
D018 | OMe | H | 2-chloro-4-fluoro-benzene | 2.4 | 92 |
D025 | OMe | H | 3-methyl-4-nitro-benzene | >30 | 3 |
D035 | OMe | H | >30 | 1 | |
D036 | OMe | H | 3-nitro-4-chloro-benzene | >30 | 11 |
D038 | OMe | H | 2-chloro-4-nitro-benzene | 1.7 | 100 |
D086 | OMe | H | >30 | 3 | |
D123 | OMe | H | 0.3 | 100 | |
D136 | Me | H | 4-fluorobenzene | 18 | 11 |
D138 | H | OMe | 2-chloro-4-nitro-benzene | 3.4 | 21 |
*100% Vmax corresponds to 20 μM ASP-11.