Table 2.
| |||||
---|---|---|---|---|---|
Cmpd | R | R1 | R2 | MrgX1 EC50, μMa | Emax (%)a |
4a | Me | H | 0.531 ± 0.16 | 238 ± 63 | |
4b | Me | H | 3.06± 1.50 | 188 ± 7 | |
4c | Me | H | 0.42 ± 0.33 | 130 ± 28 | |
4d | Me | H | Inactive | ND | |
4e | Me | H | 1.01± 0.19 | 180 ± 9 | |
4f | Me | H | 2.34± 1.30 | 241 ± 25 | |
4g | Me | Me | 0.50± 0.12 | 184 ± 14 | |
4h | Me | Me | Inactive | ND | |
4i | Me | Me | 0.55±0.17 | 149 ± 19 | |
4j | Ph | H | Inactive | ND | |
4k | Ph | H | Inactive | ND |
Assay was run in the presence of 10 nM of BAM8-22; n = 2, N.D.: not determined since Emax is too low.