Table 3.
Comparison of affinity of MEN16132 and a series of derivatives substituted in the place of the tetrahydropyranyl group (X) at the wild type and W86A mutant human B2 receptor
| Compound | i.d. compound1 | X | Ki wild type (nM) | Ki W86A mutant (nM) | Fmut |
|---|---|---|---|---|---|
| MEN16132 | 72 |  |
0.4 (0.3–0.6) | 713 (340–1500) | 1782 |
| MEN15880 | 63 |  |
1 (0.7–1.3) | 650 (330–1320) | 650 |
| MEN16318 | 70 |  |
12 (8–20) | 2860 (750–5000) | 238 |
| MEN16298 | 68 |  |
3.4 (1.8–6.3) | 808 (330–1975) | 237 |
| MEN16303 | 69 |  |
13 (11–16) | 525 (200–2400) | 40 |
Fmut index was calculated as Ki (mutant receptor)/Ki (wild type receptor), and corresponds to fold decrease in affinity.
1
Compound i.d. from Fattori et al. (2007).