Table 1.
Inhibition constants, relative inhibition potencies, and relative inhibition potencies per inhibitory unit of iminosugar clusters and monovalent references against JBα-man.
| Entry | Compound | Alkyl Chain Length | DNJ Unit | Kia (µM) | rp b | rp/n c |
|---|---|---|---|---|---|---|
| 1 | 3 [35] | C6 | 1 | 322 [35] | - | - |
| 2 | 4 [65] | C9 | 1 | 188 [65] | - | - |
| 3 | 7a | C6 | 6 | 7.7 ± 0.7 | 42 | 7 |
| 4 | 7b | C9 | 6 | 0.38 ± 0.01 | 495 | 82 |
| 5 | 6a | C6 | 8 | 80 ± 24 | 4 | 0.5 |
| 6 | 6b | C9 | 8 | 0.32 ± 0.05 | 588 | 73 |
| 7 | 7c | C9 | 18 | 0.092 ± 0.008 d 0.213 ± 0.042 |
2043 | 113 |
| 8 | 6c | C9 | 24 | 0.050±0.012 e | 3760 | 157 |
a Means ± SD obtained from experiments performed in triplicate; b Relative inhibition potency = Ki (monovalent reference 3 or 4)/Ki (cluster); c rp/n = rp/number of DNJ units; d mixed inhibition mode; e fast tight binding competitive inhibition mode.