From: Enhanced A3 adenosine receptor selectivity of multivalent nucleoside-dendrimer conjugates
Compound | A1 Ki (nM) | A2A Ki (nM) | A3 Ki (nM) |
---|---|---|---|
Nucleoside Monomers | |||
1 | 10.4 ± 3.8 | 370 ± 100 | 12.2 ± 4.1 |
4 d | 30 ± 9 | 800 ± 360 | 74 ± 20 |
7 d | 43 ± 5 | 300 ± 20 | 9.5 ± 2.0 |
Dendrimer Derivatives | |||
11 | NBb | (20 ± 7%)c | (26 ± 3%)c |
12 | 21 ± 5 | 250 ± 40 | 27 ± 2 |
13 | 55 ± 10 | 405 ± 170 | 42 ± 17 |
15 | NBb | NBb | NBb |
16 | 175 ± 60 | 610 ± 110 | 14.0 ± 2.1 |
17 d | 320 ± 20 | 470 ± 50 | 2.4 ± 0.4 |