Extended Data Table 2.
Binding affinities for different P2Y12R constructs. Affinity values of the agonist [3H]2MeSADP determined in saturation binding to WT and mutant P2Y12Rs expressed transiently in COS7 cells (a) and inhibition by antagonist AZD1283 (b).
| a | |
|---|---|
|
| |
| Constructs | [3H]2MeSADP(Kd, nM) |
| WT | 4.9±1.3 |
| S83A | 5.6±1.4 |
| C97A | N.S. |
| R256A | 16.1±6.2 |
| C175A | N.S. |
| K280A | N.S. |
| b | |
|---|---|
|
| |
| Constructs | AZD1283 (Ki, nM) |
| WT | 41.8±16.3 |
| S83A | 36.5±6.8 |
| R256A | 140±39 |
Footnote: Results are expressed as mean ± SEM from 3-6 independent experiments performed in duplicate by methods described in Zhang et al5. N.S., not saturable or negligible specific binding within the radioligand concentrations used (0.4-46 nM).