Table 1 Summary table showing compound name, binding affinity, and functional activity
A2A | A2B | |||||
|---|---|---|---|---|---|---|
Compound | pKi (± SD) | pIC50 (± SD) | pEC50 (± SD) | Emax (%± SD) | pEC50 | pIC50 |
1 | 4.8 (±0.3) | Inactive | Inactive | ND | Inactive | Inactive |
2 | 5.0 (±0.8) | Inactive | Inactive | ND | Inactive | Inactive |
3 | 5.9 (±0.3) | Inactive | Inactive | ND | Inactive | Inactive |
4 (Isomer 1) | 6.4 (±0.0) | 5.3 (±0.4) | Inactive | ND | Inactive | Inactive |
4 (Isomer 2) | 6.2 (±0.1) | 6.5 (±0.4) | Inactive | ND | Inactive | Inactive |
5 | 5.7 (±0.1) | Inactive | 7.3 (±0.1) | 65 (±6.8) | Inactive | Inactive |
6 | 5.9 (±0.0) | Inactive | Inactive | ND | Inactive | Inactive |
7 | 7.3 (±0.1) | 7.6 (±0.1) | 7.7 (±0.2) | −289 (±17.1) | Inactive | Inactive |
8 | 4.4 (±0.1) | Inactive | 5.9 (±0.2) | −179 (±3.8) | Inactive | Inactive |
9 | 7.5 (±0.1) | 7.7 (±0.1) | 6.5 (±0.1) | −181 (±5.9) | Inactive | Inactive |
