Table 3.
Compound 2 selectivity and human A2a potency
| Compound | A1 human | A2b human | A3 human | Human TNFα PBMC | |||||
|---|---|---|---|---|---|---|---|---|---|
| EC50 (μmol/L) | n | EC50 (μmol/L) | n | EC50 (μmol/L) | n | IC50 (nmol/L) | Intrinsic activity (%) | n | |
| 2 | 2.1 (1.2) | 4 | 3.6 (2.4) | 3 | 6.6 (3.3) | 4 | 0.5 (0.09) | 72.4 (2.5) | 2 |
EC50 values correspond to averages, standard deviations are in brackets. Assay methods for A1, A2b and A3 human in Data S1. PBMC, peripheral blood mononuclear cells; EC50, half maximal effective concentration; IC50, half maximal inhibitory concentration.