Relative β adrenoceptor and PDE4 enzyme inhibitor potency for GS-5759 and comparator compounds
Data are mean nanomolar values from n = 1–3 separate experiments performed in triplicate.
| Compound | Inhibition: IC50 | Binding: IC50 | Cell cAMP: EC50 | β1 vs. β Fold Ratio | ||||
|---|---|---|---|---|---|---|---|---|
| PDE4A1A Enzyme | PDE4B1 Enzyme | PDE4B2 Enzyme | PDE4D2 Enzyme | β2 Receptor | β2 Receptor | β1 Receptor | ||
| Roflumilast | 3 ± 1 | NA | NA | NA | NA | |||
| GSK256066 | 0.06 ± 0.002 | 0.1 | <0.1 | 0.04 ± 0.007 | >300 | >300 | NA | NA |
| Indacaterol | NA | 6 ± 10 | 1 ± 0.2 | 26 ± 12 | 26 | |||
| GS-5759 | 67 ± 19 | 40 ± 6 | 5 ± 3 | 56 ± 9 | 11 ± 2 | 8 ± 4 | 33 ± 20 | 4 |