Table 1.
Selectivity Data for PDE7i and PDE8i
|
|
|
PDE7i
|
PDE8i
|
|---|---|---|---|
| PDE | Substrate | Ki, nM | Ki, nM |
| PDE1B1 | cAMP | 7200 | >9900 |
| PDE2A1 | cGMP | >9900 | >9900 |
| PDE3A1 | cAMP | >9800 | >9800 |
| PDE4D3 | cAMP | 3800 | 3000 |
| PDE5A1 | cGMP | >9600 | >9600 |
| PDE6 | cGMP | >9900 | >9900 |
| PDE7B | cAMP | 7.8 | 2500 |
| PDE8B | cAMP | >9500 | 0.1 |
| PDE9A1 | cGMP | >9600 | >9600 |
| PDE10A1 | cAMP | >9300 | >9300 |
| PDE11A4 | cGMP | >9200 | >9200 |
Assays were performed using recombinant human PDE proteins, except for PDE6, which was extracted from bovine retina. Mean values for the dissociation constant of the enzyme inhibitor complex (Ki) for PDE7i and for PDE8i, determined for the indicated PDEs and substrates.
Abbreviations: cGMP, cyclic guanosine monophosphate; n, number of assays.