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Literature summary for 3.1.4.17 extracted from
- Potency, selectivity, and consequences of nonselectivity of PDE inhibition (2004), Int. J. Impot. Res., 16, S11-S14.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| additional information | IC50 for vardenafil, sildenafil and tadalafil is above 10000 nM, PDE2 | Homo sapiens | |
| sildenafil | IC50: 1725 nM, PDE11; IC50: 350 nM, PDE1 | Homo sapiens |  |
| tadalafil | IC50: 67 nM, PDE11; IC50: above 10000 nM, PDE1 | Homo sapiens | |
| vardenafil | IC50: 121 nM, PDE1; IC50: 308 nM, PDE11 | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
PDE1 | - |
| Homo sapiens | - |
PDE11 | - |
| Homo sapiens | - |
PDE2 | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| adrenal cortex | PDE2 | Homo sapiens | - |
| brain | PDE1 | Homo sapiens | - |
| brain | PDE2 | Homo sapiens | - |
| corpus cavernosum | PDE2 | Homo sapiens | - |
| heart | PDE1 | Homo sapiens | - |
| heart | PDE2 | Homo sapiens | - |
| kidney | PDE11 | Homo sapiens | - |
| liver | PDE11 | Homo sapiens | - |
| pituitary gland | PDE11 | Homo sapiens | - |
| prostate gland | PDE11 | Homo sapiens | - |
| skeletal muscle | PDE11 | Homo sapiens | - |
| testis | PDE11 | Homo sapiens | - |
| vascular smooth muscle | PDE1 | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 3',5'-cAMP + H2O | activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE11 | Homo sapiens | 5'-AMP | - |
? | |
| 3',5'-cAMP + H2O | activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE2 | Homo sapiens | 5'-AMP | - |
? | |
| 3',5'-cAMP + H2O | activity with 3',5'-cGMP is higher than with 3',5'-cAMP | Homo sapiens | 5'-AMP | - |
? | |
| 3',5'-cGMP + H2O | activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE11 | Homo sapiens | 5'-GMP | - |
? | |
| 3',5'-cGMP + H2O | activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE2 | Homo sapiens | 5'-GMP | - |
? | |
| 3',5'-cGMP + H2O | activity with 3',5'-cGMP is higher than with 3',5'-cAMP | Homo sapiens | 5'-GMP | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PDE1 | - |
Homo sapiens |
| PDE11 | - |
Homo sapiens |
| PDE2 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000067 | - |
IC50: 67 nM, PDE11 | Homo sapiens | tadalafil | |
| 0.000121 | - |
IC50: 121 nM, PDE1 | Homo sapiens | vardenafil | |
| 0.000308 | - |
IC50: 308 nM, PDE11 | Homo sapiens | vardenafil | |
| 0.00035 | - |
IC50: 350 nM, PDE1 | Homo sapiens | sildenafil | |
| 0.001725 | - |
IC50: 1725 nM, PDE11 | Homo sapiens | sildenafil | |
| 0.01 | - |
IC50 for vardenafil, sildenafil and tadalafil is above 10000 nM, PDE2 | Homo sapiens | additional information | |
| 0.01 | - |
IC50: above 10000 nM, PDE1 | Homo sapiens | tadalafil | |
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