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Literature summary for 3.1.4.53 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 | IC 50 for sildenafil and tadalafil is above 10000 nM, PDE7; IC50 for sildenafil is above 100000 nM and IC50 for tadalafil and vardenafil is above 10000 nM, PDE8 | Homo sapiens | |
| sildenafil | IC50: 3190 nM, PDE4 | Homo sapiens |  |
| tadalafil | IC50: above 10000 nM, PDE4 | Homo sapiens | |
| vardenafil | IC50: 2055 nM, PDE4; IC50: 4600 nM, PDE4 | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
PDE4 | - |
| Homo sapiens | - |
PDE7 | - |
| Homo sapiens | - |
PDE8 | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| lung | PDE4 | Homo sapiens | - |
| mast cell | PDE4 | Homo sapiens | - |
| skeletal muscle | PDE7 | Homo sapiens | - |
| T-cell | PDE7 | Homo sapiens | - |
| testis | PDE8 | Homo sapiens | - |
| thyroid gland | PDE8 | Homo sapiens | - |
| vascular smooth muscle | PDE4 | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 3',5'-cAMP + H2O | activity with 3',5'-cAMP is much higher than activity with 3',5'-cGMP, PDE7 | Homo sapiens | 5'-AMP | - |
? | |
| 3',5'-cAMP + H2O | specific for 3',5'-cAMP, PDE4 | Homo sapiens | 5'-AMP | - |
? | |
| 3',5'-cAMP + H2O | specific for 3',5'-cAMP, PDE8 | Homo sapiens | 5'-AMP | - |
? | |
| 3',5'-cGMP + H2O | activity with 3',5'-cAMP is much higher than activity with 3',5'-cGMP, PDE7 | Homo sapiens | 5'-GMP | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PDE4 | - |
Homo sapiens |
| PDE7 | - |
Homo sapiens |
| PDE8 | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.002055 | - |
IC50: 2055 nM, PDE4 | Homo sapiens | vardenafil | |
| 0.00319 | - |
IC50: 3190 nM, PDE4 | Homo sapiens | sildenafil | |
| 0.0046 | - |
IC50: 4600 nM, PDE4 | Homo sapiens | vardenafil | |
| 0.01 | - |
IC 50 for sildenafil and tadalafil is above 10000 nM, PDE7 | Homo sapiens | additional information | |
| 0.01 | - |
IC50: above 10000 nM, PDE4 | Homo sapiens | tadalafil | |
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