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Literature summary extracted from
- High biochemical selectivity of tadalafil, sildenafil and vardenafil for human phosphodiesterase 5A1 (PDE5) over PDE11A4 suggests the absence of PDE11A4 cross-reaction in patients (2005), Int. J. Impot. Res., 17, 5-9.
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 3.1.4.35 | medicine | use of PDE5 inhibitors in the trteatment of erectile dysfunction and pulmonary hypertension | Homo sapiens |
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 3.1.4.17 | baculovirus expression system, PDE11A4 | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.1.4.17 | cAMP | IC50: 1200 nM, PDE11A4 | Homo sapiens |  |
| 3.1.4.17 | cGMP | IC50: 560 nM, PDE11A4 | Homo sapiens | |
| 3.1.4.17 | dipyridamole | IC50: 840 nM, PDE11A4 | Homo sapiens | |
| 3.1.4.17 | sildenafil | IC50: 3800 nM, 1000fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | |
| 3.1.4.17 | tadalafil | IC50: 73 nM, 40fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | |
| 3.1.4.17 | vardenafil | IC50: 840 nM, 9300fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | |
| 3.1.4.35 | sildenafil | IC50: 3.7 nM, 1000fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | |
| 3.1.4.35 | tadalafil | IC50: 1.8 nM, 40fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | |
| 3.1.4.35 | vardenafil | IC50: 0.091 nM, 9300fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.1.4.17 | 0.00097 | - |
3',5'-cGMP | 30°C, pH 7.5, PDE11A4 | Homo sapiens | |
| 3.1.4.17 | 0.0024 | - |
3',5'-cAMP | 30°C, pH 7.5, PDE11A4 | Homo sapiens | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.1.4.17 | Homo sapiens | - |
- |
- |
| 3.1.4.35 | Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.1.4.17 | 3',5'-cAMP + H2O | maximal velocity for cAMP is 4fold to 10fold higher than for cGMP, PDE11A4 | Homo sapiens | 5'-AMP | - |
? | |
| 3.1.4.17 | 3',5'-cGMP + H2O | maximal velocity for cAMP is 4fold to 10fold higher than for cGMP, PDE11A4 | Homo sapiens | 5'-GMP | - |
? | |
| 3.1.4.35 | 3',5'-cGMP + H2O | PDE5A1 | Homo sapiens | 5'-GMP | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.1.4.17 | PDE11A4 | - |
Homo sapiens |
| 3.1.4.35 | PDE5A1 | - |
Homo sapiens |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 3.1.4.17 | 0.000073 | - |
IC50: 73 nM, 40fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | tadalafil | |
| 3.1.4.17 | 0.00056 | - |
IC50: 560 nM, PDE11A4 | Homo sapiens | cGMP | |
| 3.1.4.17 | 0.00084 | - |
IC50: 840 nM, 9300fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | vardenafil | |
| 3.1.4.17 | 0.00084 | - |
IC50: 840 nM, PDE11A4 | Homo sapiens | dipyridamole | |
| 3.1.4.17 | 0.0012 | - |
IC50: 1200 nM, PDE11A4 | Homo sapiens | cAMP | |
| 3.1.4.17 | 0.0038 | - |
IC50: 3800 nM, 1000fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | sildenafil | |
| 3.1.4.35 | 0.0000018 | - |
IC50: 1.8 nM, 40fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | tadalafil | |
| 3.1.4.35 | 0.0000037 | - |
IC50: 3.7 nM, 1000fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | sildenafil | |
| 3.1.4.35 | 0.000091 | - |
IC50: 0.091 nM, 9300fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication | Homo sapiens | vardenafil | |
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