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Literature summary for 3.1.4.35 extracted from

  • Weeks, J.L.; Zoraghi, R.; Beasley, A.; Sekhar, K.R.; Francis, S.H.; Corbin, J.D.
    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.
    View publication on PubMed
Search for more literature for 3.1.4.35

Application

Application Comment Organism
medicine use of PDE5 inhibitors in the trteatment of erectile dysfunction and pulmonary hypertension Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
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
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
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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3',5'-cGMP + H2O PDE5A1 Homo sapiens 5'-GMP
-
 ?

Synonyms

Synonyms Comment Organism
PDE5A1
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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