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Literature summary for 3.1.4.35 extracted from

  • Bischoff, E.
    Potency, selectivity, and consequences of nonselectivity of PDE inhibition (2004), Int. J. Impot. Res., 16, S11-S14.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
sildenafil IC50: 49 nM, PDE6 Bos taurus
sildenafil IC50: 8.5 nM, PDE5; IC50: above 10000 nM, PDE9 Homo sapiens
tadalafil IC50: 9.4 nM, PDE5; IC50: above 10000 nM, PDE9 Homo sapiens
vardenafil IC50: 11 nM, PDE6 Bos taurus
vardenafil IC50: 0.89 nM, PDE5; IC50: 3370 nM, PDE9 Homo sapiens

Organism

Organism UniProt Comment Textmining
Bos taurus
-
PDE6
-
Bos taurus PDE6
-
PDE6
-
Homo sapiens
-
PDE5
-
Homo sapiens
-
PDE9
-

Source Tissue

Source Tissue Comment Organism Textmining
blood platelet PDE5 Homo sapiens
-
brain PDE5 Homo sapiens
-
corpus cavernosum PDE5 Homo sapiens
-
esophagus PDE5 Homo sapiens
-
lung PDE5 Homo sapiens
-
retina PDE6 Bos taurus
-
vascular smooth muscle PDE5 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 higher than with 3',5'-cGMP, PDE6 Bos taurus 5'-AMP
-
?
3',5'-cAMP + H2O activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6 Bos taurus PDE6 5'-AMP
-
?
3',5'-cGMP + H2O activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6 Bos taurus 5'-GMP
-
?
3',5'-cGMP + H2O selective for 3',5'-cGMP, PDE9 Homo sapiens 5'-GMP
-
?
3',5'-cGMP + H2O specific for 3',5'-cGMP Homo sapiens 5'-GMP
-
?
3',5'-cGMP + H2O activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6 Bos taurus PDE6 5'-GMP
-
?

Synonyms

Synonyms Comment Organism
PDE5
-
Homo sapiens
PDE6
-
Bos taurus
PDE9
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000089
-
IC50: 0.89 nM, PDE5 Homo sapiens vardenafil
0.0000085
-
IC50: 8.5 nM, PDE5 Homo sapiens sildenafil
0.0000094
-
IC50: 9.4 nM, PDE5 Homo sapiens tadalafil
0.000011
-
IC50: 11 nM, PDE6 Bos taurus vardenafil
0.000049
-
IC50: 49 nM, PDE6 Bos taurus sildenafil
0.00337
-
IC50: 3370 nM, PDE9 Homo sapiens vardenafil
0.01
-
IC50: above 10000 nM, PDE9 Homo sapiens sildenafil
0.01
-
IC50: above 10000 nM, PDE9 Homo sapiens tadalafil