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Literature summary 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

EC Number Inhibitors Comment Organism Structure
3.1.4.17 additional information IC50 for vardenafil, sildenafil and tadalafil is above 10000 nM, PDE2 Homo sapiens
3.1.4.17 sildenafil IC50: 1725 nM, PDE11; IC50: 350 nM, PDE1 Homo sapiens
3.1.4.17 tadalafil IC50: 67 nM, PDE11; IC50: above 10000 nM, PDE1 Homo sapiens
3.1.4.17 vardenafil IC50: 121 nM, PDE1; IC50: 308 nM, PDE11 Homo sapiens
3.1.4.35 sildenafil IC50: 49 nM, PDE6 Bos taurus
3.1.4.35 sildenafil IC50: 8.5 nM, PDE5; IC50: above 10000 nM, PDE9 Homo sapiens
3.1.4.35 tadalafil IC50: 9.4 nM, PDE5; IC50: above 10000 nM, PDE9 Homo sapiens
3.1.4.35 vardenafil IC50: 11 nM, PDE6 Bos taurus
3.1.4.35 vardenafil IC50: 0.89 nM, PDE5; IC50: 3370 nM, PDE9 Homo sapiens
3.1.4.53 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
3.1.4.53 sildenafil IC50: 3190 nM, PDE4 Homo sapiens
3.1.4.53 tadalafil IC50: above 10000 nM, PDE4 Homo sapiens
3.1.4.53 vardenafil IC50: 2055 nM, PDE4; IC50: 4600 nM, PDE4 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.17 Homo sapiens
-
 PDE1
-
3.1.4.17 Homo sapiens
-
 PDE11
-
3.1.4.17 Homo sapiens
-
 PDE2
-
3.1.4.35 Bos taurus
-
 PDE6
-
3.1.4.35 Bos taurus PDE6
-
 PDE6
-
3.1.4.35 Homo sapiens
-
 PDE5
-
3.1.4.35 Homo sapiens
-
 PDE9
-
3.1.4.53 Homo sapiens
-
 PDE4
-
3.1.4.53 Homo sapiens
-
 PDE7
-
3.1.4.53 Homo sapiens
-
 PDE8
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.4.17 adrenal cortex PDE2 Homo sapiens
-
3.1.4.17 brain PDE1 Homo sapiens
-
3.1.4.17 brain PDE2 Homo sapiens
-
3.1.4.17 corpus cavernosum PDE2 Homo sapiens
-
3.1.4.17 heart PDE1 Homo sapiens
-
3.1.4.17 heart PDE2 Homo sapiens
-
3.1.4.17 kidney PDE11 Homo sapiens
-
3.1.4.17 liver PDE11 Homo sapiens
-
3.1.4.17 pituitary gland PDE11 Homo sapiens
-
3.1.4.17 prostate gland PDE11 Homo sapiens
-
3.1.4.17 skeletal muscle PDE11 Homo sapiens
-
3.1.4.17 testis PDE11 Homo sapiens
-
3.1.4.17 vascular smooth muscle PDE1 Homo sapiens
-
3.1.4.35 blood platelet PDE5 Homo sapiens
-
3.1.4.35 brain PDE5 Homo sapiens
-
3.1.4.35 corpus cavernosum PDE5 Homo sapiens
-
3.1.4.35 esophagus PDE5 Homo sapiens
-
3.1.4.35 lung PDE5 Homo sapiens
-
3.1.4.35 retina PDE6 Bos taurus
-
3.1.4.35 vascular smooth muscle PDE5 Homo sapiens
-
3.1.4.53 lung PDE4 Homo sapiens
-
3.1.4.53 mast cell PDE4 Homo sapiens
-
3.1.4.53 skeletal muscle PDE7 Homo sapiens
-
3.1.4.53 T-cell PDE7 Homo sapiens
-
3.1.4.53 testis PDE8 Homo sapiens
-
3.1.4.53 thyroid gland PDE8 Homo sapiens
-
3.1.4.53 vascular smooth muscle PDE4 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 activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE11 Homo sapiens 5'-AMP
-
 ?
3.1.4.17 3',5'-cAMP + H2O activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE2 Homo sapiens 5'-AMP
-
 ?
3.1.4.17 3',5'-cAMP + H2O activity with 3',5'-cGMP is higher than with 3',5'-cAMP Homo sapiens 5'-AMP
-
 ?
3.1.4.17 3',5'-cGMP + H2O activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE11 Homo sapiens 5'-GMP
-
 ?
3.1.4.17 3',5'-cGMP + H2O activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE2 Homo sapiens 5'-GMP
-
 ?
3.1.4.17 3',5'-cGMP + H2O activity with 3',5'-cGMP is higher than with 3',5'-cAMP Homo sapiens 5'-GMP
-
 ?
3.1.4.35 3',5'-cAMP + H2O activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6 Bos taurus 5'-AMP
-
 ?
3.1.4.35 3',5'-cAMP + H2O activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6 Bos taurus PDE6 5'-AMP
-
 ?
3.1.4.35 3',5'-cGMP + H2O activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6 Bos taurus 5'-GMP
-
 ?
3.1.4.35 3',5'-cGMP + H2O selective for 3',5'-cGMP, PDE9 Homo sapiens 5'-GMP
-
 ?
3.1.4.35 3',5'-cGMP + H2O specific for 3',5'-cGMP Homo sapiens 5'-GMP
-
 ?
3.1.4.35 3',5'-cGMP + H2O activity with 3',5'-cAMP is higher than with 3',5'-cGMP, PDE6 Bos taurus PDE6 5'-GMP
-
 ?
3.1.4.53 3',5'-cAMP + H2O activity with 3',5'-cAMP is much higher than activity with 3',5'-cGMP, PDE7 Homo sapiens 5'-AMP
-
 ?
3.1.4.53 3',5'-cAMP + H2O specific for 3',5'-cAMP, PDE4 Homo sapiens 5'-AMP
-
 ?
3.1.4.53 3',5'-cAMP + H2O specific for 3',5'-cAMP, PDE8 Homo sapiens 5'-AMP
-
 ?
3.1.4.53 3',5'-cGMP + H2O activity with 3',5'-cAMP is much higher than activity with 3',5'-cGMP, PDE7 Homo sapiens 5'-GMP
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.4.17 PDE1
-
 Homo sapiens
3.1.4.17 PDE11
-
 Homo sapiens
3.1.4.17 PDE2
-
 Homo sapiens
3.1.4.35 PDE5
-
 Homo sapiens
3.1.4.35 PDE6
-
 Bos taurus
3.1.4.35 PDE9
-
 Homo sapiens
3.1.4.53 PDE4
-
 Homo sapiens
3.1.4.53 PDE7
-
 Homo sapiens
3.1.4.53 PDE8
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.17 0.000067
-
 IC50: 67 nM, PDE11 Homo sapiens tadalafil
3.1.4.17 0.000121
-
 IC50: 121 nM, PDE1 Homo sapiens vardenafil
3.1.4.17 0.000308
-
 IC50: 308 nM, PDE11 Homo sapiens vardenafil
3.1.4.17 0.00035
-
 IC50: 350 nM, PDE1 Homo sapiens sildenafil
3.1.4.17 0.001725
-
 IC50: 1725 nM, PDE11 Homo sapiens sildenafil
3.1.4.17 0.01
-
 IC50 for vardenafil, sildenafil and tadalafil is above 10000 nM, PDE2 Homo sapiens additional information
3.1.4.17 0.01
-
 IC50: above 10000 nM, PDE1 Homo sapiens tadalafil
3.1.4.35 0.00000089
-
 IC50: 0.89 nM, PDE5 Homo sapiens vardenafil
3.1.4.35 0.0000085
-
 IC50: 8.5 nM, PDE5 Homo sapiens sildenafil
3.1.4.35 0.0000094
-
 IC50: 9.4 nM, PDE5 Homo sapiens tadalafil
3.1.4.35 0.000011
-
 IC50: 11 nM, PDE6 Bos taurus vardenafil
3.1.4.35 0.000049
-
 IC50: 49 nM, PDE6 Bos taurus sildenafil
3.1.4.35 0.00337
-
 IC50: 3370 nM, PDE9 Homo sapiens vardenafil
3.1.4.35 0.01
-
 IC50: above 10000 nM, PDE9 Homo sapiens sildenafil
3.1.4.35 0.01
-
 IC50: above 10000 nM, PDE9 Homo sapiens tadalafil
3.1.4.53 0.002055
-
 IC50: 2055 nM, PDE4 Homo sapiens vardenafil
3.1.4.53 0.00319
-
 IC50: 3190 nM, PDE4 Homo sapiens sildenafil
3.1.4.53 0.0046
-
 IC50: 4600 nM, PDE4 Homo sapiens vardenafil
3.1.4.53 0.01
-
 IC 50 for sildenafil and tadalafil is above 10000 nM, PDE7 Homo sapiens additional information
3.1.4.53 0.01
-
 IC50: above 10000 nM, PDE4 Homo sapiens tadalafil