EC Number |
Inhibitors |
Structure |
---|
3.1.4.17 | (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone |
IC50: 0.0001 mM, PDE3A; IC50: 0.00028 mM, PDE3B |
|
3.1.4.17 | (2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol |
IC50: 0.0043 mM, PDE2 |
|
3.1.4.17 | (2S,3R)-3-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)nonan-2-ol |
- |
|
3.1.4.17 | (2Z)-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one |
IC50: 0.000006 mM, PDE3; IC50: 0.0012 mM, PDE2; IC50: 0.015 mM, PDE1 |
|
3.1.4.17 | (6aS,9aR)-3-benzyl-2-(biphenyl-4-ylmethyl)-5-methyl-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[2,1-b]purin-4(3H)-one |
comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context |
|
3.1.4.17 | (Rp)-guanosine-3',5'-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate |
time-dependent and irreversible inactivation of PDE3A |
|
3.1.4.17 | (S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-(trifluoromethyl)-1H-imidazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide |
- |
|
3.1.4.17 | (S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-6-methyl-5-(4-methyl-1H-1,2,3-triazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide |
- |
|
3.1.4.17 | 1-(2-chlorophenyl)-4-methyl-8-[(morpholin-4-yl)methyl][1,2,4]triazolo[4,3-a]quinoxaline |
compound shows good combined potency, acceptable brain uptake and high selectivity for both PDE2 and PDE10 enzymes. In microdosing experiment in rats, the compound shows preferential distribution in brain areas |
|
3.1.4.17 | 1-(2-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione |
- |
|