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2',3'-cAMP + H2O
3'-AMP
-
in PdeB the phosphodiesterase activity for 2',3'-cAMP is about 1.7fold higher than that for 3',5'-cAMP
-
-
?
3',5'-cAMP + H2O
adenosine 5'-phosphate
3',5'-cdAMP + H2O
5'-dAMP
-
-
-
-
?
3',5'-cGMP + H2O
guanosine 5'-phosphate
3'-AMP + H2O
?
-
high activity
-
-
?
3'-GMP + H2O
?
-
high activity
-
-
?
5'-dAMP + H2O
?
-
low activity
-
-
?
5'-pApG + H2O
5'-AMP + 5'-GMP
5'-UMP + H2O
?
-
high activity
-
-
?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
bis-(4-nitrophenyl) phosphate + H2O
4-nitrophenyl phosphate + 4-nitrophenol
cAMP + H2O
5'-AMP
-
degradation of extracellular cAMP by isoforms PDE1, PDE7. Degradation of intracellular cAMP by isoform PDE2
-
-
?
cGMP + H2O
5'-GMP
-
degradation of intracellular cGMP by isoform PDE3
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
UDP-D-glucose + H2O
?
-
UDP-D-glucose is hydrolyzed by PdeB, but not by PdeA
-
-
?
additional information
?
-
2',3'-cAMP + H2O

5'-AMP
-
-
-
?
2',3'-cAMP + H2O
5'-AMP
-
-
-
?
2',3'-cAMP + H2O

?
-
-
-
?
2',3'-cAMP + H2O
?
-
-
-
-
?
3',5'-cAMP + H2O

5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
specific for 3',5'-cGMP and 3',5'-cAMP, PDE1
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
specific for 3',5'-cGMP and 3',5'-cAMP, PDE11
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
135219, 135271, 135273, 667684, 668133, 669403, 678221, 679784, 691887, 703570, 750304, 751697 -
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
inhibition of cAMP hydrolysis by cGMP is likely to contribute to cGMP-mediated signaling in myocardium
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE11
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE2
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
activity with 3',5'-cGMP is higher than with 3',5'-cAMP
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
maximal velocity for cAMP is 4fold to 10fold higher than for cGMP, PDE11A4
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
3',5'-cAMP is predominantly hydrolyzed by PDE3A
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
3',5'-cAMP is completely hydrolyzed to adenosine when incubated with PdeA for a prolonged time
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
135233, 135236, 135265, 135273, 135276, 135279, 691887, 692197, 693820, 693825, 694373 -
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
the enzyme is preferentially degrading linear dinucleotides, such as 5'-pApA, 5'-pGpG, and 5'-pApG, compared with cyclic dinucleotide substrates
-
-
?
3',5'-cAMP + H2O
5'-AMP
the enzyme is preferentially degrading linear dinucleotides, such as 5'-pApA, 5'-pGpG, and 5'-pApG, compared with cyclic dinucleotide substrates
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O
5'-AMP
-
-
-
-
?
3',5'-cAMP + H2O

adenosine 5'-phosphate
-
PDE1
-
-
?
3',5'-cAMP + H2O
adenosine 5'-phosphate
-
PDE2
-
-
?
3',5'-cAMP + H2O
adenosine 5'-phosphate
-
PDE3A
-
-
?
3',5'-cAMP + H2O
adenosine 5'-phosphate
-
PDE3B
-
-
?
3',5'-cCMP + H2O

5'-CMP
-
-
-
-
?
3',5'-cCMP + H2O
5'-CMP
-
-
-
-
?
3',5'-cGMP + H2O

5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
specific for 3',5'-cGMP and 3',5'-cAMP, PDE1
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
specific for 3',5'-cGMP and 3',5'-cAMP, PDE11
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE11
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
activity with 3',5'-cGMP and 3',5'-cAMP is nearly identical, PDE2
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
activity with 3',5'-cGMP is higher than with 3',5'-cAMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
maximal velocity for cAMP is 4fold to 10fold higher than for cGMP, PDE11A4
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
highest affinity for 3',5'-cGMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
highest affinity for 3',5'-cGMP
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
PDE1 and PDE2 are the main PDEs that act to degrade cGMP in methacholine-stimulated cells
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
the technique can be used to measure Ca2+/CaM-stimulated PDE activity in cultured cells or tissues
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O
5'-GMP
-
-
-
-
?
3',5'-cGMP + H2O

guanosine 5'-phosphate
-
PDE1
-
-
?
3',5'-cGMP + H2O
guanosine 5'-phosphate
-
PDE3A
-
-
?
3',5'-cGMP + H2O
guanosine 5'-phosphate
-
PDE3B
-
-
?
3',5'-cGMP + H2O
guanosine 5'-phosphate
-
-
-
-
?
5'-pApA + H2O

5'-AMP
-
-
-
?
5'-pApA + H2O
5'-AMP
-
-
-
?
5'-pApG + H2O

5'-AMP + 5'-GMP
-
-
-
?
5'-pApG + H2O
5'-AMP + 5'-GMP
-
-
-
?
5'-pGpG + H2O

5'-GMP
-
-
-
?
5'-pGpG + H2O
5'-GMP
-
-
-
?
adenosine 3',5'-cyclic phosphate + H2O

adenosine 5'-phosphate
-
-
-
-
?
adenosine 3',5'-cyclic phosphate + H2O
adenosine 5'-phosphate
-
-
-
-
?
bis-(4-nitrophenyl) phosphate + H2O

4-nitrophenyl phosphate + 4-nitrophenol
-
-
-
-
?
bis-(4-nitrophenyl) phosphate + H2O
4-nitrophenyl phosphate + 4-nitrophenol
-
-
-
-
?
cAMP + H2O

AMP
-
-
-
?
cGMP + H2O

GMP
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O

guanosine 5'-phosphate
-
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
-
?
guanosine 3',5'-cyclic phosphate + H2O
guanosine 5'-phosphate
-
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O

nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
nucleoside 3',5'-cyclic phosphate + H2O
nucleoside 5'-phosphate
-
-
-
?
additional information

?
-
-
overview on physiological role
-
?
additional information
?
-
-
muscarinic antagonists acting possibly as inverse agonists on M2/M3 muscarinic acetylcholine receptors anchored to sarcolemma membranes can initiate a new signal transducing cascade leading to inhibition of PDEI, which produces a simultaneous rise in both cAMP and cGMP intracellular levels in tracheal smooth muscle
-
-
?
additional information
?
-
-
real-time monitoring of PDE2 activity by a fluorescent cAMP sensor shows that activation of PDE2 results in a rapid decrease of intracellular cAMP from high micromolar to sub-micromolar range within a few seconds. High catalytic activity and fast action in regulating cAMP signaling in a physiological system
-
-
?
additional information
?
-
-
the enzyme is unable to dephosphorylate 5'-AMP
-
-
?
additional information
?
-
-
the enzyme is unable to dephosphorylate 5'-AMP
-
-
?
additional information
?
-
-
isoforms PDE1 and PDE7 are dual-specificity enzymes with negative cooperativity and very different kinetics. Both have 2-3fold lower affinity for cGMP than for cAMP
-
-
?
additional information
?
-
-
h-prune activity is suppressed by dipyridamole and enhanced by the interaction with nm23-H1. Activity is involved in promoting cancer metastasis
-
-
?
additional information
?
-
-
the enzyme might be involved in multiple physiological processes in various organs via its ability to modulate intracellular cAMP and cGMP levels
-
-
?
additional information
?
-
-
isoform PDE1B2 predominantly regulates cGMP and plays a lesser role in cAMP regulation in response to cyclase agonists
-
-
?
additional information
?
-
-
the effect of increasing concentrations of cGMP on endothelial permeability is biphasic, attributable to the relative amounts of enzyme isoforms PDE2A and PDE3A in endothelial cells
-
-
?
additional information
?
-
-
splice variants PDE11A1 and PDE11A2 show higher affinity for cAMP and cGMP than PDE11A4
-
-
?
additional information
?
-
-
NAD+ is not a substrate of PDE3A
-
-
?
additional information
?
-
-
PDE3A physically and functionally interacts with cystic fibrosis transmembrane conductance regulator, CFTR, channel
-
-
?
additional information
?
-
-
structure analysis of phosphodiesterase 10 binding with cAMP and cGMP by hybrid quantum mechanical/molecular mechanical calculations using cyrstal structures of the substrate-bound enzyme, detailed overview
-
-
?
additional information
?
-
-
PDE2 can hydrolyze both cAMP and cGMP with similar maximal rates. PDE1A prefers cGMP, PDE1B cAMP, and PDE1C hydrolyzes both substrates equally. The PDE3 family can hydrolyze both cAMP and cGMP
-
-
?
additional information
?
-
-
overview on physiological role
-
?
additional information
?
-
-
PDE1 in Pukinje neurons may play a role in limiting the cGMP-mediated long-term depression response
-
-
?
additional information
?
-
PDE1A_v7 is the major form of cyclic nucleotide phosphodiesterase 1A expressed in mature sperm and is therefore likely to play an important role in cyclic nucleotide regulation of mature sperm function
-
-
?
additional information
?
-
-
PDE1A_v7 is the major form of cyclic nucleotide phosphodiesterase 1A expressed in mature sperm and is therefore likely to play an important role in cyclic nucleotide regulation of mature sperm function
-
-
?
additional information
?
-
isoform PDE2 regulates the basal cGMP concentration in thalamic neuron
-
-
?
additional information
?
-
-
Rv0805 protein could have an important role to play in regulating cAMP levels in Mycobacterium tuberculosis
-
-
?
additional information
?
-
-
3',5'-cGMP is either not hydrolysed or is cleaved very slowly by PdeA and PdeB, PdeA and PdeB show no activities toward 2'-AMP and 2'-GMP
-
-
?
additional information
?
-
-
PdeA and PdeB hydrolyze 3',5'- and 2',3'-cyclic AMP to adenosine, and also demonstrate phosphatase activity toward nucleoside 5'-tri-, 5'-di-, 5'- and 3'-monophosphates with highest activities for nucleoside 5'-monophosphates
-
-
?
additional information
?
-
-
substrate specificity of PdeE, overview
-
-
?
additional information
?
-
-
not: 2',3'-cAMP
-
-
?
additional information
?
-
-
PDE1A is involved in cGMP breakdown in parotid acinar cells of Oryctolagus cuniculus
-
-
?
additional information
?
-
-
insulin-induced activation of the membrane bound PDE3B is a key step in insulin-mediated inhibition of lipolysis and is also involved in the regulation of insulin-mediated glucose uptake and lipogenesis in adipocytes
-
-
?
additional information
?
-
cGMP levels in the spinal cord are controlled by a number of enzyme isoforms, that can be present in the same cell. Role of NO-cGMP signaling in nociceptive processing
-
-
?
additional information
?
-
-
cytoplasmic isoform PDE1A regulates myosin light chain phosphorylation with little effect on apoptosis, whereas nuclear enzyme isoform PDE1A is important in vascular smoth muscle cell growth and survival
-
-
?
additional information
?
-
-
PDE10A regulates both cAMP and cGMP signaling cascades to impact early signal processing in the corticostriatothalamic circuit
-
-
?
additional information
?
-
enzyxme displays dual specificity for hydrolysis of both cAMP and cGMP
-
-
?
additional information
?
-
-
enzyxme displays dual specificity for hydrolysis of both cAMP and cGMP
-
-
?
additional information
?
-
-
not: 2',3'-cAMP
-
-
?
additional information
?
-
-
PDE3A physically and functionally interacts with cystic fibrosis transmembrane conductance regulator, CFTR, channel
-
-
?
additional information
?
-
the enzyme is preferentially degrading linear dinucleotides, such as 5'-pApA, 5'-pGpG, and 5'-pApG, compared with cyclic dinucleotide substrates
-
-
?
additional information
?
-
-
the enzyme is preferentially degrading linear dinucleotides, such as 5'-pApA, 5'-pGpG, and 5'-pApG, compared with cyclic dinucleotide substrates
-
-
?
additional information
?
-
the enzyme is preferentially degrading linear dinucleotides, such as 5'-pApA, 5'-pGpG, and 5'-pApG, compared with cyclic dinucleotide substrates
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.0001 mM, PDE3A; IC50: 0.00028 mM, PDE3B
(2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol
-
IC50: 0.0043 mM, PDE2
(2S,3R)-3-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)nonan-2-ol
-
-
(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
(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
(Rp)-guanosine-3',5'-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate
-
time-dependent and irreversible inactivation of PDE3A
(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
-
-
(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
-
-
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
1-(2-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(2-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-benzyl-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
-
IC50: 0.00000034 mM, PDE3A, highly selective PDE3 inhibitor; IC50: 0.0000019 mM, PDE3B; IC50: 0.0.0209 mM, PDE2; IC50: 0.1129 mM, PDE1
2-[1-(2,4-dichlorobenzyl)-2-methyl-5-(methylmercapto)-1H-indol-3-yl] ethanaminium chloride
-
IC50: 0.005 mM, PDE1; IC50: 0.037 mM, PDE2
2-[[4-[4-pyridin-4-yl-1-(2,2, 2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline succinic acid
3'-benzyl-2'-(biphenyl-4-ylmethyl)-5'-methyl-3'H-spiro[cyclopentane-1,7'-imidazo[2,1-b]purin]-4'(5'H)-one
-
comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione
3-isobutyl-1-methylxanthine
3-isobutyl-8-(methoxymethyl)-1-methyl-3,9-dihydro-1H-purine-2,6-dione
-
i.e. 8MM-IBMX, comparison of inhibitory effect on several recombinant human PDE isoforms
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
-
Ro20-1724
5-(1-(difluoromethyl)-1H-pyrazol-4-yl)-N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
5-(2-propoxyphenyl)-2,3-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidin-7-one
-
-
5-(3-cyclopentyloxy-4-methoxy-phenyl)-pyrrolidin-2-one
-
50% inhibition at about 0.1 mM
5-methyl-2-[4-(trifluoromethyl)benzyl]-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[2,1-b]purin-4(1H)-one
-
i.e. SCH51866, comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.00000032 mM, PDE3A, highly selective PDE3 inhibitor; IC50: 0.0000015 mM, PDE3B; IC50: 0.0429 mM, PDE1; IC50: 0.0523 mM, PDE2
6-methyl-N-[(1R)-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
8-hydroxyquinoline
2 mM, 28% residual activity
8-methoxymethyl(-3-isobutyl-1-)methylxanthine
8-methoxymethyl-3-isobutyl-1-methylxanthine
8-methoxymethyl-isobutylmethylxanthine
-
inhibits activated PDE1 and PDE2 isoforms as well as PDE4 and PDE5, is 3times more potent in inhibiting PDE5 than PDE1
adenine
-
at 2.5 mM, strong
amantadine
-
brain 60 kDa isozyme
amrinone
-
IC50: 0.0167 mM, PDE3A; IC50: 0.0312 mM, PDE3B
apigenin
-
IC50: 0.0105 mM, PDB3; IC50: 0.0167 mM, PDB2; IC50: 0.0254 mM, PDB1
BAY60-7550
inhibition of isoform PDE2, results in increase in basal cGMP levels after application to thalamic neurons
Biochanin A
-
IC50: 0.0279 mM, PDE2; IC50: 0.0291 mM, PDE1
Calmidazolium
-
soluble but not particulate form
Chloropromazine
-
soluble but not particulate form
daidzein
-
IC50: 0.0286 mM, PDE3
diosmetin
-
IC50: 0.0048 mM, PDB2; IC50: 0.0144 mM, PDB1
E4021
-
50% inhibition at about 0.0005-0.001 mM
EHNA
-
a selective PDE2 inhibitor
eriodictyol
-
IC50: 0.0525 mM, PDB3
erythro-9-(2-hydroxy-3-nonyl)-adenine
-
IC50: 0.0092 mM, PDE2
erythro-9-(2-hydroxy-3-nonyl)adenine
etazolate
-
IC50: 0.0007 mM
ethylene glycol bis(beta-aminoethyl ether)-N,N'-tetraacetic acid
-
soluble but not particulate form
GDP
1 mM, 41% residual activity
genistein
-
IC50: 0.0017 mM, PDB2; IC50: 0.0129 mM, PDB3; IC50: 0.0168 mM, PDB1
GMP
1 mM, 31% residual activity
GTP
1 mM, 44% residual activity
luteolin
-
IC50: 0.0101 mM, PDB3; IC50: 0.0133 mM, PDB2; IC50: 0.0215 mM, PDB1
luteolin-7-glucoside
-
IC50: 0.0351 mM, PDB2
myricetin
-
IC50: 0.0124 mM, PDB3; IC50: 0.0128 mM, PDB2; IC50: 0.0249 mM, PDB1
N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
-
TAK-915
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(1H-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(2-methylpyridin-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-1,2,3-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-imidazol-1-yl)pyrazolo [1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(6-methylpyridin-3-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(tetrahydro-2H-pyran-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-isopropylpyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-6-methyl-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide
-
soluble but not particulate form
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]-6-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-[1-(4-methoxyphenyl)propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-[1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-hydroxy-2-methylpropyl]-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
-
-
N-[1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
NADH
1 mM, 76% residual activity
NADPH
1 mM, 25% residual activity
NaF
1 mM, 79% residual activity
orthovanadate
-
PdeA shows 26% relative activity and PdeB shows 29% relative activity in the hydrolysis of 3',5'-cAMP in the presence of 0.05 mM orthovanadate
phosphate
-
PdeA and PdeB enzyme activities are strongly inhibited by 0.1 M sodium phosphate buffer (pH 6.0 and 7.0), the PdeB activity is more strongly inhibited by 0.1 M phosphate than is PdeA activity
phosphoserine
-
PdeA shows 59% relative activity and PdeB shows 73% relative activity in the hydrolysis of 3',5'-cAMP in the presence of 0.05 mM phosphoserine
phosphotyrosine
-
PdeA shows 44% relative activity and PdeB shows 52% relative activity in the hydrolysis of 3',5'-cAMP in the presence of 0.05 mM phosphotyrosine
quercetin-3,5,7,3',4'-O-pentaacetate
-
-
quercetin-3,5,7,3',4'-O-pentamethylether
-
-
quercetin-3,7,3',4'-O-tetramethylether
-
-
quercetin-3,7,4'-O-trimethylether
-
ayanin
quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate
-
-
quercetin-3-O-methylether
-
-
quinazolinamine
-
IC50: 0.01 mM, PDE3; IC50: 0.23 mM, PDE1; IC50: 0.241 mM, PDE2
RP-73401
-
IC50: 0.05 mM, PDE3; IC50: 0.067 mM, PDE2; IC50: 0.13 mM, PDE1
SKF 94120
-
weak inhibitor
TAK-915
-
i.e. 2 N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
trequinsin
-
IC50: 0.0039 mM
2-[[4-[4-pyridin-4-yl-1-(2,2, 2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline succinic acid

-
potent inhibitor
2-[[4-[4-pyridin-4-yl-1-(2,2, 2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline succinic acid
-
selective PDE10A inhibitor, inhibition of striatal PDE10A activity increases the responsiveness of medium-sized spiny projection neurons to depolarising stimuli
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione

-
IC50: 0.0402 mM
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione
-
IC50: 0.02654 mM, PDE4A4
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione
-
IC50: 0.068 mM
3-isobutyl-1-methylxanthine

-
marked differences in inhibition for isozymes
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
broad-spectrum PDE inhibitor; broad-spectrum PDE inhibitor; broad-spectrum PDE inhibitor
8-methoxymethyl(-3-isobutyl-1-)methylxanthine

-
-
8-methoxymethyl(-3-isobutyl-1-)methylxanthine
-
8-methoxymethyl-3-isobutyl-1-methylxanthine

0.02 mM selectively inhibits PDE1; 0.02 mM selectively inhibits PDE1
8-methoxymethyl-3-isobutyl-1-methylxanthine
-
-
adenosine

-
-
adenosine
-
at 2.5 mM, strong
ADP

1 mM, 56% residual activity
Al3+

-
strongly inhibitory at 2.5 mM
AMP

1 mM, 15% residual activity
ATP

1 mM, 46% residual activity
BAY 60-7550

-
-
BAY 60-7550
-
PDE2 inhibitor
Ca2+

2 mM, 69% residual activity
Ca2+
-
micromolar concentrations
Caffeine

-
-
Caffeine
-
noncompetitive, dog heart
cAMP

-
-
cAMP
-
IC50: 1200 nM, PDE11A4
cAMP
-
particulate enzyme
cGMP

-
IC50: 0.000075 mM, PDE3A; IC50: 0.00032 mM, PDE3B
cGMP
-
IC50: 560 nM, PDE11A4
cGMP
-
competitive inhibitor of PDE3A acting directly at the catalytic site
cGMP
-
the hydrolysis of cGMP by PDE3 inhibits the hydrolysis of cAMP
Cilostamide

-
IC50: 0.000027 mM, PDE3A; IC50: 0.00005 mM, PDE3B; IC50: 0.0125 mM, PDE2
Cilostamide
-
IC50: 0.00013 mM, PDE3; IC50: 0.048 mM, PDE2; IC50: 0.221 mM, PDE1
Cilostamide
-
50 mM, inhibits growth of acinar epithelial cells by 63%
cilostazol

-
IC50: 0.0002 mM, PDE3A; IC50: 0.00038 mM, PDE3B; IC50: 0.0452 mM, PDE2
cilostazol
-
a PDE3 inhibitor
cilostazol
-
a PDE3 inhibitor
Co2+

-
inhibits at concentrations higher than optimal
Co2+
-
inhibits at higher concentrations
Co2+
-
PdeA and PdeB are inhibited (20-30%) at 0.25 mM Co2+
Cu2+

2 mM, 27% residual activity
dibutyryl cyclic AMP

-
-
dibutyryl cyclic AMP
-
94% inhibition at 2.5 mM
dioclein

-
potent selective and calmodulin-independent inhibitor of PDE1, competitive inhibitor for cGMP hydrolysis by PDE1 in basal-activated (1 mM EGTA) and calmodulin-activated (18 nM calmodulin with 0.01 mM CaCl2) states. Dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 11fold more selective for the activated PDE1 isoform compared to basal PDE2 (70fold), activated PDE2 (26fold), PDE3 (19fold), PDE4 (11fold), and PDE5 (16fold)
dioclein
-
dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 11fold more selective for the activated PDE1 isoform compared to basal PDE2 (70fold), activated PDE2 (26fold)
dipyridamole

1 mM, 71% residual activity
dipyridamole
50% inhibition at 0.00082 mM; 50% inhibition at 0.0018 mM
dipyridamole
-
IC50: 0.00078 mM
dipyridamole
-
IC50: 840 nM, PDE11A4
dipyridamole
-
IC50: 0.00034 mM, PDE4A4
dipyridamole
-
inhibits with micromolar potency
dipyridamole
-
50% inhibition at about 0.0002-0.00055 mM
dipyridamole
-
inhibits with micromolar potency
dipyridamole
-
IC50: 0.0069 mM
EDTA

2 mM, 44% residual activity
EDTA
-
complete loss of activity for mutants H23A, H169A, H207A
EDTA
-
PdeA and PdeB show 39% relative activity in the hydrolysis of 3',5'-cAMP in the presence of 0.05 mM EDTA
erythro-9-(2-hydroxy-3-nonyl)adenine

-
IC50: 0.00061 mM for wild-type enzyme
erythro-9-(2-hydroxy-3-nonyl)adenine
inhibition of isoform PDE2, results in increase in basal cGMP levels after application to thalamic neurons
erythro-9-(2-hydroxy-3-nonyl)adenine
-
50% inhibition at about 0.1 mM
Fe2+

-
strong inhibition at 1 mM
Fe2+
-
strongly inhibitory at 2.5 mM
Fe3+

-
strongly inhibitory at 2.5 mM
IBMX

-
-
isobutylmethylxanthine

-
inhibits with micromolar potency
isobutylmethylxanthine
-
50% inhibition at about 0.05 mM
isobutylmethylxanthine
-
inhibits with micromolar potency
Mg2+

-
inhibits at concentrations higher than optimal
Mg2+
-
inhibits at higher amounts
Milrinone

-
0.2627 mM, PDE1; IC50: 0.0001 mM, PDE3B; IC50: 0.00045 mM, PDE3A
Milrinone
-
50% inhibition at about 0.1 mM
Mn2+

-
inhibits at concentrations higher than optimal
Mn2+
-
PdeA and PdeB are inhibited (20-30%) at 0.25 mM Mn2+
nicardipine

-
-
nicardipine
-
weak inhibitor
papaverine

-
-
papaverine
-
competitive inhibitor
papaverine
-
competitive inhibitor
papaverine
-
selective PDE10A inhibitor
papaverine
-
IC50: 0.025 mM
quercetin

-
IC50: 0.0056 mM, PDB3; IC50: 0.0179 mM, PDB2; IC50: 0.0278 mM, PDB1
rolipram

-
-
rolipram
-
IC50: 0.15 mM for wild-type enzyme
rolipram
-
weak inhibitor
sildenafil

-
IC50: IC50: 0.00012 mM, PDE11; IC50: IC50: 0.0013 mM, PDE1
sildenafil
-
IC50: 1725 nM, PDE11; IC50: 350 nM, PDE1
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
sildenafil
-
IC50: 0.00315 mM, PDE4A4
sildenafil
-
viagra, potent selective PDE5 inhibitor
tadalafil

-
IC50: 67 nM, PDE11; IC50: above 10000 nM, PDE1
tadalafil
-
partially inhibits PDE11
tadalafil
-
PDE11 inhibition has impacts on sperm quality. Reasonable caution should by suggested in patients taking the prescribed dosages of tadalafil, a PDE5 inhibitor which could crossreact with human PDE11A splicing variants
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
theophylline

1 mM, 70% residual activity
vardenafil

-
IC50: 121 nM, PDE1; IC50: 308 nM, PDE11
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
vinpocetine

-
IC50: 0.0232 mM, PDE1
vinpocetine
-
inhibitor of activated PDE1
vinpocetine
-
IC50: 0.0223
vinpocetine
-
comparison of inhibitory effect on several recombinant human PDE isoforms
vinpocetine
-
50% inhibition at about 0.06-0.09 mM
zaprinast

-
-
zaprinast
-
IC50: 0.0016 mM, PDE11; IC50: 0.071 mM, PDE1
zaprinast
50% inhibition at 0.005 mM; 50% inhibition at 0.028 mM
zaprinast
-
IC50: 0.00816 mM, PDE4A4
zaprinast
-
weak inhibitor
zaprinast
-
50% inhibition at about 0.016-0.02 mM
Zn2+

-
PdeA and PdeB are potently inhibited in the hydrolysis of 3',5'-cAMP by 0.05 mM Zn2+ with 24% and 28% of remaining activity
Zn2+
-
strong inhibition at 1 mM
Zn2+
-
strongly inhibitory at 2.5 mM
additional information

-
IC50 for vardenafil, sildenafil and tadalafil is above 10000 nM, PDE2
-
additional information
-
treatment with oxidant t-butylhydroperoxide results in release of significant amounts of interleukin-8, which is prevented by inhibition of enzyme isoforms PDE1 and PDE4
-
additional information
-
NAD+ is not an inhibitor of PDE3A
-
additional information
not inhibited by rolipram and sildenafil
-
additional information
-
the oxidant t-butylhydroperoxide signifcantly increases the cytosolic calcium concentration, which is prevented by inhibition of enzyme isoform PDE1. Inhibition of both isoforms PDE1 and PDE4 completely prevent the t-butylhydroperoxide stimulated TNF-alpha release
-
additional information
-
PdeA and PdeB are not stimulated by 3-isobuthyl-1-methylxanthine, theophylline, beta-glycerophosphate, Ca2+, Mg2+, Fe2+, and Fe3+
-
additional information
-
the broad-spectrum phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine, IBMX, has no effect on the activity of PdeE at 1 mM. No inhibition by theophylline at 1 mM, beta-glycerophosphate at 0.1 mM, and by orthovanadate
-
additional information
-
inhibition by monoclonal antibodies
-
additional information
-
-
-
additional information
-
-
-
additional information
-
not inhibitory: EDTA up to 2.5 mM
-
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0.0001 - 0.00028
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.0043
(2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol
Homo sapiens
-
IC50: 0.0043 mM, PDE2
0.0023
(2S,3R)-3-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)nonan-2-ol
Homo sapiens
-
isoform PDE2, pH and temperature not specified in the publication
0.000006 - 0.015
(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
0.0000071
(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
Homo sapiens
-
at pH 7.4 and 25°C
0.00000031
(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
Homo sapiens
-
at pH 7.4 and 25°C
0.0000028
1-(2-chlorophenyl)-4-methyl-8-[(morpholin-4-yl)methyl][1,2,4]triazolo[4,3-a]quinoxaline
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.052
1-(2-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.053
1-(2-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0097
1-(3-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0095
1-(3-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.016
1-(3-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0023
1-(4-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0007
1-(4-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0014
1-(4-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.0015
1-(4-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.028
1-benzyl-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
Cavia porcellus
-
-
0.00000034 - 0.1129
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
0.005 - 0.037
2-[1-(2,4-dichlorobenzyl)-2-methyl-5-(methylmercapto)-1H-indol-3-yl] ethanaminium chloride
0.000001
2-[[4-[4-pyridin-4-yl-1-(2,2, 2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline succinic acid
Rattus norvegicus
-
the IC50 of the compound for inhibition of PDE10A in vitro is less than 1 nM
0.02654 - 0.068
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione
0.0000017
5-(1-(difluoromethyl)-1H-pyrazol-4-yl)-N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00000032 - 0.0523
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.000024
6-methyl-N-[(1R)-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0152
8-methoxymethyl-isobutylmethylxanthine
Bos taurus
-
isoform PDE1 in basal-activated state, pH and temperature not specified in the publication
0.0279 - 0.0291
Biochanin A
0.0012
cAMP
Homo sapiens
-
IC50: 1200 nM, PDE11A4
0.000027 - 0.221
Cilostamide
0.0002 - 0.0452
cilostazol
0.0286
daidzein
Cavia porcellus
-
IC50: 0.0286 mM, PDE3
0.0048 - 0.0144
diosmetin
0.00034 - 0.0069
dipyridamole
0.0525
eriodictyol
Cavia porcellus
-
IC50: 0.0525 mM, PDB3
0.0092
erythro-9-(2-hydroxy-3-nonyl)-adenine
Bos taurus
-
IC50: 0.0092 mM, PDE2
0.00061
erythro-9-(2-hydroxy-3-nonyl)adenine
Homo sapiens
-
IC50: 0.00061 mM for wild-type enzyme
0.0007
etazolate
Trypanosoma cruzi
-
IC50: 0.0007 mM
0.0017 - 0.0168
genistein
0.0351
luteolin-7-glucoside
Cavia porcellus
-
IC50: 0.0351 mM, PDB2
0.0124 - 0.0249
myricetin
0.000061
N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000054
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(1H-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00000077
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(2-methylpyridin-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.000011
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000054
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-1,2,3-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000012
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-imidazol-1-yl)pyrazolo [1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00000098
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(6-methylpyridin-3-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000012
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00001
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(tetrahydro-2H-pyran-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.000034
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-isopropylpyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00000051
N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-6-methyl-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0000051
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]-6-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.000066
N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0038
N-[1-(4-methoxyphenyl)propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.000024
N-[1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-hydroxy-2-methylpropyl]-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.00048
N-[1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
Homo sapiens
-
at pH 7.4 and 25°C
0.0032
nimodipine
Bos taurus
-
isoform PDE1, pH and temperature not specified in the publication
0.000036 - 0.025
papaverine
0.0056 - 0.0278
quercetin
0.002
quercetin-3,5,7,3',4'-O-pentaacetate
Cavia porcellus
-
PDE3
0.0047
quercetin-3,5,7,3',4'-O-pentamethylether
Cavia porcellus
-
PDE3
0.0228
quercetin-3,7,3',4'-O-tetramethylether
Cavia porcellus
-
PDE3
0.0041
quercetin-3,7,4'-O-trimethylether
Cavia porcellus
-
PDE3
0.0008
quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate
Cavia porcellus
-
PDE3
0.0016 - 0.0869
quercetin-3-O-methylether
0.01 - 0.241
quinazolinamine
0.15
rolipram
Homo sapiens
-
IC50: 0.15 mM for wild-type enzyme
0.00012 - 0.0038
sildenafil
0.000015 - 0.01
tadalafil
0.000061
TAK-915
Homo sapiens
-
at pH 7.4 and 25°C
0.0039
trequinsin
Trypanosoma cruzi
-
IC50: 0.0039 mM
0.000121 - 0.00084
vardenafil
0.0223 - 0.185
vinpocetine
0.01
additional information
Homo sapiens
-
IC50 for vardenafil, sildenafil and tadalafil is above 10000 nM, PDE2
-
0.0001
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone

Bos taurus
-
IC50: 0.0001 mM, PDE3A
0.00028
(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.00028 mM, PDE3B
0.000006
(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

Homo sapiens
-
IC50: 0.000006 mM, PDE3
0.0012
(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
Homo sapiens
-
IC50: 0.0012 mM, PDE2
0.015
(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
Homo sapiens
-
IC50: 0.015 mM, PDE1
0.00000034
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide

Bos taurus
-
IC50: 0.00000034 mM, PDE3A, highly selective PDE3 inhibitor
0.0000019
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.0000019 mM, PDE3B
0.0209
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.0.0209 mM, PDE2
0.1129
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
Bos taurus
-
IC50: 0.1129 mM, PDE1
0.005
2-[1-(2,4-dichlorobenzyl)-2-methyl-5-(methylmercapto)-1H-indol-3-yl] ethanaminium chloride

Homo sapiens
-
IC50: 0.005 mM, PDE1
0.037
2-[1-(2,4-dichlorobenzyl)-2-methyl-5-(methylmercapto)-1H-indol-3-yl] ethanaminium chloride
Homo sapiens
-
IC50: 0.037 mM, PDE2
0.02654
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione

Homo sapiens
-
IC50: 0.02654 mM, PDE4A4
0.0402
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione
Homo sapiens
-
IC50: 0.0402 mM
0.068
3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione
Trypanosoma cruzi
-
IC50: 0.068 mM
0.00000032
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone

Bos taurus
-
IC50: 0.00000032 mM, PDE3A, highly selective PDE3 inhibitor
0.0000015
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0000015 mM, PDE3B
0.0429
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0429 mM, PDE1
0.0523
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
Bos taurus
-
IC50: 0.0523 mM, PDE2
0.0167
amrinone

Bos taurus
-
IC50: 0.0167 mM, PDE3A
0.0312
amrinone
Bos taurus
-
IC50: 0.0312 mM, PDE3B
0.0105
apigenin

Cavia porcellus
-
IC50: 0.0105 mM, PDB3
0.0167
apigenin
Cavia porcellus
-
IC50: 0.0167 mM, PDB2
0.0254
apigenin
Cavia porcellus
-
IC50: 0.0254 mM, PDB1
0.0279
Biochanin A

Cavia porcellus
-
IC50: 0.0279 mM, PDE2
0.0291
Biochanin A
Cavia porcellus
-
IC50: 0.0291 mM, PDE1
0.000059
cGMP

Homo sapiens
-
isoform PDE3A
0.000075
cGMP
Bos taurus
-
IC50: 0.000075 mM, PDE3A
0.00032
cGMP
Bos taurus
-
IC50: 0.00032 mM, PDE3B
0.00056
cGMP
Homo sapiens
-
IC50: 560 nM, PDE11A4
0.000027
Cilostamide

Bos taurus
-
IC50: 0.000027 mM, PDE3A
0.00005
Cilostamide
Bos taurus
-
IC50: 0.00005 mM, PDE3B
0.00013
Cilostamide
Homo sapiens
-
IC50: 0.00013 mM, PDE3
0.00037
Cilostamide
Homo sapiens
-
0.0125
Cilostamide
Bos taurus
-
IC50: 0.0125 mM, PDE2
0.048
Cilostamide
Homo sapiens
-
IC50: 0.048 mM, PDE2
0.221
Cilostamide
Homo sapiens
-
IC50: 0.221 mM, PDE1
0.0002
cilostazol

Bos taurus
-
IC50: 0.0002 mM, PDE3A
0.00038
cilostazol
Bos taurus
-
IC50: 0.00038 mM, PDE3B
0.0452
cilostazol
Bos taurus
-
IC50: 0.0452 mM, PDE2
0.00144
dioclein

Bos taurus
-
isoform PDE1 in basal-activated state, pH and temperature not specified in the publication
0.00247
dioclein
Bos taurus
-
isoform PDE1 in calmodulin-activated state, pH and temperature not specified in the publication
0.0382
dioclein
Homo sapiens
-
isoform PDE2 in calmodulin-activated state, pH and temperature not specified in the publication
0.1
dioclein
Homo sapiens
-
isoform PDE2 in basal-activated state, pH and temperature not specified in the publication
0.0048
diosmetin

Cavia porcellus
-
IC50: 0.0048 mM, PDB2