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Literature summary extracted from

  • Sudo, T.; Tachibana, K.; Toga, K.; Tochizawa, S.; Inoue, Y.; Kimura, Y.; Hidaka, H.
    Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity (2000), Biochem. Pharmacol., 59, 347-356.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.4.17 baculovirus-expressed PDE1 in Sf9 cells Bos taurus
3.1.4.17 baculovirus-expressed PDE2 in Sf9 cells Bos taurus
3.1.4.17 baculovirus-expressed PDE3A in Sf9 cells Bos taurus
3.1.4.17 baculovirus-expressed PDE3B in Sf9 cells Bos taurus
3.1.4.35 baculovirus-expressed PDE5 in Sf9 cells Bos taurus
3.1.4.53 baculovirus-expressed PDE4 in Sf9 cells Bos taurus
3.1.4.53 baculovirus-expressed PDE7 in Sf9 cells Bos taurus

Inhibitors

EC Number Inhibitors Comment Organism 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 Bos taurus
3.1.4.17 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 Bos taurus
3.1.4.17 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 Bos taurus
3.1.4.17 amrinone IC50: 0.0167 mM, PDE3A; IC50: 0.0312 mM, PDE3B Bos taurus
3.1.4.17 cGMP IC50: 0.000075 mM, PDE3A; IC50: 0.00032 mM, PDE3B Bos taurus
3.1.4.17 Cilostamide IC50: 0.000027 mM, PDE3A; IC50: 0.00005 mM, PDE3B; IC50: 0.0125 mM, PDE2 Bos taurus
3.1.4.17 cilostazol IC50: 0.0002 mM, PDE3A; IC50: 0.00038 mM, PDE3B; IC50: 0.0452 mM, PDE2 Bos taurus
3.1.4.17 erythro-9-(2-hydroxy-3-nonyl)-adenine IC50: 0.0092 mM, PDE2 Bos taurus
3.1.4.17 Milrinone 0.2627 mM, PDE1; IC50: 0.0001 mM, PDE3B; IC50: 0.00045 mM, PDE3A Bos taurus
3.1.4.17 vinpocetine IC50: 0.0232 mM, PDE1 Bos taurus
3.1.4.35 (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone IC50: 0.0121 mM, PDE5 Bos taurus
3.1.4.35 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide IC50: 0.0027 mM, PDE5 Bos taurus
3.1.4.35 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone IC50: 0.0025 mM, PDE5 Bos taurus
3.1.4.35 amrinone IC50: 0.2296 mM, PDE5 Bos taurus
3.1.4.35 Cilostamide IC50: 0.0152 mM, PDE5 Bos taurus
3.1.4.35 cilostazol IC50: 0.0044 mM, PDE5 Bos taurus
3.1.4.35 dipyridamole IC50: 0.00026 mM, PDE5 Bos taurus
3.1.4.35 Milrinone IC50: 0.0491 mM, PDE5 Bos taurus
3.1.4.53 (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone IC50: 0.1195 mM, PDE7 Bos taurus
3.1.4.53 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide IC50: 0.0203 mM, PDE7; IC50: 0.0453 mM, PDE4 Bos taurus
3.1.4.53 3-isobutyl-1-methylxanthine IC50: 0.007 mM, PDE7 Bos taurus
3.1.4.53 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone IC50: 0.0513 mM, PDE7; IC50: 0.1008 mM, PDE4 Bos taurus
3.1.4.53 Cilostamide IC50: 0.022 mM, PDE7; IC50: 0.0888 mM, PDE4 Bos taurus
3.1.4.53 cilostazol IC50: 0.0214 mM, PDE7; IC50: 0.088 mM, PDE4 Bos taurus
3.1.4.53 Milrinone IC50: 0.0175 mM, PDE4; IC50: 0.0583 mM, PDE7 Bos taurus
3.1.4.53 rolipram IC50: 0.00045 mM, PDE4 Bos taurus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.4.17 0.000094
-
 3',5'-cAMP 30°C, pH 8.0, PDE3A Bos taurus
3.1.4.17 0.00024
-
 3',5'-cAMP 30°C, pH 8.0, PDE3A Bos taurus
3.1.4.17 0.00029
-
 3',5'-cAMP 30°C, pH 8.0, PDE3B Bos taurus
3.1.4.17 0.00047
-
 3',5'-cAMP 30°C, pH 8.0, PDE3B Bos taurus
3.1.4.17 0.0464
-
 3',5'-cGMP 30°C, pH 8.0, PDE1 Bos taurus
3.1.4.17 0.0464
-
 3',5'-cAMP 30°C, pH 8.0, PDE2 Bos taurus
3.1.4.35 0.00098
-
 3',5'-cAMP 30°C, pH 8.0, PDE5 Bos taurus
3.1.4.53 0.00025
-
 3',5'-cAMP 30°C, pH 8.0, PDE7 Bos taurus
3.1.4.53 0.0025
-
 3',5'-cAMP 30°C, pH 8.0, PDE4 Bos taurus

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.17 Bos taurus
-
-
-
3.1.4.35 Bos taurus
-
-
-
3.1.4.53 Bos taurus
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.17 3',5'-cAMP + H2O PDE1 Bos taurus adenosine 5'-phosphate
-
 ?
3.1.4.17 3',5'-cAMP + H2O PDE2 Bos taurus adenosine 5'-phosphate
-
 ?
3.1.4.17 3',5'-cAMP + H2O PDE3A Bos taurus adenosine 5'-phosphate
-
 ?
3.1.4.17 3',5'-cAMP + H2O PDE3B Bos taurus adenosine 5'-phosphate
-
 ?
3.1.4.17 3',5'-cGMP + H2O PDE1 Bos taurus guanosine 5'-phosphate
-
 ?
3.1.4.17 3',5'-cGMP + H2O PDE3A Bos taurus guanosine 5'-phosphate
-
 ?
3.1.4.17 3',5'-cGMP + H2O PDE3B Bos taurus guanosine 5'-phosphate
-
 ?
3.1.4.35 3',5'-cAMP + H2O
-
 Bos taurus 5'-AMP
-
 ?
3.1.4.35 3',5'-cGMP + H2O PDE5 Bos taurus guanosine 5'-phosphate
-
 ?
3.1.4.53 3',5'-cAMP + H2O PDE4 Bos taurus adenosine 5'-phosphate
-
 ?
3.1.4.53 3',5'-cAMP + H2O PDE7 Bos taurus adenosine 5'-phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.4.17 PDE1
-
 Bos taurus
3.1.4.17 PDE2
-
 Bos taurus
3.1.4.17 PDE3A
-
 Bos taurus
3.1.4.17 PDE3B
-
 Bos taurus
3.1.4.35 PDE5
-
 Bos taurus
3.1.4.53 PDE4
-
 Bos taurus
3.1.4.53 PDE7
-
 Bos taurus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.4.17 0.00000022
-
 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
 Bos taurus
3.1.4.17 0.0000003
-
 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
-
 Bos taurus
3.1.4.17 0.000062
-
 (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
 Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.17 0.00000032
-
 IC50: 0.00000032 mM, PDE3A, highly selective PDE3 inhibitor Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.17 0.00000034
-
 IC50: 0.00000034 mM, PDE3A, highly selective PDE3 inhibitor Bos taurus 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
3.1.4.17 0.0000015
-
 IC50: 0.0000015 mM, PDE3B Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.17 0.0000019
-
 IC50: 0.0000019 mM, PDE3B Bos taurus 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
3.1.4.17 0.000027
-
 IC50: 0.000027 mM, PDE3A Bos taurus Cilostamide
3.1.4.17 0.00005
-
 IC50: 0.00005 mM, PDE3B Bos taurus Cilostamide
3.1.4.17 0.000075
-
 IC50: 0.000075 mM, PDE3A Bos taurus cGMP
3.1.4.17 0.0001
-
 IC50: 0.0001 mM, PDE3A Bos taurus (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.17 0.0001
-
 IC50: 0.0001 mM, PDE3B Bos taurus Milrinone
3.1.4.17 0.0002
-
 IC50: 0.0002 mM, PDE3A Bos taurus cilostazol
3.1.4.17 0.00028
-
 IC50: 0.00028 mM, PDE3B Bos taurus (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.17 0.00032
-
 IC50: 0.00032 mM, PDE3B Bos taurus cGMP
3.1.4.17 0.00038
-
 IC50: 0.00038 mM, PDE3B Bos taurus cilostazol
3.1.4.17 0.00045
-
 IC50: 0.00045 mM, PDE3A Bos taurus Milrinone
3.1.4.17 0.0092
-
 IC50: 0.0092 mM, PDE2 Bos taurus erythro-9-(2-hydroxy-3-nonyl)-adenine
3.1.4.17 0.0125
-
 IC50: 0.0125 mM, PDE2 Bos taurus Cilostamide
3.1.4.17 0.0167
-
 IC50: 0.0167 mM, PDE3A Bos taurus amrinone
3.1.4.17 0.0209
-
 IC50: 0.0.0209 mM, PDE2 Bos taurus 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
3.1.4.17 0.0232
-
 IC50: 0.0232 mM, PDE1 Bos taurus vinpocetine
3.1.4.17 0.0312
-
 IC50: 0.0312 mM, PDE3B Bos taurus amrinone
3.1.4.17 0.0429
-
 IC50: 0.0429 mM, PDE1 Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.17 0.0452
-
 IC50: 0.0452 mM, PDE2 Bos taurus cilostazol
3.1.4.17 0.0523
-
 IC50: 0.0523 mM, PDE2 Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.17 0.1129
-
 IC50: 0.1129 mM, PDE1 Bos taurus 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
3.1.4.35 0.00026
-
 IC50: 0.00026 mM, PDE5 Bos taurus dipyridamole
3.1.4.35 0.0025
-
 IC50: 0.0025 mM, PDE5 Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.35 0.0027
-
 IC50: 0.0027 mM, PDE5 Bos taurus 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
3.1.4.35 0.0044
-
 IC50: 0.0044 mM, PDE5 Bos taurus cilostazol
3.1.4.35 0.0121
-
 IC50: 0.0121 mM, PDE5 Bos taurus (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.35 0.0152
-
 IC50: 0.0152 mM, PDE5 Bos taurus Cilostamide
3.1.4.35 0.0491
-
 IC50: 0.0491 mM, PDE5 Bos taurus Milrinone
3.1.4.35 0.2296
-
 IC50: 0.2296 mM, PDE5 Bos taurus amrinone
3.1.4.53 0.00045
-
 IC50: 0.00045 mM, PDE4 Bos taurus rolipram
3.1.4.53 0.007
-
 IC50: 0.007 mM, PDE7 Bos taurus 3-isobutyl-1-methylxanthine
3.1.4.53 0.0175
-
 IC50: 0.0175 mM, PDE4 Bos taurus Milrinone
3.1.4.53 0.0203
-
 IC50: 0.0203 mM, PDE7 Bos taurus 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
3.1.4.53 0.0214
-
 IC50: 0.0214 mM, PDE7 Bos taurus cilostazol
3.1.4.53 0.022
-
 IC50: 0.022 mM, PDE7 Bos taurus Cilostamide
3.1.4.53 0.0453
-
 IC50: 0.0453 mM, PDE4 Bos taurus 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
3.1.4.53 0.0513
-
 IC50: 0.0513 mM, PDE7 Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.53 0.0583
-
 IC50: 0.0583 mM, PDE7 Bos taurus Milrinone
3.1.4.53 0.088
-
 IC50: 0.088 mM, PDE4 Bos taurus cilostazol
3.1.4.53 0.0888
-
 IC50: 0.0888 mM, PDE4 Bos taurus Cilostamide
3.1.4.53 0.1008
-
 IC50: 0.1008 mM, PDE4 Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
3.1.4.53 0.1195
-
 IC50: 0.1195 mM, PDE7 Bos taurus (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone