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Literature summary for 3.1.4.17 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
Search for more literature for 3.1.4.17

Cloned(Commentary)

Cloned (Comment) Organism
baculovirus-expressed PDE1 in Sf9 cells Bos taurus
baculovirus-expressed PDE2 in Sf9 cells Bos taurus
baculovirus-expressed PDE3A in Sf9 cells Bos taurus
baculovirus-expressed PDE3B in Sf9 cells Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
(-)-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
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
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
amrinone IC50: 0.0167 mM, PDE3A; IC50: 0.0312 mM, PDE3B Bos taurus
cGMP IC50: 0.000075 mM, PDE3A; IC50: 0.00032 mM, PDE3B Bos taurus
Cilostamide IC50: 0.000027 mM, PDE3A; IC50: 0.00005 mM, PDE3B; IC50: 0.0125 mM, PDE2 Bos taurus
cilostazol IC50: 0.0002 mM, PDE3A; IC50: 0.00038 mM, PDE3B; IC50: 0.0452 mM, PDE2 Bos taurus
erythro-9-(2-hydroxy-3-nonyl)-adenine IC50: 0.0092 mM, PDE2 Bos taurus
Milrinone 0.2627 mM, PDE1; IC50: 0.0001 mM, PDE3B; IC50: 0.00045 mM, PDE3A Bos taurus
vinpocetine IC50: 0.0232 mM, PDE1 Bos taurus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000094
-
 3',5'-cAMP 30°C, pH 8.0, PDE3A Bos taurus
0.00024
-
 3',5'-cAMP 30°C, pH 8.0, PDE3A Bos taurus
0.00029
-
 3',5'-cAMP 30°C, pH 8.0, PDE3B Bos taurus
0.00047
-
 3',5'-cAMP 30°C, pH 8.0, PDE3B Bos taurus
0.0464
-
 3',5'-cGMP 30°C, pH 8.0, PDE1 Bos taurus
0.0464
-
 3',5'-cAMP 30°C, pH 8.0, PDE2 Bos taurus

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3',5'-cAMP + H2O PDE1 Bos taurus adenosine 5'-phosphate
-
 ?
3',5'-cAMP + H2O PDE2 Bos taurus adenosine 5'-phosphate
-
 ?
3',5'-cAMP + H2O PDE3A Bos taurus adenosine 5'-phosphate
-
 ?
3',5'-cAMP + H2O PDE3B Bos taurus adenosine 5'-phosphate
-
 ?
3',5'-cGMP + H2O PDE1 Bos taurus guanosine 5'-phosphate
-
 ?
3',5'-cGMP + H2O PDE3A Bos taurus guanosine 5'-phosphate
-
 ?
3',5'-cGMP + H2O PDE3B Bos taurus guanosine 5'-phosphate
-
 ?

Synonyms

Synonyms Comment Organism
PDE1
-
 Bos taurus
PDE2
-
 Bos taurus
PDE3A
-
 Bos taurus
PDE3B
-
 Bos taurus

Ki Value [mM]

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
0.0000015
-
 IC50: 0.0000015 mM, PDE3B Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
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
0.000027
-
 IC50: 0.000027 mM, PDE3A Bos taurus Cilostamide
0.00005
-
 IC50: 0.00005 mM, PDE3B Bos taurus Cilostamide
0.000075
-
 IC50: 0.000075 mM, PDE3A Bos taurus cGMP
0.0001
-
 IC50: 0.0001 mM, PDE3A Bos taurus (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.0001
-
 IC50: 0.0001 mM, PDE3B Bos taurus Milrinone
0.0002
-
 IC50: 0.0002 mM, PDE3A Bos taurus cilostazol
0.00028
-
 IC50: 0.00028 mM, PDE3B Bos taurus (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.00032
-
 IC50: 0.00032 mM, PDE3B Bos taurus cGMP
0.00038
-
 IC50: 0.00038 mM, PDE3B Bos taurus cilostazol
0.00045
-
 IC50: 0.00045 mM, PDE3A Bos taurus Milrinone
0.0092
-
 IC50: 0.0092 mM, PDE2 Bos taurus erythro-9-(2-hydroxy-3-nonyl)-adenine
0.0125
-
 IC50: 0.0125 mM, PDE2 Bos taurus Cilostamide
0.0167
-
 IC50: 0.0167 mM, PDE3A Bos taurus amrinone
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
0.0232
-
 IC50: 0.0232 mM, PDE1 Bos taurus vinpocetine
0.0312
-
 IC50: 0.0312 mM, PDE3B Bos taurus amrinone
0.0429
-
 IC50: 0.0429 mM, PDE1 Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.0452
-
 IC50: 0.0452 mM, PDE2 Bos taurus cilostazol
0.0523
-
 IC50: 0.0523 mM, PDE2 Bos taurus 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
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