Literature summary for 3.1.4.53 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.

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Cloned(Commentary)

Cloned (Comment)	Organism
baculovirus-expressed PDE4 in Sf9 cells	Bos taurus
baculovirus-expressed PDE7 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: 0.1195 mM, PDE7	Bos taurus
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-isobutyl-1-methylxanthine	IC50: 0.007 mM, PDE7	Bos taurus
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
Cilostamide	IC50: 0.022 mM, PDE7; IC50: 0.0888 mM, PDE4	Bos taurus
cilostazol	IC50: 0.0214 mM, PDE7; IC50: 0.088 mM, PDE4	Bos taurus
Milrinone	IC50: 0.0175 mM, PDE4; IC50: 0.0583 mM, PDE7	Bos taurus
rolipram	IC50: 0.00045 mM, PDE4	Bos taurus

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.00025	-	3',5'-cAMP	30°C, pH 8.0, PDE7	Bos taurus
0.0025	-	3',5'-cAMP	30°C, pH 8.0, PDE4	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	PDE4	Bos taurus	adenosine 5'-phosphate	-	?
3',5'-cAMP + H2O	PDE7	Bos taurus	adenosine 5'-phosphate	-	?

Synonyms

Synonyms	Comment	Organism
PDE4	-	Bos taurus
PDE7	-	Bos taurus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00045	-	IC50: 0.00045 mM, PDE4	Bos taurus	rolipram
0.007	-	IC50: 0.007 mM, PDE7	Bos taurus	3-isobutyl-1-methylxanthine
0.0175	-	IC50: 0.0175 mM, PDE4	Bos taurus	Milrinone
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
0.0214	-	IC50: 0.0214 mM, PDE7	Bos taurus	cilostazol
0.022	-	IC50: 0.022 mM, PDE7	Bos taurus	Cilostamide
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
0.0513	-	IC50: 0.0513 mM, PDE7	Bos taurus	6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.0583	-	IC50: 0.0583 mM, PDE7	Bos taurus	Milrinone
0.088	-	IC50: 0.088 mM, PDE4	Bos taurus	cilostazol
0.0888	-	IC50: 0.0888 mM, PDE4	Bos taurus	Cilostamide
0.1008	-	IC50: 0.1008 mM, PDE4	Bos taurus	6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
0.1195	-	IC50: 0.1195 mM, PDE7	Bos taurus	(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone

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Release 2023.1 (January 2023)