BDBM14363 3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0]nona-1,3,6-trien-5-one::5-(2-propoxyphenyl)-2H,3H,7H-[1,2,3]triazolo[4,5-d]pyrimidin-7-one::Tocris-0947::Zaprinast

SMILES CCCOc1ccccc1-c1nc2nn[nH]c2c(=O)[nH]1

InChI Key InChIKey=REZGGXNDEMKIQB-UHFFFAOYSA-N

Data  11 KI  43 IC50  21 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 43 hits for monomerid = 14363   

TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  2.00E+3nMAssay Description:Inhibition of Phosphodiesterase 5 from human corpus cavernosumMore data for this Ligand-Target Pair
In DepthDetails Article
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  300nMAssay Description:In vitro inhibition of phosphodiesterase (PDE V).More data for this Ligand-Target Pair
In DepthDetails Article
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  2.70E+3nMAssay Description:Inhibitory activity against phosphodiesterase 5 from human plateletsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  900nMAssay Description:Concentration required to inhibit 50% activity of phosphodiesterase VA isoenzyme at 100 microM.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  200nMAssay Description:Inhibition of Phosphodiesterase 5 from humanMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphodiesterase(Bos taurus)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.22E+5nMAssay Description:Inhibitory activity against phosphodiesterase 3 (PDE3) purified from bovine heartMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.00E+3nMAssay Description:In vitro inhibition of PDE-V isolated from porcine pulmonary artery.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  3.22E+4nMAssay Description:Inhibition of [Ca(2+)]-calmodulin-dependent cGMP-phosphodiesterase 1 from porcine coronary arteriesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  450nMAssay Description:Inhibitory activity against cyclic GMP-phosphodiesterase (PDE V) isolated from porcine aorta.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C(Homo sapiens (Human))
Smithkline Beecham Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.30E+4nMAssay Description:Inhibition of phosphodiesterase 1C at 100 uMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Bos taurus)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  500nMAssay Description:Evaluated for inhibitory activity against Phosphodiesterase 5 (PDE5) purified from bovine lungMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  6.00E+3nMAssay Description:Inhibition of human phosphodiesterase 1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  2.00E+3nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Homo sapiens (Human))
University Of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.05E+4nMAssay Description:Antagonist activity at GPR35 in human HT-29 cells assessed as inhibition of zaprinast-induced DMR by dynamic mass redistribution assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Homo sapiens (Human))
University Of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.22E+3nMAssay Description:Agonist activity at GPR35 in human HT-29 cells assessed as desensitization of 1 uM zaprinast-induced DMR after 1 hr by dynamic mass redistribution as...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.70E+5nMAssay Description:Inhibition of cyclic GMP sensitive phosphodiesterase PDE 2 of human lungMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphodiesterase(Sus scrofa)
Eisai

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of cGMP-inhibited phosphodiesterase from porcine coronary arteriesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3',5'-cyclic-AMP phosphodiesterase(Sus scrofa)
Eisai

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  7.96E+4nMAssay Description:Inhibition of cAMP specific phosphodiesterase from porcine aortaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  4.68E+4nMAssay Description:Inhibition of cGMP-stimulated phosphodiesterase 2 of porcine coronary arteriesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Rattus norvegicus)
Biofor

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.00E+5nMAssay Description:Inhibition of rat brain Phosphodiesterase 2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphodiesterase(Sus scrofa)
Eisai

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of phosphodiesterase 3 (PDE3) from porcine plateletsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target3',5'-cyclic-AMP phosphodiesterase(Sus scrofa)
Eisai

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of phosphodiesterase 4 (PDE4) from porcine liverMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  9.02E+4nMAssay Description:Inhibition of phosphodiesterase 2 (PDE2) from porcine platelets, range 68.1-119More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.11E+3nMAssay Description:Inhibition of phosphodiesterase 5 (PDE5) from porcine platelets, range 0.733-1.68More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphodiesterase(Bos taurus)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of bovine aorta PDE3 (phosphodiesterase 3)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Bos taurus)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  200nMAssay Description:Inhibitory activity against bovine PDE5 (phosphodiesterase-5).More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human recombinant PDE2 (phosphodiesterase 2)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  2.20E+4nMAssay Description:Inhibitory concentration value against phosphodiesterase 10More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A/3B(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of Phosphodiesterase 3 from rabbit plateletsMore data for this Ligand-Target Pair
In DepthDetails Article
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  9.40E+3nMAssay Description:Inhibition of Phosphodiesterase 1 from rat liverMore data for this Ligand-Target Pair
In DepthDetails Article
TargetcGMP-dependent 3',5'-cyclic phosphodiesterase(Rattus norvegicus)
Biofor

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  6.31E+4nMAssay Description:Inhibition of rat brain particulate cGMP phosphodiesteraseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlkaline phosphatase, germ cell type(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  6.25E+6nMAssay Description:50% inhibition of human placental alkaline phosphatase in the presence of 10 mM p-nitrophenyl phosphate as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAlkaline phosphatase, tissue-nonspecific isozyme(Rattus norvegicus)
TBA

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.75E+6nMAssay Description:Concentration required for 50% inhibition of human leukocyte alkaline phosphatase in the presence of 10 mM p-nitrophenyl phosphate as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.10E+3nMAssay Description:Inhibition of [Ca(2+)]/calmodulin dependent phosphodiesterase PDE 1 of human lungMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Homo sapiens (Human))
University Of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.22E+3nMAssay Description:Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Bos taurus)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  600nMAssay Description:Inhibition of bovine platelet PDE5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  6.00E+3nMAssay Description:In vitro inhibition of phosphodiesterase (PDE I).More data for this Ligand-Target Pair
In DepthDetails Article
TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A/3B(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  1.33E+5nMAssay Description:In vitro inhibition of phosphodiesterase (PDE III).More data for this Ligand-Target Pair
In DepthDetails Article
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  3.16E+3nMAssay Description:Inhibition of PDE5 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  3.16E+3nMAssay Description:Inhibition of PDE5 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Bos taurus)
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  300nMAssay Description:Inhibition of bovine aortic smooth muscle PDE5 using cGMP as substrate incubated for 30 mins in presence of EGTA and [3H]cGMP by liquid scintillation...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Homo sapiens (Human))
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  6.52E+3nMAssay Description:Inhibition of human recombinant PDE5A using cGMP as substrate incubated for 20 mins measured by Kinase Glo reagent based microplate reader assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Homo sapiens (Human))
University Of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataIC50:  48nMAssay Description:Agonist activity at human GPR35 receptor expressed in CHO-K1 cells assessed as desensitization of zaprinast-induced DMR response preincubated for 1 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed