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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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 75 hits for monomerid = 14363   

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

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi:  130nMAssay Description:Inhibition of human phosphodiesterase 5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetO43924/P16499/P18545/P35913/P51160/Q13956(Human)
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi:  400nMAssay Description:Inhibition of human phosphodiesterase 6More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Human)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi:  401nMAssay Description:Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysisChecked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Rat)
University of Tennessee

Curated by PDSP Ki Database
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi:  1.00E+3nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi:  8.76E+3nMAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A(Human)
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi:  1.20E+4nMAssay Description:Inhibition of human phosphodiesterase 11More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A(Human)
Monash University (Parkville Campus)

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi:  3.50E+4nMAssay Description:Inhibition of human phosphodiesterase 9More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi: >5.00E+4nMAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi: >5.00E+4nMAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi: >5.00E+4nM ΔG°: >-5.80kcal/molepH: 8.0 T: 22°CAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataKi: >5.00E+4nMAssay Description:PDE4 enzyme activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using SPA kit. [3H]-AMP was captured by the SPA beads, and qu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(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(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(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(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(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(Bovine)
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(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(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
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
TargetG-protein coupled receptor 35(Human)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataEC50:  140nMAssay Description:Agonist activity at GPR35 in human HT-29 cells measured after 10 mins by dynamic mass redistribution assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Bovine)
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(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(Human)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataEC50:  4.20E+3nMAssay Description:Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and GPR35-GA14-VP16 transcription factor fusion protein assessed as transcrip...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Human)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataEC50:  160nMAssay Description:Agonist activity at GPR35 in human HT-29 cells after 1 hr by dynamic mass redistribution assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(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(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
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(Pig)
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(Pig)
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
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
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(Pig)
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(Pig)
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
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(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(Bovine)
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(Bovine)
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
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(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
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
TargetG-protein coupled receptor 35(Human)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataEC50:  130nMAssay Description:Agonist activity at human GPR35 by Ca+2 release assayChecked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Human)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataEC50:  2.24E+3nMAssay Description:Agonist activity at human GPR35b expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase report...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG protein-coupled receptor GPR35(Rat)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataEC50:  61nMAssay Description:Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Mouse)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataEC50:  980nMAssay Description:Agonist activity at mouse GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporte...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Human)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataEC50:  1.96E+3nMAssay Description:Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporte...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetG-protein coupled receptor 35(Human)
University of Bonn

Curated by ChEMBL
LigandPNGBDBM14363(3-(2-propoxyphenyl)-2,4,7,8,9-pentazabicyclo[4.3.0...)
Affinity DataEC50:  5.30E+3nMAssay Description:Agonist activity at human GPR35 expressed in U2OS cells coexpressing Gal4-VP16/beta-arrestin fusion protein after 5 hrs by tango beta-arrestin transl...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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