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
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 75 hits for monomerid = 14363
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
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
Affinity DataEC50: 63nMAssay Description:Agonist activity at human GPR35 receptor expressed in CHO-K1 cells assessed as dynamic mass redistribution response by DMR assayMore data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataKi: 130nMAssay Description:Inhibition of human phosphodiesterase 5More data for this Ligand-Target Pair
Affinity DataEC50: 130nMAssay Description:Agonist activity at human GPR35 by Ca+2 release assayMore data for this Ligand-Target Pair
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
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
Affinity DataEC50: 160nMAssay Description:Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assayMore data for this Ligand-Target Pair
Affinity DataEC50: 160nMAssay Description:Agonist activity at GPR35 in human HT-29 cells by dynamic mass redistribution assayMore data for this Ligand-Target Pair
Affinity DataEC50: 160nMAssay Description:Agonist activity at human GPR35 expressed in CHO-K1 cells by DMR assayMore data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 200nMAssay Description:Inhibition of Phosphodiesterase 5 from humanMore data for this Ligand-Target Pair
Affinity DataIC50: 200nMAssay Description:Inhibitory activity against bovine PDE5 (phosphodiesterase-5).More data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 300nMAssay Description:In vitro inhibition of phosphodiesterase (PDE V).More data for this Ligand-Target Pair
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
Affinity DataEC50: 340nMAssay Description:Agonist activity at GPR35 in human HT-29 cells by DMR assayMore data for this Ligand-Target Pair
Affinity DataEC50: 340nMAssay Description:Agonist activity at human GPR35 receptor expressed in HT-29 cells assessed as dynamic mass redistribution response by DMR assayMore data for this Ligand-Target Pair
TargetO43924/P16499/P18545/P35913/P51160/Q13956(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataKi: 400nMAssay Description:Inhibition of human phosphodiesterase 6More data for this Ligand-Target Pair
Affinity DataKi: 401nMAssay Description:Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysisMore data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 450nMAssay Description:Inhibitory activity against cyclic GMP-phosphodiesterase (PDE V) isolated from porcine aorta.More data for this Ligand-Target Pair
Affinity DataIC50: 500nMAssay Description:Evaluated for inhibitory activity against Phosphodiesterase 5 (PDE5) purified from bovine lungMore data for this Ligand-Target Pair
Affinity DataIC50: 600nMAssay Description:Inhibition of bovine platelet PDE5More data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 900nMAssay Description:Concentration required to inhibit 50% activity of phosphodiesterase VA isoenzyme at 100 uMMore data for this Ligand-Target Pair
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
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4B(Rat)
University of Tennessee
Curated by PDSP Ki Database
University of Tennessee
Curated by PDSP Ki Database
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 1.00E+3nMAssay Description:In vitro inhibition of PDE-V isolated from porcine pulmonary artery.More data for this Ligand-Target Pair
TargetDual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A/1B/1C(Human)
TBA
Curated by ChEMBL
TBA
Curated by ChEMBL
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of [Ca(2+)]/calmodulin dependent phosphodiesterase PDE 1 of human lungMore data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
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
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
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
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
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of PDE5More data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of Phosphodiesterase 5 from human corpus cavernosumMore data for this Ligand-Target Pair
Affinity DataEC50: 2.00E+3nMAssay Description:Agonist activity at human GPR35 assessed as induction of beta-arrestin recruitmentMore data for this Ligand-Target Pair
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
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 2.70E+3nMAssay Description:Inhibitory activity against phosphodiesterase 5 from human plateletsMore data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 3.16E+3nMAssay Description:Inhibition of PDE5 (unknown origin)More data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
Affinity DataIC50: 3.16E+3nMAssay Description:Inhibition of PDE5 (unknown origin)More data for this Ligand-Target Pair
Affinity DataEC50: 3.52E+3nMAssay Description:Agonist activity at TEV protease cleavage site linked GAL4-VP16-fused GPR35 in human Tango GPR35-bla U2OS cells assessed as induction of TEV protease...More data for this Ligand-Target Pair
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
Affinity DataEC50: 4.20E+3nMAssay Description:Agonist activity at human GPR35 expressed in CHO-K1 cells after 90 mins by beta-arrestin 2 recruitment assayMore data for this Ligand-Target Pair
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
TargetDual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A/1B/1C(Human)
TBA
Curated by ChEMBL
TBA
Curated by ChEMBL
Affinity DataIC50: 6.00E+3nMAssay Description:Inhibition of human phosphodiesterase 1More data for this Ligand-Target Pair
TargetDual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A/1B/1C(Human)
TBA
Curated by ChEMBL
TBA
Curated by ChEMBL
Affinity DataIC50: 6.00E+3nMAssay Description:In vitro inhibition of phosphodiesterase (PDE I).More data for this Ligand-Target Pair
Affinity DataEC50: 6.10E+3nMAssay Description:Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactama...More data for this Ligand-Target Pair
Affinity DataEC50: 6.20E+3nMAssay Description:Agonist activity at GPR35 in human U20S cells expressing beta-lactamase and Gal4-VP16 transcription factor assessed as beta arrestin translocation af...More data for this Ligand-Target Pair
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Human)
Monash University (Parkville Campus)
Curated by ChEMBL
Monash University (Parkville Campus)
Curated by ChEMBL
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
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
TargetcGMP-specific 3',5'-cyclic phosphodiesterase(Rat)
Laboratories Glaxo Wellcome Centre De Recherches
Curated by ChEMBL
Laboratories Glaxo Wellcome Centre De Recherches
Curated by ChEMBL
Affinity DataEC50: 9.00E+3nMAssay Description:Compound was tested for inhibition of stimulation of rat aortic smooth muscle cells (RSMC)More data for this Ligand-Target Pair
TargetDual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B/Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C/Phosphodiesterase(Rat)
TBA
Curated by ChEMBL
TBA
Curated by ChEMBL
Affinity DataIC50: 9.40E+3nMAssay Description:Inhibition of Phosphodiesterase 1 from rat liverMore data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of bovine aorta PDE3 (phosphodiesterase 3)More data for this Ligand-Target Pair
