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Assay Detail

CHEMBL762827

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Binding
Inhibitory concentration against phosphodiesterase 5 (PDE5) from human platelet
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
Pitts WJ, Vaccaro W, Huynh T, Leftheris K, Roberge JY, Barbosa J, Guo J, Brown B, Watson A, Donaldson K, Starling GC, Kiener PA, Poss MA, Dodd JH, Barrish JC.
Bioorg Med Chem Lett (2004) 14 : 2955 -2958
PubMed 15125967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.30 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192 SILDENAFIL 4.0 1 7.96
CHEMBL100779 1 6.57
CHEMBL516604 1 5.52
CHEMBL34431 CILOSTAMIDE 2.0 1 5.15
CHEMBL63 ROLIPRAM 2.0 1 -
CHEMBL313842 ZARDAVERINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192 SILDENAFIL IC50 = 11.0 nM 7.96
CHEMBL100779 IC50 = 270.0 nM 6.57
CHEMBL516604 IC50 = 3020.0 nM 5.52
CHEMBL34431 CILOSTAMIDE IC50 = 7150.0 nM 5.15
CHEMBL63 ROLIPRAM IC50 > 10000.0 nM -
CHEMBL313842 ZARDAVERINE IC50 > 10000.0 nM -