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Assay Detail

CHEMBL870381

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Binding
Inhibition of PDE6
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 6 (CHEMBL2097163)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Novel pyrazolopyrimidopyridazinones with potent and selective phosphodiesterase 5 (PDE5) inhibitory activity as potential agents for treatment of erectile dysfunction.
Giovannoni MP, Vergelli C, Biancalani C, Cesari N, Graziano A, Biagini P, Gracia J, Gavaldà A, Dal Piaz V.
J Med Chem (2006) 49 : 5363 -5371
PubMed 16913726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.27 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192 SILDENAFIL 4.0 1 7.40
CHEMBL213060 1 7.21
CHEMBL212397 1 6.55
CHEMBL377563 1 6.48
CHEMBL378255 1 6.48
CHEMBL213219 1 6.26
CHEMBL438451 1 6.21
CHEMBL213425 1 6.07
CHEMBL377144 1 6.00
CHEMBL213113 1 5.66
CHEMBL213265 1 5.58
CHEMBL213094 1 5.33
CHEMBL215503 1 -
CHEMBL215268 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192 SILDENAFIL IC50 = 40.0 nM 7.40
CHEMBL213060 IC50 = 62.0 nM 7.21
CHEMBL212397 IC50 = 280.0 nM 6.55
CHEMBL377563 IC50 = 330.0 nM 6.48
CHEMBL378255 IC50 = 330.0 nM 6.48
CHEMBL213219 IC50 = 550.0 nM 6.26
CHEMBL438451 IC50 = 610.0 nM 6.21
CHEMBL213425 IC50 = 860.0 nM 6.07
CHEMBL377144 IC50 = 1000.0 nM 6.00
CHEMBL213113 IC50 = 2200.0 nM 5.66
CHEMBL213265 IC50 = 2600.0 nM 5.58
CHEMBL213094 IC50 = 4700.0 nM 5.33
CHEMBL215503 IC50 - -
CHEMBL215268 IC50 - -