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Assay Detail

CHEMBL762826

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Phosphodiesterase 5 from human platelets
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
Yu G, Mason H, Wu X, Wang J, Chong S, Beyer B, Henwood A, Pongrac R, Seliger L, He B, Normandin D, Ferrer P, Zhang R, Adam L, Humphrey WG, Krupinski J, Macor JE.
J Med Chem (2003) 46 : 457 -460
PubMed 12570368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 9.37 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410215 1 10.52
CHEMBL344018 1 10.00
CHEMBL139998 1 9.52
CHEMBL266960 1 9.22
CHEMBL140520 1 9.15
CHEMBL1520 VARDENAFIL 4.0 1 9.15
CHEMBL7868 1 9.10
CHEMBL779 TADALAFIL 4.0 1 8.89
CHEMBL192 SILDENAFIL 4.0 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410215 IC50 = 0.03 nM 10.52
CHEMBL344018 IC50 = 0.1 nM 10.00
CHEMBL139998 IC50 = 0.3 nM 9.52
CHEMBL266960 IC50 = 0.6 nM 9.22
CHEMBL140520 IC50 = 0.7 nM 9.15
CHEMBL1520 VARDENAFIL IC50 = 0.7 nM 9.15
CHEMBL7868 IC50 = 0.8 nM 9.10
CHEMBL779 TADALAFIL IC50 = 1.3 nM 8.89
CHEMBL192 SILDENAFIL IC50 = 1.6 nM 8.80