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Assay Detail

CHEMBL757897

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

Binding
Inhibition of PDE5 of human platelets
6
Total Activities
6
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 pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
Yu G, Mason HJ, Wu X, Wang J, Chong S, Dorough G, Henwood A, Pongrac R, Seliger L, He B, Normandin D, Adam L, Krupinski J, Macor JE.
J Med Chem (2001) 44 : 1025 -1027
PubMed 11297448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.90 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266960 1 9.22
CHEMBL8132 1 9.00
CHEMBL269079 1 8.85
CHEMBL8198 1 8.80
CHEMBL192 SILDENAFIL 4.0 1 8.80
CHEMBL8410 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266960 IC50 = 0.6 nM 9.22
CHEMBL8132 IC50 = 1.0 nM 9.00
CHEMBL269079 IC50 = 1.4 nM 8.85
CHEMBL8198 IC50 = 1.6 nM 8.80
CHEMBL192 SILDENAFIL IC50 = 1.6 nM 8.80
CHEMBL8410 IC50 = 1.8 nM 8.74