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Assay Detail

CHEMBL762822

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

Binding
Inhibition of phosphodiesterase 5 from human platelets
11
Total Activities
11
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

Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Bi Y, Stoy P, Adam L, He B, Krupinski J, Normandin D, Pongrac R, Seliger L, Watson A, Macor JE.
Bioorg Med Chem Lett (2004) 14 : 1577 -1580
PubMed 15006407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.76 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38735 1 10.30
CHEMBL291127 1 9.40
CHEMBL289047 1 9.32
CHEMBL39065 1 9.26
CHEMBL41083 1 9.22
CHEMBL442348 1 8.89
CHEMBL41236 1 8.85
CHEMBL192 SILDENAFIL 4.0 1 8.80
CHEMBL40371 1 8.40
CHEMBL42869 1 7.14
CHEMBL41950 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38735 IC50 = 0.05 nM 10.30
CHEMBL291127 IC50 = 0.4 nM 9.40
CHEMBL289047 IC50 = 0.48 nM 9.32
CHEMBL39065 IC50 = 0.55 nM 9.26
CHEMBL41083 IC50 = 0.6 nM 9.22
CHEMBL442348 IC50 = 1.3 nM 8.89
CHEMBL41236 IC50 = 1.4 nM 8.85
CHEMBL192 SILDENAFIL IC50 = 1.6 nM 8.80
CHEMBL40371 IC50 = 4.0 nM 8.40
CHEMBL42869 IC50 = 73.0 nM 7.14
CHEMBL41950 IC50 = 160.0 nM 6.80