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Assay Detail

CHEMBL762831

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

Binding
Inhibition of phosphodiesterase type 5 (PDE5) of human platelets
5
Total Activities
5
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

N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Rotella DP, Sun Z, Zhu Y, Krupinski J, Pongrac R, Seliger L, Normandin D, Macor JE.
J Med Chem (2000) 43 : 1257 -1263
PubMed 10753463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.41 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278354 1 9.32
CHEMBL192 SILDENAFIL 4.0 1 8.80
CHEMBL22906 1 8.28
CHEMBL283122 1 8.28
CHEMBL25391 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278354 IC50 = 0.48 nM 9.32
CHEMBL192 SILDENAFIL IC50 = 1.6 nM 8.80
CHEMBL22906 IC50 = 5.3 nM 8.28
CHEMBL283122 IC50 = 5.3 nM 8.28
CHEMBL25391 IC50 = 44.0 nM 7.36