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Assay Detail

CHEMBL762828

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

Binding
Inhibition of Phosphodiesterase 5
7
Total Activities
7
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

Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors.
Haning H, Niewöhner U, Schenke T, Es-Sayed M, Schmidt G, Lampe T, Bischoff E.
Bioorg Med Chem Lett (2002) 12 : 865 -868
PubMed 11958981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.32 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL168949 1 9.22
CHEMBL1339 VARDENAFIL HYDROCHLORIDE 4.0 1 9.15
CHEMBL352722 1 8.30
CHEMBL192 SILDENAFIL 4.0 1 8.18
CHEMBL169843 1 8.00
CHEMBL353248 1 8.00
CHEMBL54079 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL168949 IC50 = 0.6 nM 9.22
CHEMBL1339 VARDENAFIL HYDROCHLORIDE IC50 = 0.7 nM 9.15
CHEMBL352722 IC50 = 5.0 nM 8.30
CHEMBL192 SILDENAFIL IC50 = 6.6 nM 8.18
CHEMBL169843 IC50 = 10.0 nM 8.00
CHEMBL353248 IC50 = 10.0 nM 8.00
CHEMBL54079 IC50 = 40.0 nM 7.40