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Assay Detail

CHEMBL902514

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Binding
Inhibition of bovine PDE5 after 24 hrs by HTRF
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL3478)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
Beghyn T, Hounsou C, Deprez BP.
Bioorg Med Chem Lett (2007) 17 : 789 -792
PubMed 17107795 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.24 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL779 TADALAFIL 4.0 1 8.48
CHEMBL247073 1 7.80
CHEMBL248087 1 7.75
CHEMBL397116 1 7.55
CHEMBL397383 1 7.28
CHEMBL247893 1 7.24
CHEMBL398079 1 7.17
CHEMBL245611 1 7.04
CHEMBL394999 1 6.91
CHEMBL429476 1 6.87
CHEMBL394963 1 6.85
CHEMBL397115 1 6.82
CHEMBL396831 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL779 TADALAFIL IC50 = 3.3 nM 8.48
CHEMBL247073 IC50 = 16.0 nM 7.80
CHEMBL248087 IC50 = 18.0 nM 7.75
CHEMBL397116 IC50 = 28.0 nM 7.55
CHEMBL397383 IC50 = 53.0 nM 7.28
CHEMBL247893 IC50 = 57.0 nM 7.24
CHEMBL398079 IC50 = 68.0 nM 7.17
CHEMBL245611 IC50 = 91.0 nM 7.04
CHEMBL394999 IC50 = 122.0 nM 6.91
CHEMBL429476 IC50 = 134.0 nM 6.87
CHEMBL394963 IC50 = 141.0 nM 6.85
CHEMBL397115 IC50 = 152.0 nM 6.82
CHEMBL396831 IC50 = 377.0 nM 6.42