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Assay Detail

CHEMBL762508

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Binding
Inhibition of phosphodiesterase 5 of rabbit platelets
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5(')-sulfonamide moiety of phenyl ring.
Kim DK, Young Lee J, Park HJ, Minh Thai K.
Bioorg Med Chem Lett (2004) 14 : 2099 -2103
PubMed 15080987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 9.37 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL245317 1 9.77
CHEMBL245517 1 9.74
CHEMBL63548 1 9.55
CHEMBL541468 1 9.55
CHEMBL67064 1 9.54
CHEMBL245315 1 9.52
CHEMBL245323 1 9.49
CHEMBL394040 1 9.47
CHEMBL245522 1 9.39
CHEMBL63686 1 9.24
CHEMBL245922 1 9.15
CHEMBL245721 1 9.03
CHEMBL246536 1 8.98
CHEMBL192 SILDENAFIL 4.0 1 8.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL245317 IC50 = 0.17 nM 9.77
CHEMBL245517 IC50 = 0.18 nM 9.74
CHEMBL63548 IC50 = 0.28 nM 9.55
CHEMBL541468 IC50 = 0.28 nM 9.55
CHEMBL67064 IC50 = 0.29 nM 9.54
CHEMBL245315 IC50 = 0.3 nM 9.52
CHEMBL245323 IC50 = 0.32 nM 9.49
CHEMBL394040 IC50 = 0.34 nM 9.47
CHEMBL245522 IC50 = 0.41 nM 9.39
CHEMBL63686 IC50 = 0.58 nM 9.24
CHEMBL245922 IC50 = 0.7 nM 9.15
CHEMBL245721 IC50 = 0.94 nM 9.03
CHEMBL246536 IC50 = 1.05 nM 8.98
CHEMBL192 SILDENAFIL IC50 = 1.78 nM 8.75