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Assay Detail

CHEMBL989632

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

Binding
Inhibition of PDE5 in human platelets after 5 mins by LC-MS/MS analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and pharmacological evaluations of sildenafil analogues for treatment of erectile dysfunction.
Flores Toque HA, Priviero FB, Teixeira CE, Perissutti E, Fiorino F, Severino B, Frecentese F, Lorenzetti R, Baracat JS, Santagada V, Caliendo G, Antunes E, De Nucci G.
J Med Chem (2008) 51 : 2807 -2815
PubMed 18393409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.83 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL505194 1 7.42
CHEMBL498866 1 7.30
CHEMBL192 SILDENAFIL 4.0 1 7.28
CHEMBL467592 1 7.22
CHEMBL467593 1 7.16
CHEMBL513873 1 7.16
CHEMBL464131 1 7.00
CHEMBL464341 1 6.85
CHEMBL468760 1 6.82
CHEMBL494817 1 6.70
CHEMBL510554 1 6.51
CHEMBL511065 1 6.50
CHEMBL504620 1 6.43
CHEMBL507524 1 6.30
CHEMBL492795 1 6.29
CHEMBL506893 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL505194 IC50 = 38.0 nM 7.42
CHEMBL498866 IC50 = 50.0 nM 7.30
CHEMBL192 SILDENAFIL IC50 = 53.0 nM 7.28
CHEMBL467592 IC50 = 60.0 nM 7.22
CHEMBL467593 IC50 = 70.0 nM 7.16
CHEMBL513873 IC50 = 70.0 nM 7.16
CHEMBL464131 IC50 = 100.0 nM 7.00
CHEMBL464341 IC50 = 140.0 nM 6.85
CHEMBL468760 IC50 = 150.0 nM 6.82
CHEMBL494817 IC50 = 200.0 nM 6.70
CHEMBL510554 IC50 = 310.0 nM 6.51
CHEMBL511065 IC50 = 320.0 nM 6.50
CHEMBL504620 IC50 = 370.0 nM 6.43
CHEMBL507524 IC50 = 500.0 nM 6.30
CHEMBL492795 IC50 = 510.0 nM 6.29
CHEMBL506893 IC50 = 530.0 nM 6.28