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Assay Detail

CHEMBL1664616

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

Binding
Inhibition of human recombinant PDE5 after 30 mins by fluorescence polarization assay
68
Total Activities
68
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 molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
Mohamed HA, Girgis NM, Wilcken R, Bauer MR, Tinsley HN, Gary BD, Piazza GA, Boeckler FM, Abadi AH.
J Med Chem (2011) 54 : 495 -509
PubMed 21189023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 6.33 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1650866 1 8.70
CHEMBL1650676 1 8.15
CHEMBL1650673 1 8.00
CHEMBL1650869 1 8.00
CHEMBL1650690 1 7.92
CHEMBL1650862 1 7.30
CHEMBL1650865 1 7.30
CHEMBL1650686 1 7.16
CHEMBL1650674 1 7.05
CHEMBL1650677 1 6.82
CHEMBL1650880 1 6.72
CHEMBL1650867 1 6.58
CHEMBL1650854 1 6.58
CHEMBL1650876 1 6.57
CHEMBL1650879 1 6.54
CHEMBL1650680 1 6.52
CHEMBL1650695 1 6.42
CHEMBL1650667 1 6.24
CHEMBL1650683 1 6.23
CHEMBL1650861 1 6.14
CHEMBL1650675 1 6.07
CHEMBL1650864 1 6.07
CHEMBL1650868 1 6.00
CHEMBL1650877 1 5.96
CHEMBL1650863 1 5.92
CHEMBL1650885 1 5.90
CHEMBL1650881 1 5.90
CHEMBL1650882 1 5.87
CHEMBL1650870 1 5.87
CHEMBL1650684 1 5.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1650866 IC50 = 2.0 nM 8.70
CHEMBL1650676 IC50 = 7.0 nM 8.15
CHEMBL1650869 IC50 = 10.0 nM 8.00
CHEMBL1650673 IC50 = 10.0 nM 8.00
CHEMBL1650690 IC50 = 12.0 nM 7.92
CHEMBL1650862 IC50 = 50.0 nM 7.30
CHEMBL1650865 IC50 = 50.0 nM 7.30
CHEMBL1650686 IC50 = 70.0 nM 7.16
CHEMBL1650674 IC50 = 90.0 nM 7.05
CHEMBL1650677 IC50 = 150.0 nM 6.82
CHEMBL1650880 IC50 = 190.0 nM 6.72
CHEMBL1650867 IC50 = 260.0 nM 6.58
CHEMBL1650854 IC50 = 260.0 nM 6.58
CHEMBL1650876 IC50 = 270.0 nM 6.57
CHEMBL1650879 IC50 = 290.0 nM 6.54
CHEMBL1650680 IC50 = 300.0 nM 6.52
CHEMBL1650695 IC50 = 380.0 nM 6.42
CHEMBL1650667 IC50 = 570.0 nM 6.24
CHEMBL1650683 IC50 = 590.0 nM 6.23
CHEMBL1650861 IC50 = 730.0 nM 6.14
CHEMBL1650675 IC50 = 850.0 nM 6.07
CHEMBL1650864 IC50 = 850.0 nM 6.07
CHEMBL1650868 IC50 = 990.0 nM 6.00
CHEMBL1650877 IC50 = 1110.0 nM 5.96
CHEMBL1650863 IC50 = 1200.0 nM 5.92
CHEMBL1650885 IC50 = 1270.0 nM 5.90
CHEMBL1650881 IC50 = 1260.0 nM 5.90
CHEMBL1650882 IC50 = 1350.0 nM 5.87
CHEMBL1650870 IC50 = 1340.0 nM 5.87
CHEMBL1650684 IC50 = 1480.0 nM 5.83
CHEMBL1649595 IC50 = 1610.0 nM 5.79
CHEMBL1650687 IC50 = 1870.0 nM 5.73
CHEMBL1650873 IC50 = 2040.0 nM 5.69
CHEMBL1650693 IC50 = 2300.0 nM 5.64
CHEMBL1650689 IC50 = 2310.0 nM 5.64
CHEMBL1650678 IC50 = 2860.0 nM 5.54
CHEMBL1650872 IC50 = 3300.0 nM 5.48
CHEMBL1650685 IC50 = 4140.0 nM 5.38
CHEMBL1650878 IC50 = 4460.0 nM 5.35
CHEMBL1650688 IC50 = 6380.0 nM 5.20
CHEMBL1650664 IC50 = 7200.0 nM 5.14
CHEMBL1650679 IC50 = 8750.0 nM 5.06
CHEMBL1650874 IC50 - -
CHEMBL1650875 IC50 - -
CHEMBL1650856 IC50 - -
CHEMBL1650855 IC50 - -
CHEMBL1650883 IC50 - -
CHEMBL1650884 IC50 - -
CHEMBL1650886 IC50 - -
CHEMBL1650887 IC50 - -