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Assay Detail

CHEMBL760746

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

Binding
Inhibitory activity against phosphodiesterase 6 (PDE6) obtained from canine or bovine retina
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 6 (CHEMBL2097163)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.
Maw GN, Allerton CM, Gbekor E, Million WA.
Bioorg Med Chem Lett (2003) 13 : 1425 -1428
PubMed 12668004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.09 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282515 2 6.90
CHEMBL284070 1 6.65
CHEMBL32255 1 6.60
CHEMBL33518 1 6.57
CHEMBL33121 1 6.45
CHEMBL418594 1 6.45
CHEMBL285737 1 6.21
CHEMBL33627 1 6.09
CHEMBL286309 1 6.07
CHEMBL779 TADALAFIL 4.0 1 5.90
CHEMBL34802 1 5.87
CHEMBL33147 1 5.80
CHEMBL286905 1 5.79
CHEMBL33381 1 5.75
CHEMBL33944 1 5.58
CHEMBL30936 1 5.53
CHEMBL284594 1 5.08
CHEMBL284258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282515 IC50 = 125.0 nM 6.90
CHEMBL284070 IC50 = 226.0 nM 6.65
CHEMBL32255 IC50 = 249.0 nM 6.60
CHEMBL33518 IC50 = 271.0 nM 6.57
CHEMBL33121 IC50 = 358.0 nM 6.45
CHEMBL418594 IC50 = 357.0 nM 6.45
CHEMBL282515 IC50 = 494.0 nM 6.31
CHEMBL285737 IC50 = 620.0 nM 6.21
CHEMBL33627 IC50 = 807.0 nM 6.09
CHEMBL286309 IC50 = 846.0 nM 6.07
CHEMBL779 TADALAFIL IC50 = 1260.0 nM 5.90
CHEMBL34802 IC50 = 1340.0 nM 5.87
CHEMBL33147 IC50 = 1601.0 nM 5.80
CHEMBL286905 IC50 = 1619.0 nM 5.79
CHEMBL33381 IC50 = 1770.0 nM 5.75
CHEMBL33944 IC50 = 2660.0 nM 5.58
CHEMBL30936 IC50 = 2966.0 nM 5.53
CHEMBL284594 IC50 = 8224.0 nM 5.08
CHEMBL284258 IC50 > 10.0 nM -