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Assay Detail

CHEMBL4419182

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

Binding
Inhibition of human PDE4D catalytic domain using [3H]-cAMP or [3H]-cGMP incubated for 30 mins by scintillation counting method
15
Total Activities
15
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

3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

FMO3 inhibitors for treating pain
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.65 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 10.70
CHEMBL193240 ROFLUMILAST 4.0 1 9.17
CHEMBL4474098 1 8.68
CHEMBL323312 1 8.62
CHEMBL4297527 REVAMILAST 2.0 1 8.57
CHEMBL4568146 ELBIMILAST 1.0 1 8.46
CHEMBL511115 CILOMILAST 3.0 1 7.96
CHEMBL2104505 1 7.52
CHEMBL332750 TETOMILAST 3.0 1 7.16
CHEMBL4297520 OGLEMILAST 2.0 1 6.78
CHEMBL362652 1 6.70
CHEMBL313842 ZARDAVERINE 2.0 1 6.41
CHEMBL404216 TOFISOPAM 2.0 1 6.05
CHEMBL590754 FILAMINAST 2.0 1 6.00
CHEMBL603830 DAXALIPRAM 2.0 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST IC50 = 0.02 nM 10.70
CHEMBL193240 ROFLUMILAST IC50 = 0.68 nM 9.17
CHEMBL4474098 IC50 = 2.1 nM 8.68
CHEMBL323312 IC50 = 2.4 nM 8.62
CHEMBL4297527 REVAMILAST IC50 = 2.7 nM 8.57
CHEMBL4568146 ELBIMILAST IC50 = 3.5 nM 8.46
CHEMBL511115 CILOMILAST IC50 = 11.0 nM 7.96
CHEMBL2104505 IC50 = 30.0 nM 7.52
CHEMBL332750 TETOMILAST IC50 = 70.0 nM 7.16
CHEMBL4297520 OGLEMILAST IC50 = 166.0 nM 6.78
CHEMBL362652 IC50 = 200.0 nM 6.70
CHEMBL313842 ZARDAVERINE IC50 = 390.0 nM 6.41
CHEMBL404216 TOFISOPAM IC50 = 900.0 nM 6.05
CHEMBL590754 FILAMINAST IC50 = 1000.0 nM 6.00
CHEMBL603830 DAXALIPRAM IC50 = 1100.0 nM 5.96