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Assay Detail

CHEMBL2345121

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Binding
Inhibition of PDE11 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay
5
Total Activities
5
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

Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (CHEMBL2717)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
Fiorito J, Saeed F, Zhang H, Staniszewski A, Feng Y, Francis YI, Rao S, Thakkar DM, Deng SX, Landry DW, Arancio O.
Eur J Med Chem (2013) 60 : 285 -294
PubMed 23313637 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.61 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL779 TADALAFIL 4.0 1 8.00
CHEMBL1520 VARDENAFIL 4.0 1 6.62
CHEMBL192 SILDENAFIL 4.0 1 5.21
CHEMBL2333220 1 -
CHEMBL2333219 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL779 TADALAFIL IC50 = 10.0 nM 8.00
CHEMBL1520 VARDENAFIL IC50 = 240.0 nM 6.62
CHEMBL192 SILDENAFIL IC50 = 6100.0 nM 5.21
CHEMBL2333220 IC50 > 10000.0 nM -
CHEMBL2333219 IC50 > 10000.0 nM -