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Assay Detail

CHEMBL3861028

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

ADMET
Inhibition of recombinant PDE3A (unknown origin) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by TR-FRET assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A (CHEMBL241)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
Rabal O, Sánchez-Arias JA, Cuadrado-Tejedor M, de Miguel I, Pérez-González M, García-Barroso C, Ugarte A, Estella-Hermoso de Mendoza A, Sáez E, Espelosin M, Ursua S, Haizhong T, Wei W, Musheng X, Garcia-Osta A, Oyarzabal J.
J Med Chem (2016) 59 : 8967 -9004
PubMed 27606546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.94 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3936651 1 6.12
CHEMBL3900593 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3936651 IC50 = 750.0 nM 6.12
CHEMBL3900593 IC50 = 1800.0 nM 5.75