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Assay Detail

CHEMBL3860975

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

Binding
Inhibition of recombinant human PDE5A
3
Total Activities
3
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

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 3 8.38 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1520 VARDENAFIL 4.0 1 9.05
CHEMBL192 SILDENAFIL 4.0 1 8.07
CHEMBL779 TADALAFIL 4.0 1 8.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1520 VARDENAFIL IC50 = 0.89 nM 9.05
CHEMBL192 SILDENAFIL IC50 = 8.5 nM 8.07
CHEMBL779 TADALAFIL IC50 = 9.4 nM 8.03