Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4425329

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

Binding
Inhibition of recombinant human PDE5A1 catalytic domain (535 to 860 residues) expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cGMP as substrate incubated for 15 mins by liquid scintillation counting method
2
Total Activities
2
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

PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
Jansen C, Kooistra AJ, Kanev GK, Leurs R, de Esch IJ, de Graaf C.
J Med Chem (2016) 59 : 7029 -7065
PubMed 26908025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.37 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4210889 1 7.77
CHEMBL1236703 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4210889 IC50 = 17.0 nM 7.77
CHEMBL1236703 IC50 = 110.0 nM 6.96