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Assay Detail

CHEMBL4014054

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

Binding
Inhibition of PDE6A (484 to 817 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using [3H]cGMP or [3H]cAMP as substrate after 15 mins by liquid scintillation counting method
1
Total Activities
1
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

Publication

Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension.
Wu D, Zhang T, Chen Y, Huang Y, Geng H, Yu Y, Zhang C, Lai Z, Wu Y, Guo X, Chen J, Luo HB.
J Med Chem (2017) 60 : 6622 -6637
PubMed 28686445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.24 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4099219 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4099219 IC50 = 58.0 nM 7.24