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Assay Detail

CHEMBL4200909

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

Binding
Inhibition of PDE2A catalytic domain (580 to 919 residues) (unknown origin) expressed in Escherichia coli BL21 using 3H-cGMP as substrate after 15 mins by liquid scintillation counting
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

Target

cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL2652)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.
Wu D, Huang Y, Chen Y, Huang YY, Geng H, Zhang T, Zhang C, Li Z, Guo L, Chen J, Luo HB.
J Med Chem (2018) 61 : 8468 -8473
PubMed 30148362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.97 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4218772 1 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4218772 IC50 = 106.0 nM 6.97